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Hydroxyfasudil hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Hydroxyfasudil hydrochloride图片
CAS NO:155558-32-0
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
羟基法舒地尔盐酸盐
HA 1100 hydrochloride
Hydroxyfasudil (HA-1100) HCl
RHO-激酶抑制剂
产品介绍
Hydroxyfasudil hydrochloride 是一种ROCK抑制剂,对ROCK1和ROCK2的IC50值分别为 0.73 和 0.72 μM。

产品描述

Hydroxyfasudil hydrochloride is a ROCK1/2 inhibitor (IC50s: 0.73/0.72 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.

Cas No.

155558-32-0

分子式

C14H18ClN3O3S

分子量

343.83

别名

羟基法舒地尔盐酸盐;HA 1100 hydrochloride;Hydroxyfasudil (HA-1100) HCl;RHO-激酶抑制剂

储存和溶解度

DMSO:62 mg/mL(180.3 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years