Melatonin

別名：NSC 56423, N-Acetyl-5-methoxytryptamine,NSC 113928,MT

製品コード：S1204 純度：99.95%

Melatonin is a MT receptor agonist, used as a dietary supplement. Melatonin is a selective ATF-6 inhibitor and downregulates COX-2. Melatonin enhances mitophagy and regulates the homeostasis of apoptosis and autophagy.

CAS No. 73-31-4

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
50mg	JPY 22000	国内在庫あり
1g	JPY 55500	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（30）

カスタマーフィードバック4例

製品安全説明書

現在のバッチを見る：純度： 99.95%

99.95

Melatonin関連製品

関連ターゲット	MT1 receptor MT2 receptor	もっと見る
関連製品	Luzindole	もっと見る
関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I GPCR Compound Library	もっと見る

シグナル伝達経路

MT Receptorシグナル伝達経路

MT Receptor阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
PC12	Neuroprotective assay	25 uM	2 hrs	Neuroprotective activity against H2O2-induced oxidative damage in rat PC12 cells assessed as increase in cell viability at 25 uM preincubated for 2 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay	28800459
PC12	Neuroprotective assay	20 uM	24 hrs	Neuroprotective activity against amyloid beta (1 to 42 residues) induced cell death in rat PC12 cells assessed as increase in cell viability at 20 uM preincubated for 24 hrs followed by amyloid beta (1 to 42 residues) addition measured after 24 hrs by MTT	27484514
PC12	Neuroprotective assay	10 uM	2 hrs	Neuroprotective activity against H2O2-induced damage in rat PC12 cells assessed as cell viability at 10 uM preincubated for 2 hrs followed by H2O2 addition for 24 hrs by MTT assay	27460699
SH-SY5Y	Neuroprotective assay	10 uM	24 hrs	Neuroprotective activity against H2O2-induced oxidative stress-associated death in human SH-SY5Y cells assessed as increase in cell viability at 10 uM incubated for 24 hrs prior to H2O2 challenge measured after 24 hrs by MTT assay	26363866
Primary neural stem cells	Neurogenic assay	10 uM	48 hrs	Neurogenic activity in Wistar rat Primary neural stem cells assessed as cell maturation by measuring MAP-2 at 10 uM after 48 hrs by DAPI staining-based immunohistochemistry	24738476
Primary neural stem cells	Neurogenic assay	10 uM	48 hrs	Neurogenic activity in Wistar rat Primary neural stem cells assessed as cell maturation by measuring TuJ1 at 10 uM after 48 hrs by DAPI staining-based immunohistochemistry	24738476
NIH3T3	Function assay	1 nM		Activity at MT1 receptor expressed in NIH3T3 cells assessed as inhibition of forskolin-stimulated cAMP synthesis at 1 nM	16759094
CHO	Function assay		1 hr	Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in CHO cells incubated for 1 hr by gamma counting method, Ki=0.00095μM	31727472
COS7	Function assay		1.5 hrs	Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method, Ki=0.00088μM	31727472
CHO	Function assay		1 hr	Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting method, Ki=0.00046μM	31727472
NIH3T3	Function assay		90 mins	Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis, Ki=0.0002042μM	31727472
NIH3T3	Function assay		90 mins	Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis, Ki=0.000302μM	31727472
COS7	Function assay		1.5 hrs	Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method, Ki=0.00018μM	31727472
MDA-MB-231	Antiproliferative assay		24 hrs	Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=0.9μM	29144746
CHO	Function assay		60 mins	Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method, IC50=0.00011μM	27876250
HEK293	Function assay		120 mins	Displacement of [125I]2-Iodomelatonin from human MT2 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay, Ki=0.00034μM	26785296
HEK293	Function assay		120 mins	Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay, Ki=0.00025μM	26785296
HEK293	Function assay		120 mins	Displacement of 2-[125I]iodomelatonin from human MT2 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting, Ki=0.00041μM	25232966
HEK293	Function assay		120 mins	Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting, Ki=0.00014μM	25232966
CHO	Function assay		1 hr	Intrinsic activity at human melatonin MT1 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr, EC50=0.0017μM	24417958
CHO	Function assay		1 hr	Intrinsic activity at human melatonin MT2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr, EC50=0.0004μM	24417958
CHOK1	Function assay		3 hrs	Displacement of [125I]2-iodomelatonin from human recombinant melatonin receptor 1 expressed in CHOK1 cells after 3 hrs, IC50=0.00021μM	23403082
CHOK1	Function assay		3 hrs	Displacement of [125I]2-iodomelatonin from human recombinant melatonin receptor 1 expressed in CHOK1 cells after 3 hrs, Ki=0.00011μM	23403082
HEK293	Function assay		2 hrs	Displacement of [125I]2-iodomelatonin from human recombinant MT2 receptor expressed in HEK293 cells after 2 hrs by gamma counting, Ki=0.0005μM	23265885
HEK293	Function assay		2 hrs	Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting, Ki=0.0002μM	23265885
CHO	Function assay		60 mins	Displacement of [3H]melatonin from human MT2 receptor expressed in CHO cells after 60 mins by microbeta scintillation method, Ki=0.000429μM	23228808
CHO	Function assay		60 mins	Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method, Ki=0.000296μM	23228808
NIH3T3	Function assay		90 mins	Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.0003388μM	22047556
NIH3T3	Function assay		90 mins	Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.000263μM	22047556
CHO	Function assay		30 mins	Agonist activity at human MT2 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader, EC50=0.00082μM	21568291
CHO	Function assay		30 mins	Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader, EC50=0.000026μM	21568291
CHO	Function assay		30 mins	Agonist activity at human MT2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers, EC50=0.0008511μM	21473625
CHO	Function assay		30 mins	Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers, EC50=0.0000257μM	21473625
CHO-Galpha16	Function assay		20 mins	Binding affinity to rat MT2 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay, EC50=0.0011μM	21237644
CHO-Galpha16	Function assay		20 mins	Binding affinity to rat MT1 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay, EC50=0.00056μM	21237644
NIH3T3	Function assay		90 mins	Displacement of [125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.0006166μM	20674373
NIH3T3	Function assay		90 mins	Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.0003311μM	20674373
CHO	Function assay		60 mins	Displacement of [3H]melatonin from human melatonin MT2 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki=0.000429μM	20227878
CHO	Function assay		60 mins	Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki=0.000296μM	20227878
CHO	Function assay		1 hr	Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis, Ki=0.0004571μM	ChEMBL
CHO	Function assay		1 hr	Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT2 expressed in CHO cells after 1 hr by gamma counting analysis, Ki=0.000955μM	ChEMBL
NIH3T3	Function assay			Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assay, Ki=0.00066μM	31727472
NIH3T3	Function assay			Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in NIH3T3 cells membranes by radioligand binding assay, Ki=0.00033μM	31727472
HEK293	Function assay			Agonist activity at MT2 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay, EC50=0.025μM	31204226
HEK293	Function assay			Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay, EC50=0.001μM	31204226
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
CHO	Function assay			Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells, IC50=0.00011μM	26988801
HEK293	Function assay			Displacement of [125L]iodomelatonin from human MT2 receptor expressed in HEK293 cells, Ki=0.00041μM	24930835
HEK293	Function assay			Displacement of [125L]iodomelatonin from human MT1 receptor expressed in HEK293 cells, Ki=0.00014μM	24930835
HEK293	Function assay			Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in human HEK293 cells by radioligand binding assay, Ki=0.00034μM	21764185
HEK293	Function assay			Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay, Ki=0.00025μM	21764185
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.00024μM	21568291
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.00021μM	21568291
CHO	Function assay			Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting, Ki=0.00024μM	21473625
CHO	Function assay			Displacement of [125I]-2-iodomelatonin from human MT2 receptor expressed on CHO cells microscintillation counting, Ki=0.00021μM	21473625
CHO	Function assay			Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.0015μM	21420861
CHO	Function assay			Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.00042μM	21420861
HEK293	Function assay			Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in HEK293 cells, Ki=0.00034μM	21420861
HEK293	Function assay			Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells, Ki=0.00025μM	21420861
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.00035μM	21392858
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.00022μM	21392858
CHO-Galpha16	Function assay			Displacement of [3H]melatonin from rat MT1 receptor expressed in CHO-Galpha16 cells, Ki=0.00099μM	21237644
CHO-Galpha16	Function assay			Displacement of [3H]melatonin from rat MT2 receptor expressed in CHO-Galpha16 cells, Ki=0.00058μM	21237644
CHO	Function assay			Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.0022μM	20444610
CHO	Function assay			Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.00049μM	20444610
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting, Ki=0.0004571μM	19473848
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells by gamma counting, Ki=0.000955μM	19473848
CHO	Function assay			Agonist activity at human MT1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding, EC50=0.00224μM	19329323
CHO	Function assay			Agonist activity at human MT2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding, EC50=0.00049μM	19329323
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.000955μM	19193160
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.0004571μM	19193160
CHO	Function assay			Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay, EC50=0.00049μM	18778943
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.00041μM	18778943
HEK293	Function assay			Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells, Ki=0.00014μM	18778943
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human melatonin MT2 receptor expressed in CHO cells, Ki=0.000741μM	18657980
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells, Ki=0.000525μM	18657980
CHO	Function assay			Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells, IC50=0.06457μM	18400335
HEK293	Function assay			Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in HEK293 cells, IC50=0.00053μM	18372181
HEK293	Function assay			Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells, IC50=0.0002μM	18372181
NIH3T3	Function assay			Displacement of 2-[125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells, Ki=0.0002399μM	18052314
NIH3T3	Function assay			Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells, Ki=0.0001413μM	18052314
NIH3T3	Function assay			Displacement of 2-[125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells, Ki=0.0003μM	17481904
NIH3T3	Function assay			Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells, Ki=0.0002μM	17481904
NIH3T3	Function assay			Displacement of 2[125I]iodomelatonin from human recombinant MT2 receptor expressed in NIH3T3 cells, Ki=0.0003388μM	17459711
NIH3T3	Function assay			Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells, Ki=0.000263μM	17459711
NIH 3T3	Function assay			Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells, Ki=0.000389μM	17346859
NIH 3T3	Function assay			Displacement of 2[125I]iodomelatonin from recombinant human MT2 receptor expressed in NIH 3T3 cells, Ki=0.0003548μM	17346859
NIH3T3	Function assay			Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in NIH3T3 cells, Ki=0.000257μM	17149869
NIH3T3	Function assay			Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells, Ki=0.0003236μM	17149869
NIH3T3	Function assay			Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells, Ki=0.00039μM	16759094
NIH3T3	Function assay			Displacement of 2-[125I]iodomelatonin from human recombinant MT2 receptor expressed in NIH3T3 cells, Ki=0.00035μM	16759094
NIH3T3	Function assay			Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1B (MT2) expressed in NIH3T3 rat fibroblast cells , Ki=0.0002818μM	15943478
NIH3T3	Function assay			Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells, Ki=0.0002884μM	15943478
NIH3T3	Function assay			Binding affinity against Melatonin receptor type 1B stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin, Ki=0.0007μM	15713384
NIH3T3	Function assay			Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin, Ki=0.0003μM	15713384
NIH3T3	Function assay			Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1B, Ki=0.0007μM	15380218
NIH3T3	Function assay			Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells, Ki=0.0002884μM	15293992
NIH3T3	Function assay			Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A, Ki=0.0003μM	15380218
NIH3T3	Function assay			Binding affinity for human recombinant Melatonin receptor type 2 expressed in NIH3T3 cells, Ki=0.0002818μM	15293992
NIH3T3	Function assay			Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A, Ki=0.0004μM	14980664
NIH3T3	Function assay			Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1B, Ki=0.0003μM	14980664
NIH3T3	Function assay			Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells., Ki=0.0004μM	14643330
NIH3T3	Function assay			Binding affinity against human MT2 melatonin receptor expressed in NIH3T3 cells, Ki=0.0003μM	14643330
HEK293	Function assay			Binding affinity for human Melatonin receptor type 1B stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand, Ki=0.00041μM	12646022
HEK293	Function assay			Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand, Ki=0.00014μM	12646022
CHO	Function assay			Binding affinity against human Melatonin receptor type 1A (MT1) in CHO cells, Ki=0.0000823μM	12213063
CHO	Function assay			Ability to inhibit 2-[125I]iodomelatonin specific binding to human melatonin receptor type 1A (MT1) expressed in CHO cells., Ki=0.0000823μM	12213062
CHO	Function assay			Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A, EC50=0.00192μM	12061881
CHO	Function assay			Intrinsic activity at human Melatonin receptor type 1B evaluated on [35S]GTP-gamma-S, binding in Chinese hamster ovarian (CHO) cells, EC50=0.00047μM	12061881
HEK293	Function assay			Binding affinity on human melatonin receptor type 1B stably transfected in human embryonic kidney (HEK 293) cells using 2-[125I]iodomelatonin as radioligand., Ki=0.00031μM	12061881
HEK293	Function assay			Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in HEK293 cells, Ki=0.00031μM	11960497
HEK293	Function assay			Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells, Ki=0.00012μM	11960497
NIH 3T3	Function assay			Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand, Ki=0.0002884μM	11520198
NIH 3T3	Function assay			Binding affinity towards melatonin receptor type 1B stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin, Ki=0.0002818μM	11520198
HEK293	Function assay			Binding affinity for melatonin receptor type 1B, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand), Ki=0.00053μM	11063602
HEK293	Function assay			Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand), Ki=0.0002μM	11063602
NIH 3T3	Function assay			Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay, Ki=0.00066μM	10737738
NIH 3T3	Function assay			Binding affinity towards recombinant human melatonin receptor type 1B expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay, Ki=0.00033μM	10737738
NIH3T3	Function assay			Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells, Ki=0.0002951μM	9733487
CHO	Function assay			Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells, Ki=0.00008μM	9435890
CHO	Function assay			Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1B expressed in CHO cells, Ki=0.00012μM	9435890
CHO	Function assay			Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells, Ki=0.00013μM	ChEMBL
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells, Ki=0.0002μM	ChEMBL
CHO	Function assay			Binding affinity against human Melatonin receptor type 1B by displacement of [125I]iodomelatonin stably expressed in CHO cells, Ki=0.00023μM	ChEMBL
CHO	Function assay			Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in CHO cells, Ki=0.00029μM	ChEMBL
CHO	Function assay			Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.0004571μM	ChEMBL
CHO	Function assay			Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells by Gamma counting, Ki=0.0004571μM	ChEMBL
CHO	Function assay			Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.000955μM	ChEMBL
CHO	Function assay			Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in CHO cells by Gamma counting, Ki=0.000955μM	ChEMBL
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生物活性

製品説明

Targets

melatonin receptor ^[1]

In Vitro
In vitro	Melatonin interacts with the highly toxic hydroxyl radical with a rate constant equivalent to that of other highly efficient hydroxyl radical scavengers. Melatonin reportedly neutralizes hydrogen peroxide, singlet oxygen, peroxynitrite anion, nitric oxide and hypochlorous acid. ^[1] Melatonin is believed to scavenge the highly toxic hydroxyl radical, the peroxynitrite anion, and possibly the peroxyl radical. Melatonin reportedly scavenges the superoxide anion radical and it quenches singlet oxygen. Melatonin stimulates mRNA levels for superoxide dismutase and the activities of glutathione peroxidase, glutathione reductase and glucose-6-phosphate dehydrogenase (all of which are antioxidative enzymes), thereby increasing its antioxidative capacity. ^[2] Melatonin in cell-free systems has been shown to directly scavenge H2O2, singlet oxygen (1O2) and nitric oxide (NO), with little or no ability to scavenge the superoxide anion radical (O2-) in vitro. Melatonin also directly detoxifies the peroxynitrite anion (ONOO-) and/or peroxynitrous acid (ONOOH), or the activated form of this molecule, ONOOH*. Melatonin acts as a direct free radical scavenger with the ability to detoxify both reactive oxygen and reactive nitrogen species. ^[3] Melatonin inhibits cAMP accumulation in most of the cells examined, but the indole effects on other messengers have been often observed only in one type of the cells or tissue, until now. Melatonin also regulates the transcription factors, namely, phosphorylation of cAMP-responsive element binding protein and expression of c-Fos. ^[4]
細胞実験	細胞株	HepG2 cells
	濃度	1.2 mM
	反応時間	24 h
	実験の流れ	Cells were treated with various concentrations of drug for 24 h.
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Western blot	MT1 / MT2 / p-CREB / CREB / BDNF p-Raf / p-ERK / p-p90RSK / PKAα / p-AKT / p-JNK / p-CaMKII		29570621

In Vivo
In Vivo	Melatonin ameliorates necrotizing enterocolitis by preventing Th17/Treg imbalance through activation of the AMPK/SIRT1 pathway
動物実験	動物モデル	C57BL/6 mice
	投与量	10 mg/kg
	投与経路	i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT04521972	Not yet recruiting	Pregnancy Related\|Labor; Poor\|Uterine Contractions Weak	Michigan State University\|McLaren Health Care	October 1 2024	Not Applicable
NCT06390267	Not yet recruiting	Acute Stress Reaction\|Cognitive Performance	Spark Biomedical Inc.\|Battelle Memorial Institute	August 2024	Not Applicable
NCT06343805	Not yet recruiting	Primary Myelofibrosis\|Post-Essential Thrombocythemia Myelofibrosis\|Post-Polycythemia Vera Myelofibrosis\|PMF\|PPV-MF\|PET-MF	Ajax Therapeutics Inc.	July 15 2024	Phase 1

参考
[1] Reiter RJ, et al. J Biomed Sci, 2000, 7(6), 444-458. [2] Reiter RJ, et al. Prog Neurobiol, 1998, 56(3), 359-384. [3] Reiter RJ, et al. Cell Biochem Biophys, 2001, 34(2), 237-256. [4] Vanecek J, et al. Physiol Rev, 1998, 78(3), 687-721. [5] Bai L, et al. Front Pharmacol. 2022 Sep 26;13:1007006. [6] Ma F, et al. Theranostics. 2020 Jun 19;10(17):7730-7746. + 展開

参考

+ 展開

化学情報

分子量	232.28	化学式	C₁₃H₁₆N₂O₂
CAS No.	73-31-4	SDF	Download Melatonin SDFをダウンロードする
Smiles	CC(=O)NCCC1=CNC2=C1C=C(C=C2)OC
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 47 mg/mL ( (202.34 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 47 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):