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Hydroxyfasudil Hydrochloride

Hydroxyfasudil Hydrochloride

产品编号 T4276   CAS 155558-32-0
别名: Hydroxyfasudil (HA-1100) HCl, 羟基法舒地尔盐酸盐, RHO-激酶抑制剂, HA 1100 hydrochloride

Hydroxyfasudil Hydrochloride (HA 1100 hydrochloride) 是一种ROCK 抑制剂,对ROCK1和ROCK2的IC50值分别为 0.73 和 0.72 μM。

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Hydroxyfasudil Hydrochloride Chemical Structure
Hydroxyfasudil Hydrochloride, CAS 155558-32-0
规格 价格/CNY 货期 数量
1 mg ¥ 228 现货
2 mg ¥ 329 现货
5 mg ¥ 578 现货
10 mg ¥ 872 现货
25 mg ¥ 1,770 现货
50 mg ¥ 3,350 现货
100 mg ¥ 4,870 现货
1 mL * 10 mM (in DMSO) ¥ 638 现货
其他形式的 Hydroxyfasudil Hydrochloride:
产品目录号及名称: Hydroxyfasudil Hydrochloride (T4276)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Hydroxyfasudil Hydrochloride (HA 1100 hydrochloride) is a ROCK1/2 inhibitor (IC50s: 0.73/0.72 μM).
靶点活性 ROCK1:0.73 μM, ROCK2:0.72 μM
体外活性 Hydroxyfasudil has a weak inhibition of PKA (IC50: 37 μM), 50-fold higher than those of the ROCKs. Hydroxyfasudil increases eNOS mRNA levels (EC50: 0.8 ± 0.3 μM). Hydroxyfasudil (0-100 μM) concentration-dependently increases eNOS activity and stimulates NO production in HAEC. Hydroxyfasudil (10 μM) increases the half-life of eNOS mRNA from 13 to 16 hours but does not affect eNOS promoter activity (0.1-100 μM).
体内活性 Hydroxyfasudil (10 mg/kg, i.p.) markedly increases both the maximal and average voided volumes in SD rats. Hydroxyfasudil also markedly reduces the maximal detrusor pressure. In spontaneously hypertensive rats (SHRs), Hydroxyfasudil (3 mg/kg, i.p.) inhibits hypercontractility induced by norepinephrine. Additionally, Hydroxyfasudil (3/10 mg/kg, i.p.) significantly ameliorates decreased penile cGMP contents in rats.
动物实验 Hydroxyfasudil is formulated in saline.Micturition behavior is studied after administration of either Hydroxyfasudil (10 mg/kg, i.p.) or a corresponding volume of saline. Each rat is placed in a metabolic cage containing a urine collection funnel that is placed over an electronic balance. The balance is connected to a personal computer via a multiport controller and used to measure the cumulative weight of the collected urine. Every 150 s during a continuous 24-h period, the computer samples and records the data for the micturition frequency and volumes. The micturition reflex parameters that are collected include: urine volume per micturition, maximal micturition volume, micturition frequency, and total urine output in the Hydroxyfasudil- or vehicle-treated animals. Each monitoring session started at 18.00 hours. Prior to being placed in the metabolic cage at the start of each experimental period, the animals received either a single injection of Hydroxyfasudil (10 mg/kg) dissolved in saline or an injection of saline without the inhibitor.
别名 Hydroxyfasudil (HA-1100) HCl, 羟基法舒地尔盐酸盐, RHO-激酶抑制剂, HA 1100 hydrochloride
分子量 343.83
分子式 C14H18ClN3O3S
CAS No. 155558-32-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 62 mg/mL(180.3 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9084 mL 14.5421 mL 29.0841 mL 72.7104 mL
5 mM 0.5817 mL 2.9084 mL 5.8168 mL 14.5421 mL
10 mM 0.2908 mL 1.4542 mL 2.9084 mL 7.271 mL
20 mM 0.1454 mL 0.7271 mL 1.4542 mL 3.6355 mL
50 mM 0.0582 mL 0.2908 mL 0.5817 mL 1.4542 mL
100 mM 0.0291 mL 0.1454 mL 0.2908 mL 0.7271 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Rikitake Y, et al. Inhibition of Rho kinase (ROCK) leads to increased cerebral blood flow and stroke protection. Stroke. 2005 Oct;36(10):2251-7. Epub 2005 Sep 1. 2. Masago T, et al. Effect of the rho-kinase inhibitor hydroxyfasudil on bladder overactivity: an experimental rat model. Int J Urol. 2009 Oct;16(10):842-7. 3. Saito M, et al. Hydroxyfasudil ameliorates penile dysfunction in the male spontaneously hypertensive rat. Pharmacol Res. 2012 Oct;66(4):325-31.

文献引用

1. Sun L, Sun L, Li X, et al. A Novel Tigecycline Adjuvant ML-7 Reverses the Susceptibility of Tigecycline-Resistant Klebsiella pneumoniae. Frontiers in cellular and infection microbiology. 2022: 1341.
Y-9738 RKI-1447 AT13148 ROCK-IN-9 Rho-Kinase-IN-1 CMPD101 ROCK-IN-8 Hydroxyfasudil

相关化合物库

该产品包含在如下化合物库中:
TGF-β/Smad靶点化合物库 抗衰老化合物库 神经再生化合物库 表型筛选靶点鉴定库 细胞骨架化合物库 细胞重编程化合物库 免疫/炎症分子化合物库 抑制剂库 抗代谢疾病化合物库 激酶抑制剂库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Hydroxyfasudil Hydrochloride 155558-32-0 Cell Cycle/Checkpoint Cytoskeletal Signaling Stem Cells ROCK Hydroxyfasudil (HA-1100) HCl HA-1100 Hydroxyfasudil Rho-associated kinase HA 1100 羟基法舒地尔盐酸盐 inhibit HA1100 HA1100 Hydrochloride Rho-kinase RHO-激酶抑制剂 Rho-associated protein kinase HA-1100 Hydrochloride ROK HA 1100 hydrochloride Inhibitor HA 1100 Hydrochloride inhibitor

 

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