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SR-3677 Sale

(Synonyms: N-[2-[2-(二甲基氨基)乙氧基]-4-(1H-吡唑-4-基)苯基]-2,3-二氢-1,4-苯并二恶烷-2-甲酰胺) 目录号 : GC10722

A ROCK1 and ROCK2 inhibitor

SR-3677 Chemical Structure

Cas No.:1072959-67-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥792.00
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5mg
¥450.00
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10mg
¥720.00
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50mg
¥2,304.00
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100mg
¥3,960.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Kinase experiment:

Assays are performed using the STK2 kinase system from Cisbio. 5 μL mixture of a 1 μM STK2 substrate and ATP (ROCK-I: 4 μM; ROCK-II: 20 μM) in STK-buffer is added to the wells. 20 nL of test compounds (SR-3677) is dispensed. Reaction is started by addition of 5 μL of 2.5 nM. ROCK-I or 0.5 nM ROCK-II in STK-buffer. After 4 h at RT the reaction is stopped by addition of 10 μL of 1x antibody and 62.5 nM Sa-XL in detection buffer[1].

References:

[1]. Feng Y, et al. Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. J Med Chem. 2008 Nov 13;51(21):6642-5.

产品描述

SR-3677 is a novel, potent and highly selective inhibitor of Rho Kinase (ROCK-II) with the IC50 value of ~0.3nM in enzyme and cell based assays [1].

SR-3677 has been reported to selectively inhibit the ROCK- II with the IC50 values of ~3nM, ~3nM, 56nM, 3.968μM,1.190μM and 7.491μM for ROCK-II,ppMLC, ROCK-I, PKA, MRCK and Akt1, respectively. In addition, SR-3677 has been shown several key binding elements that contribute to the high potency and selectivity in the docking assay. Furthermore, SR-3677 has been revealed to be efficacious in enhancing aqueous humor outflow and in target modulation in the pharmacology studies [1].

References:
[1] Feng Y1, Yin Y, Weiser A, Griffin E, Cameron MD, Lin L, Ruiz C, Schürer SC, Inoue T, Rao PV, Schröter T, Lograsso P. Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. J Med Chem. 2008 Nov 13;51(21):6642-5. doi: 10.1021/jm800986w. Epub 2008 Oct 4.

Chemical Properties

Cas No. 1072959-67-1 SDF
别名 N-[2-[2-(二甲基氨基)乙氧基]-4-(1H-吡唑-4-基)苯基]-2,3-二氢-1,4-苯并二恶烷-2-甲酰胺
化学名 N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxine-3-carboxamide
Canonical SMILES CN(C)CCOC1=C(C=CC(=C1)C2=CNN=C2)NC(=O)C3COC4=CC=CC=C4O3
分子式 C22H24N4O4 分子量 408.45
溶解度 DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 5 mg/ml 储存条件 Store at -20°C
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1 mM 2.4483 mL 12.2414 mL 24.4828 mL
5 mM 0.4897 mL 2.4483 mL 4.8966 mL
10 mM 0.2448 mL 1.2241 mL 2.4483 mL
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