计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase ( ROCK ) inhibitor (ROCK2 IC 50 =3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research
In Vitro
Rho-Kinase-IN-2 (0-10 mM, 1 hour) treatment shows an increase in AKT phosphorylation and a decrease in MYPT1 phosphorylation. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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).
In Vivo
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 . Rho-Kinase-IN-2 (oral adiministration; 10 or 20 mg/kg; QD or BID; 2 weeks) treatment shows excellent tolerability assessment . 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 . 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 . Rho-Kinase-IN-2 (oral adiministration; 10 mg/kg; twice a day; 90 days) treatment leads to lower-than-expected brain concentrations . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL/6 mice 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 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 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 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 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.
Form:Solid
IC50& Target:ROCK2 3 nM (IC 50 )
规格
别名
Rho-激酶-IN-2
规格或纯度
≥99%
英文名称
Rho-Kinase-IN-2
生化机理
Rho-激酶-IN-2（化合物 23）是一种口服活性、选择性和中枢神经系统（CNS）渗透性 Rho 激酶（ROCK）抑制剂（ROCK2 IC 50 =3 nM）。Rho-Kinase-IN-2 可用于亨廷顿氏症的研究。
储存条件
-20°C储存
运输条件
超低温运输
纯度
≥99%
名称和识别符
分子类型
小分子
Smiles
O=C(N1[C@H](C)CN(C2=C(F)C=NC=C2)CC1)N[C@@H](C3=CC=CC(OC)=C3)C
分子量
372.44
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 50 mg/mL (134.25 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品的纯度是多少？
本产品的化学纯度（含量）为 ≥99%。批次的具体数值以分析证书（COA）为准。
本产品应如何储存？
请于?20 °C条件下保存。需冷冻保存以维持规定的有效期。
本产品如何运输？
本产品采用保温箱配冰袋运输。收货后请立即拆包，并按上述储存条件保存。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 2573071-18-6，分子式为 C20H25FN4O2，分子量为 372.44 g/mol。
如何获取批次专用COA？
每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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危险品化学品经营许可证（带存储）