Nicotinamide

別名：Niacinamide, Vitamin PP, Nicotinic acid amide, Vitamin B3, NSC 27452,NSC 13128

製品コード：S1899 純度：99.98%

Nicotinamide, a water-soluble vitamin, is an active component of coenzymes NAD and NADP, and also act as an inhibitor of sirtuins.

CAS No. 98-92-0

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
100mg	JPY 37000	国内在庫あり
1g	JPY 104500	国内在庫あり
5g	JPY 208500	国内在庫なし(納期7~10日)

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（43）

製品安全説明書

現在のバッチを見る：純度： 99.98%

99.98

Nicotinamide関連製品

関連ターゲット	SIRT1 SIRT2 SIRT3 SIRT6 SIRT5	もっと見る
関連製品	Selisistat (EX 527) SRT1720 HCl Sirtinol Quercetin Fisetin 3-TYP AGK2 OSS_128167 SRT2104 (GSK2245840) SirReal2 Thiomyristoyl Salvianolic acid B SRT2183 UBCS039 Salermide SRT3025 HCl AK 7 NRD167 Inauhzin CAY10602	もっと見る
関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Apoptosis Compound Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

Sirtuinシグナル伝達経路

Sirtuin阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
SK-MEL-28	Function assay	100 uM	24 hrs	Reduction in ATP level in human SK-MEL-28 cells at 100 uM maintained in Locke's solution after 24 hrs by luciferase-based assay in absence of GF and glucose	22835719
HEK293T	Function assay		60 mins	Inhibition of StrepTag-tagged human SARM1 TIR (561 to 724 residues) expressed in HEK293T cells assessed as reduction in NADase activity in presence of NAD+ incubated for 60 mins by HPLC analysis, IC50=43.8μM.	ChEMBL
BL21(DE3)	Function assay			Inhibition of recombinant Schistosoma mansoni sirtuin 2 (21 to 322 residues) expressed in Escherichia coli BL21(DE3) cells in presence of (Z)-(Oct)Lys-AMC	31496251
BL21(DE3)	Function assay			Inhibition of recombinant Schistosoma mansoni sirtuin 2 (21 to 322 residues) expressed in Escherichia coli BL21(DE3) cells in presence of (Z)-(But)Lys-AMC	31496251
BL21(DE3)	Function assay			Inhibition of recombinant Schistosoma mansoni sirtuin 2 (21 to 322 residues) expressed in Escherichia coli BL21(DE3) cells in presence of (Z)-(Hex)Lys-AMC	31496251
BL21(DE3)	Function assay			Inhibition of recombinant Schistosoma mansoni sirtuin 2 (21 to 322 residues) expressed in Escherichia coli BL21(DE3) cells in presence of ZMAL	31496251
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
BL21(DE3)	Function assay			Inhibition of recombinant Schistosoma mansoni sirtuin 2 (21 to 322 residues) expressed in Escherichia coli BL21(DE3) cells assessed as inhibition of substrate deacetylation using ZMAL as substrate, IC50=23.1μM.	31496251
BL21 (DE3)	Function assay			Inhibition of full length human SIRT2 expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay, IC50=10.5μM.	25275824
BL21 (DE3)	Function assay			Inhibition of catalytically active human SIRT3 (102 to 399 amino acids) expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay, IC50=6.2μM.	25275824
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生物活性

製品説明

Nicotinamide, a water-soluble vitamin, is an active component of coenzymes NAD and NADP, and also act as an inhibitor of sirtuins.

Targets

Sirtuin ^[1]

In Vitro
In vitro	Nicotinamide strongly inhibits yeast silencing, increases rDNA recombination, and shortens replicative life span to that of a sir2 mutant. Nicotinamide abolishes silencing and leads to an eventual delocalization of Sir2 even in G(1)-arrested cells, demonstrating that silent heterochromatin requires continual Sir2 activity. ^[1] Nicotinamide results in a twofold increase in DNA content and a threefold increase in insulin content in the fetal cells. Nicotinamide induces differentiation and maturation of human fetal pancreatic islet cells. ^[2] Nicotinamide regulates sirtuins by switching between deacetylation and base exchange. Nicotinamide switching is quantitated for the Sir2s from Archeaglobus fulgidus (Sir2Af2), Saccharomyces cerevisiae (Sir2p), and mouse (Sir2alpha). ^[3] Nicotinamide selectively reduces a specific phospho-species of tau (Thr231) that is associated with microtubule depolymerization in Alzheimer's disease transgenic mice, in a manner similar to inhibition of SirT1. Nicotinamide also dramatically increases acetylated alpha-tubulin, a primary substrate of SirT2, and MAP2c in Alzheimer's disease transgenic mice, both of which are linked to increased microtubule stability. ^[4] Nicotinamide fosters DNA integrity and maintains phosphatidylserine membrane asymmetry to prevent cellular inflammation, cellular phagocytosis and vascular thrombosis. Nicotinamide both prevents and reverses neuronal and vascular cell injury. ^[5]
細胞実験	細胞株	HaCaT cells
	濃度	33 μM
	反応時間	7 days and 14 days
	実験の流れ	The established cell line of human epidermal keratinocytes (HaCaT cells) was routinely cultured in Dulbecco's modified Eagle medium (DMEM) containing 10% fetal bovine serum and kept in a humidified atmosphere containing 5% CO2 at 37°C. For NAD(P) modulation, cells were grown in DMEM and 10% dialyzed fetal bovine serum and with addition of 33 μM nicotinamide (33 μM Nam) or without added nicotinamide (0 μM Nam). Cell number was measured by counting. Sensitivity to glutaminase inhibition was performed using 0.1 μM 6-diazo-5-oxo-L-norleucine (DON) on cells grown in 33 μM Nam or 0 μM Nam for 7 days.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	p-MLC / MLC / p-MYPT1 / MYPT1 p-β-catenin / β-catenin Sp1 / ERK		30503259
	Immunofluorescence	p-MLC		30503259

In Vivo
In Vivo	In the mouse, nicotinamide given i.p. at doses of 100-500 mg/kg showed biphasic elimination with dose-dependent changes in half-life. The initial half-life increased significantly (P <0.05) from 0.8 to 2 h and the terminal half-life increased from 3.4 to 5.6 h over the dose range studied. Clearance, however, decreased significantly from 0.3 to 0.24 L/kg/h only at the highest dose. Peak concentrations increased in a dose-dependent manner from 1,000 to 4,800 nmol/ml. The bioavailability given via the i.p. as compared with the i. v. route was close to 100%^[6].
動物実験	動物モデル	Mice (strain CBA/Ht/GyfBSVS)
	投与量	100, 200, 300 and 500 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)
NCT06280482	Recruiting	Smooth Muscle Dysfunction Syndrome (SMDS)	The University of Texas Health Science Center Houston	March 6 2024	Phase 1
NCT05938036	Not yet recruiting	Acute Respiratory Distress Syndrome (ARDS)	Aqualung Therapeutics Corp.	January 14 2024	Phase 2
NCT06249581	Active not recruiting	Chronic Stable Angina	Auxilius Pharma sp.z.o.o.	November 27 2023	Early Phase 1
NCT06036355	Not yet recruiting	Postoperative Prevention of Tumor	Shanghai Cell Therapy Group Co.Ltd	September 30 2023	Early Phase 1

参考
[1] Bitterman KJ, et al. J Biol Chem, 2002, 277(47), 45099-45107. [2] Otonkoski T, et al. J Clin Invest, 1993, 92(3), 1459-1466. [3] Sauve AA, et al. Biochemistry, 2003, 42(31), 9249-9256. [4] Green KN, et al. J Neurosci, 2008, 28(45), 11500-11510. [5] Maiese K, et al. Trends Pharmacol Sci, 2003, 24(5), 228-232. [6] Stratford MR, et al. Cancer Chemother Pharmacol. 1994, 34(5):399-404. [7] Benavente CA, et al. Free Radic Biol Med. 2008, 44(4):527-37. + 展開

参考

+ 展開

化学情報

分子量	122.12	化学式	C₆H₆N₂O
CAS No.	98-92-0	SDF	Download Nicotinamide SDFをダウンロードする
Smiles	C1=CC(=CN=C1)C(=O)N
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ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 24 mg/mL ( (196.52 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。)

Water : 24 mg/mL

Ethanol : 24 mg/mL

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。

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