BAY-549|867017-68-3|(ROCK-IN-2; Azaindole 1; TC-S 7001)-陌孚医药/Medlife

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BAY-549 (Synonyms: ROCK-IN-2; Azaindole 1; TC-S 7001)

目录号: PL11058 纯度: ≥98%

CAS No. :867017-68-3

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中文名称	BAY-549
中文别名	6-氯-N4-[3,5-二氟-4-[(3-甲基-1H-吡咯并[2,3-B]吡啶-4-基)氧]苯基]-2,4-嘧啶二胺
英文名称	BAY-549
英文别名	6-Chloro-N4-{3,5-difluoro-4-[(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl}pyrimidin-2,4-diamine;6-chloro-4-N-[3,5-difluoro-4-[(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl]pyrimidine-2,4-diamine;6-Chloro-N4-{3,5-difluoro-4-[(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl}pyrimidin-2,4-...;ROCK inhibitor;TC-S 7001;Rho Kinase Inhibitor;Rho-kinase inhibitor;ROCK;6-Chloro-N4-[3,5-difluoro-4-[(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl]-2,4-pyrimidinediamine;ROCK-IN-2;Azaindole 1;Azaindole-1;6-CHLORO-N4-[3,5-DIFLUORO-4-({3-METHYL-1H-PYRROLO[2,3-B]PYRIDIN-4-YL}OXY)PHENYL]PYRIMIDINE-2,4-DIAMINE;6-Chloro-N4-{3,5-difluoro-4-[(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl}pyrimidine-2,4-diamine;Kinome_3805;NRSGWEVTVGZDFC-U;BAY-549
Cas No.	867017-68-3
分子式	C₁₈H₁₃ClF₂N₆O
分子量	402.79
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	BAY-549 (Azaindole 1) 是有口服活性，ATP-竞争型的 ROCK 抑制剂，对 ROCK-1 和 ROCK-2 的 IC₅₀ 值分别为 0.6 和 1.1 nM。
生物活性	BAY-549 (Azaindole 1) is an orally active and ATP-competitive ROCK inhibitor with IC 50 s of 0.6 and 1.1?nM for human ROCK-1 and ROCK-2, respectively.
性状	Solid
IC50 & Target[1][2]	ROCK-1 0.6 nM (IC50) ROCK-2 1.1 nM (IC
体外研究(In Vitro)	BAY-549 (Azaindole 1) is a highly potent inhibitor of human ROCK-1 and ROCK-2, with IC50s of 0.6 and 1.1?nM, respectively, and also inhibits murine ROCK-2 or rat ROCK-2 with IC50s of 2.4 and 0.8?nM, respectively. BAY-549 also inhibits receptor tyrosine kinases TRK and FLT3, with IC50s of 252 and 303?nM, respectively, but shows slight inhibition of MLCK and ZIP-kinase with IC50s of 7.4?μM and 4.1?μM, respectively. BAY-549 induces vasorelaxation in vitro, and suppresses the phenylephrine-induced contraction of rabbit saphenous artery in a concentration dependent manner with an IC50 value of 65?nM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	BAY-549 (Azaindole 1) (0.03, 0.1, 0.3?mg/kg, i.v.) results in a dose-dependent and long-lasting decrease in blood pressure in anaesthetized normotensive rats. BAY-549 (3 and 10?mg/kg, p.o.) decreases blood pressure dose-dependently and persistently both in normotensive and hypertensive rats, and shows such effects even at 1?mg/kg in hypertensive rats. BAY-549 (0.1 and 0.3?mg/kg, i.v. bolus injections) causes decreased mean arterial blood pressure in a dose-related manner and only leads to a moderate and dose-independent increase in heart rate of anaesthetized dogs. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Kast R, et al. Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase. Br J Pharmacol. 2007 Dec;152(7):1070-80. Epub 2007 Oct 15.

溶解度数据	In Vitro: DMSO : 33.33 mg/mL (82.75 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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