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  • 化合物 Rho-Kinase-IN-2|T61497|TargetMol

化合物 Rho-Kinase-IN-2|T61497|TargetMol

Rho-Kinase-IN-2
2573071-18-6
￥2980 2mg 起订
￥4480 5mg 起订
￥11500 25mg 起订
上海 更新日期：2025-11-17

TargetMol中国（陶术生物）

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联系人：邵小姐
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邮箱：marketing@targetmol.cn

产品详情:

中文名称：
化合物 Rho-Kinase-IN-2
英文名称：
Rho-Kinase-IN-2
CAS号：
2573071-18-6
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
产品类别：
抑制剂
货号：
T61497

Product Introduction

Bioactivity

名称Rho-Kinase-IN-2
描述Rho-Kinase-IN-2 (Compound 23) is an orally active and selective inhibitor of Rho Kinase (ROCK), which can penetrate the central nervous system (CNS). It exhibits a high affinity for ROCK2 with an inhibition constant (IC50) of 3 nM. This compound is of potential interest for further investigations in the field of Huntington's disease research [1].
体外活性Rho-Kinase-IN-2 (0-10 mM, 1 hour) treatment shows an increase in AKT phosphorylation and a decrease in MYPT1 phosphorylation [1]. Western Blot Analysis [1] Cell Line: A7r5 and PANC1 cells Concentration: 0-10 mM Incubation Time: 1 hour Result: Showed concentration-dependent effects, leading to an increase in AKT phosphorylation (EC 50 =28 nM) and a decrease in MYPT1 phosphorylation (IC 50 =14 nM).
体内活性Rho-Kinase-IN-2 (Oral adiministration; 10 mg/kg; 6 times; 0.5, 1, 2, 4, 8, and 12 h) treatment shows dose- and time-dependent ROCK1 and ROCK2 target engagement [1]. Rho-Kinase-IN-2 (Oral adiministration; 10 or 20 mg/kg; QD or BID; 2 weeks) treatment shows excellent tolerability assessment [1]. Rho-Kinase-IN-2 (Oral adiministration; 1-20 mg/kg; once) treatment shows a direct dose- and time-dependent relationship between brain exposure and MYPT1 phosphorylation status [1]. Rho-Kinase-IN-2 (Oral adiministration; 10 or 20 mg/kg; once) treatment decreases in the mean arterial, systolic, diastolic blood pressure, and heart rate [1]. Rho-Kinase-IN-2 (Oral adiministration; 10 mg/kg; twice a day; 90 days) treatment leads to lower-than-expected brain concentrations [1]. Animal Model: Male C57BL/6 mice [1] Dosage: 10 mg/kg Administration: Oral adiministration; 10 mg/kg; 6 times; 0.5, 1, 2, 4, 8, and 12 h Result: Observed dose- and time-dependent ROCK1 and ROCK2 TE, with a free brain KiNativ ROCK1 and ROCK2 IC 50 =～6 nM. Animal Model: 3 4 months old heterozygote Q175DN KI and wild-type littermate mice [1] Dosage: 10 or 20 mg/kg Administration: Oral adiministration; 10 or 20 mg/kg; once a day or twice a day; 2 weeks Result: Scored neurological index normally at all doses although a slight loss in bodyweight (～2%) in the 20 mg/kg treatment group. Animal Model: Heterozygote HTT zQ175DN knock-in mice [1] Dosage: 1-20 mg/kg Administration: Oral adiministration; 1-20 mg/kg; once Result: Remained over MYPT1 IC 50 for over 2 h of the free brain at 10 mg/kg, and observed the dose- and time-dependent inhibition of MYPT1 phosphorylation in the striatum following acute in vivo dosing. Animal Model: CD1 mice [1] Dosage: 10 and 20 mg/kg Administration: Oral adiministration; 10 or 20 mg/kg; once Result: Observed the decreases in the mean arterial (maximum change of 61.0 ± 8.5 mmHg from baseline), systolic (maximum change of 59.5 ± 8.4 mmHg from baseline), diastolic blood pressure (maximum change of 56.4 ± 9.0 mmHg from baseline), and heart rate (maximum change from predose of 107 bpm) when compared to the control group from ～0.5 to 2 h post dose. Animal Model: Heterozygote Q175DN KI mouse model of HD [1] Dosage: 10 mg/kg Administration: Oral adiministration; 10 mg/kg; twice a day; 90 days Result: Led to lower-than-expected brain concentrations compared to single dosing.
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
相关产品Y-27632 dihydrochloride | CID-5056270 | ROCK-IN-5 | Fasudil hydrochloride | SB-747651A Dihydrochloride | CAY10746 | Y-27632 | RKI-1447 | GSK270822A | SAR407899 hydrochloride | Thiazovivin | GSK180736A
Rho-Kinase-IN-2|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (13年)
注册资本 589.8595万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 中间体,天然产物,生物化工,化学试剂,生物技术服务

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