SCH58261

製品コード：S8104 純度：99.77%

SCH 58261 is a potent and selective A2a adenosine receptor antagonist with K_i of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively.

CAS No. 160098-96-4

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫なし(納期7~10日)
5mg	JPY 22000	国内在庫あり
25mg	JPY 56500	国内在庫あり
100mg	JPY 145500	国内在庫なし(納期7~10日)
1g	JPY 598500	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（7）

製品安全説明書

現在のバッチを見る：純度： 99.77%

99.77

SCH58261関連製品

関連ターゲット	Adenosine A1 receptor	もっと見る
関連製品	Reversine CGS 21680 HCl ZM241385 A2AR antagonist 1 Ciforadenant (CPI-444) Imaradenant (AZD4635)	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 Bioactive Compound Library-Ⅱ GPCR Compound Library	もっと見る

Adenosine Receptor阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
HEK293	Function assay	100 nM	24 hrs	Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP accumulation at 100 nM after 24 hrs (Rvb= 0.40 pmol/ml)	20303771
HEK293	Function assay	1 uM	15 mins	Antagonist activity at human A2A receptor expressed in HEK293 cells assessed as decrease in NECA-induced cAMP release at 1 uM after 15 mins	23953686
HEK293	Function assay		60 mins	Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis, Ki = 0.0006 μM.	23200243
CHO	Function assay		60 mins	Displacement of [3H]-ZM 241385 from human adenosine A2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting, Ki = 0.0011 μM.	22204739
HEK293	Function assay		60 mins	Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by rapid filtration assay, Ki = 0.00123 μM.	20303771
HEK293	Function assay		60 mins	Competitive binding affinity to human adenosine A2A receptor expressed in HEK293 cells after 60 mins by fluorescence polarization assay in presence of MRS5346, Ki = 0.0019 μM.	23200243
CHO	Function assay		120 mins	Displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in CHO cells after 120 mins by liquid scintillation counting, Ki = 0.549 μM.	22204739
HEK293	Function assay		60 mins	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in HEK293 cells after 60 mins by rapid filtration assay, Ki = 0.5941 μM.	20303771
CHO	Function assay		120 mins	Displacement of [3H]-MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cells after 120 mins by liquid scintillation counting, Ki = 10 μM.	22204739
HEK293	Function assay		60 mins	Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins, Ki = 10 μM.	22204739
CHO	Function assay			Displacement of [3H]-SCH- 58261 from human Adenosine A2A receptor expressed in CHO cells, Ki = 0.0011 μM.	9622554
HEK293	Function assay			Displacement of specific [3H]-SCH- 58261 binding at human Adenosine A2A receptor expressed in HEK293 cells., Ki = 0.0011 μM.	11754583
CHO	Function assay			Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells, Ki = 0.0011 μM.	19501513
CHO	Function assay			Displacement of [3H]CHA from human Adenosine A1 receptor expressed in CHO cells, Ki = 0.549 μM.	9622554
CHO	Function assay			Displacement of specific [3H]DPCPX binding at human Adenosine A1 receptor expressed in CHO cells., Ki = 0.549 μM.	11754583
HEK293	Function assay			Displacement of [3H]-AB MECA from human Adenosine A3 receptor expressed in HEK293 cells, Ki = 1 μM.	12646033
HEK293	Function assay			Displacement of [125I]AB-MECA from human Adenosine A3 receptor expressed in HEK293 cells, Ki = 10 μM.	9622554
HEK293	Function assay			Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells., Ki = 10 μM.	11754583
CHO	Function assay			Displacement of specific [3H]MRE3008-F20 binding at human adenosine A3 receptor expressed in CHO cells., Ki = 10 μM.	11754583
CHO	Function assay			Displacement of [3H]NECA from human adenosine A3 receptor expressed in CHO cells, Ki = 10 μM.	19501513
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生物活性

製品説明

SCH 58261 is a potent and selective A2a adenosine receptor antagonist with K_i of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively.

Targets

bovine A2a ^[1]	rat A2a ^[1]
2.0 nM(Ki)	2.3 nM(Ki)

In Vitro
In vitro	SCH 58261 causes the inhibition of rabbit platelet aggregation and porcine coronary artery relaxation by antagonizing competitively the effects induced by CGS 21680. ^[1]
Kinase Assay	Receptor binding assay
Kinase Assay	Rat brain tissues (cortex and striatum) are obtained from male Sprague-Dawley rats weighing 250 to 300 g. Bovine brain tissues (frontal cortex and striatum) are obtained from a local abattoir within 10 mm from animal sacrifice. A1 and A2a ADO receptor binding assays are performed using [³H]CHA and [³H]CGS 21680 [³H]2-[4-(2-carboxyethyl)-phenethylamino]- 5’-N-ethylcarboxamidoadenosinel as radioligands, respectively. Binding assay to CHO cells stably transfected with the rat brain A3 ADO receptor is performed using [¹²⁵I]AB-MECA as radioligand. In order to determine the type of inhibition (competitive or noncompetitive), saturation experiments at A1 ADO ([³H]CHA, 0.125-64 nM) and A2a ADO receptors ([³HJCGS 21680, 1-128 aM) are carried out on rat brain tissues in the absence or in the presence of different concentrations of SCH 58261 (7-(2-phenylethyl)-5-amino-2-(2-furyl)-pyrazolo-[4,3-e]-1,2,4- triazolo[1,5-c]pyrimidine}. The affinity of SCH 58261 for several neurotransmitter binding sites, such as alpha-1, alpha-2 and beta-1 adrenoceptors, D1 and D2 dopamine receptors, 5-HT1 and 5-HT2 receptors, M1 and M2 muscarinic receptors, mu-opioid, benzodiazepine and N-methyl-D-aspartate receptors, is measured according to standard methods.

In Vivo
In Vivo	In mice with Spinal cord injury, SCH58261 (0.01 mg/kg, i.p.) reduces demyelination and levels of TNF-α, Fas-L, PAR, Bax expression and activation of JNK MAPK. Chronic SCH58261 administration improves the neurological deficit up. ^[2] In rats with 6-OHDA-induced Parkinson's disease, SCH58261 (2 mg/kg, i.p.) improves the 6-OHDA-induced bradykinesia and motor disturbance. ^[3]
動物実験	動物モデル	Mice with Spinal cord injury
	投与量	0.01 mg/kg
	投与経路	i.p.

参考
[1] Zocchi C, et al. J Pharmacol Exp Ther. 1996, 276(2), 398-404. [2] Paterniti I, et al. J Neuroinflammation. 2011, 8, 31. [3] Reyhani-Rad S, et al. Acta Cir Bras. 2016, 31(2), 133-137. [4] Hou X, et al. PPAR Res. 2020 Mar 6;2020:2410264. + 展開

参考

[4] Hou X, et al. PPAR Res. 2020 Mar 6;2020:2410264.

+ 展開

化学情報

分子量	345.36	化学式	C₁₈H₁₅N₇O
CAS No.	160098-96-4	SDF	Download SCH58261 SDFをダウンロードする
Smiles	C1=CC=C(C=C1)CCN2C3=C(C=N2)C4=NC(=NN4C(=N3)N)C5=CC=CO5
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 : 69 mg/mL ( (199.79 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 : Insoluble

Ethanol : 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
	Clear solution	5% DMSO 1 95% Corn oil	0.4mg/ml (1.16mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	1.15mg/ml (3.33mM)	Taking the 1 mL working solution as an example, add 50 μL of 23 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	1.15mg/ml (3.33mM)	Taking the 1 mL working solution as an example, add 50 μL of 23 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	4%DMSO 1 40%PEG300 2 4%Tween80 3 52%ddH2O	2.0mg/ml (5.79mM)	Taking the 1 mL working solution as an example, add 40 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 40 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 520 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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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