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H-1152 dihydrochloride

目录号: PL09259 纯度: ≥99%

H-1152 dihydrochloride 是一种膜通透的，选择性的 ROCK 抑制剂，Ki 值为 1.6 nM，对 ROCK2 的 IC50 值为 12 nM。

CAS No. :871543-07-6

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中文名称	H-1152 dihydrochloride
中文别名	2-氯-5-(三氟甲基)吡啶-4-甲醛;H-1152二氢氯化物;H-1152双盐酸盐
英文名称	H-1152 dihydrochloride
英文别名	H-1152 Dihydrochloride;H 1152 dihydrochloride;H1152;C16H21N3O2S.2HCl;(S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]-hexahydro-1H-1,4-diazepine dihydrochloride;H 1152 dichloride;H1152 dihydrochloride;brd7446 dihydrochloride;dimethyl fasudil dihydrochloride;SYN1221;BCP25257;1781AH;SR-;H-1152 dihydrochloride
Cas No.	871543-07-6
分子式	C₁₆H₂₃Cl₂N₃O₂S
分子量	392.34
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	H-1152 dihydrochloride 是一种膜通透的，选择性的 ROCK 抑制剂，Ki 值为 1.6 nM，对 ROCK2 的 IC50 值为 12 nM。

产品详情	H-1152 dihydrochloride 是一种膜通透的，选择性的 ROCK 抑制剂，K_i 值为 1.6 nM，对 ROCK2 的 IC₅₀ 值为 12 nM。
生物活性	H-1152 dihydrochloride is a membrane-permeable and selective ROCK inhibitor, with a K i value of 1.6 nM, and an IC 50 value of 12 nM for ROCK2.
性状	Solid
IC50 & Target[1][2]	ROCKII 12 nM (IC50) CaMKII 0.18 μM (IC
体外研究(In Vitro)	H-1152 dihydrochloride is an inhibitor of Rho-kinase, with an IC50 of 12 nM for ROCK2. H-1152 (H-1152P) also shows less inhibitory activities against CaMKII, PKG, AuroraA, PKA, Src, PKC, MLCK, Abl, EGFR, MKK4, GSK3α, AMPK, and P38α, with IC50s of 0.180, 0.360, 0.745, 3.03, 3.06, 5.68, 28.3, 7.77, 50.0, 16.9, 60.7, 100, and 100 μM, respectively. H-1152 potently inhibits Rho kinase, with a Ki of 1.6 nM, and slightly suppresses PKA, PKC and MLCK, with Kis of?0.63, 9.27, and 10.1 μM, respectively. H-1152 (0.1-10 μM) highly inhibits MARCKS phosphorylation, with an IC50 value of 2.5 μM in LPA-treated cells, but shows no such obvious effects in PDBu-treated cells. H-1152 (0.5-10 μM) cuases no decreased neuronal survival. H-1152 (1, 5 or 10 μM) also exerts no alterations in the ratios of different neuronal morphologies. Furthermor
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Tamura M, et al. Development of specific Rho-kinase inhibitors and their clinical application. Biochim Biophys Acta. 2005 Dec 30;1754(1-2):245-52. Epub 2005 Sep 12. [2]. Ikenoya M, et al. Inhibition of rho-kinase-induced myristoylated alanine-rich C kinase substrate (MARCKS) phosphorylation in human neuronal cells by H-1152, a novel and specific Rho-kinase inhibitor. J Neurochem. 2002 Apr;81(1):9-16.

溶解度数据	In Vitro: DMSO : 50 mg/mL (127.44 mM; Need ultrasonic)H₂O : 35.71 mg/mL (91.02 mM; Need ultrasonic)配制储备液

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[1]. Tamura M, et al. Development of specific Rho-kinase inhibitors and their clinical application. Biochim Biophys Acta. 2005 Dec 30;1754(1-2):245-52. Epub 2005 Sep 12.
[2]. Ikenoya M, et al. Inhibition of rho-kinase-induced myristoylated alanine-rich C kinase substrate (MARCKS) phosphorylation in human neuronal cells by H-1152, a novel and specific Rho-kinase inhibitor. J Neurochem. 2002 Apr;81(1):9-16.

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。

H-1152 dihydrochloride

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