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CAS No.: 874119-56-9

GSK-25 Catalog No. CSN25217

GSK-25 is a ROCK1 inhibitor with IC50 value of 6nM. It showed oral bioavailability (49% in rat and 19% in monkey), good half-life (1.8 h in rat and 2.2 h in monkey) and gave a robust 25 mmHg reduction mean arterial pressure in spontaneously hypertensive rats at a single dose of 30 mg/kg.

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生物活性

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技术信息

生物活性

描述Rho-associated kinase isoform 1 (ROCK1) is an enzymeinvolved in diverse cellular signaling functions such as smooth muscle contraction, cytoskeleton rearrangement, cell migration, and proliferation ^[1]. GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor which maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC₅₀=398 nM, p70S6K IC₅₀=1000 nM), and adramatically improves P450 profile (>2.2μM at all isozymestested). GSK-25 has promising oral bioavailability (49% in rats and 19% in monkey), good half-life (1.8 h in rat and 2.2 h in monkey). A spontaneously hypertensive rat (SHR) model of hypertension was treated with GSK-25 by single dose oral gavage. GSK-25 (30 mg/kg; p.o.; 3 hr) induces a 25 mmHg drop in blood pressure, thus demonstrating potent in vivo activityfor the series ^[1].
参考文献

[1] Sehon CA, Wang GZ, Viet AQ, Goodman KB, Dowdell SE, Elkins PA, Semus SF, Evans C, Jolivette LJ, Kirkpatrick RB, Dul E, Khandekar SS, Yi T, Wright LL, Smith GK, Behm DJ, Bentley R, Doe CP, Hu E, Lee D. Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic agents for cardiovascular diseases. J Med Chem. 2008 Nov 13;51(21):6631-4. doi: 10.1021/jm8005096. Epub 2008 Oct 9. PMID: 18842034.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9481 mL
- 9.7404 mL
- 19.4808 mL
- 5 mM
- 0.3896 mL
- 1.9481 mL
- 3.8962 mL
- 10 mM
- 0.1948 mL
- 0.9740 mL
- 1.9481 mL

技术信息

CAS号	874119-56-9	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C24H16Cl2F2N6O	运输	蓝冰
分子量	513.33	别名

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GSK-25 Catalog No. CSN25217

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