Hydroxyfasudil-HA-1100-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEHydroxyfasudilCat. No.: HY-13911CAS No.: 105628-72-6Synonyms: HA-1100分式: CHNOS分量: 307.37作靶点: ROCK作通路: Cell Cycle/DNA Damage; Stem Cell/Wnt; TGF-beta/Smad储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据

2、体外实验 DMSO : 31 mg/mL (100.86 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.2534 mL 16.2670 mL 32.5341 mL5 mM 0.6507 mL 3.2534 mL 6.5068 mL10 mM 0.3253 mL 1.6267 mL 3.2534 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制

3、澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.5 mg/mL (1.63 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.5 mg/mL (1.63 mM); Clear solution1/3 Mas

4、ter of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 0.5 mg/mL (1.63 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Hydroxyfasudil种 ROCK 抑制剂，可抑制 ROCK1 和 ROCK2 的活性，IC50 值分别为 0.73 和 0.72 M。IC50 & Target ROCK2 ROCK1 PKA0.72 M (IC50) 0.73 M (IC50) 37 M (IC50)体外研究 Hydroxyfa

5、sudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 M for ROCK1 and ROCK2, respectively.Hydroxyfasudil also less potently inhibits PKA, with an IC50 of 37 M, 50-fold higher than those of theROCKs. Hydroxyfasudil increases eNOS mRNA levels, with an EC50 value of 0.8 0.3 M. Hydroxyfasudil(0-100 M)

6、concentration-dependently increases eNOS activity and stimulates NO production in humanaortic endothelial cells (HAEC). Hydroxyfasudil (10 M) increases the half-life of eNOS mRNA from 13 to 16hours, but does not affect eNOS promoter activity at concentrations from 0.1 to 100 M 1.体内研究 Hydroxyfasudil

7、(10 mg/kg, i.p.) significantly increases both the average and maximal voided volumes in SDrats. Hydroxyfasudil also significantly decreases the maximal detrusor pressure 2. Hydroxyfasudil (3 mg/kg,i.p) inhibits hypercontractility induced by norepinephrine in spontaneously hypertensive rats (SHRs).Fu

8、rthermore, Hydroxyfasudil (3, 10 mg/kg, i.p) significantly ameliorates decreased penile cGMP contents inrats 3.PROTOCOLAnimal Micturition behavior is studied after intraperitoneal injection of either Hydroxyfasudil (10 mg/kg) or aAdministration 2 corresponding volume of saline. Each rat is placed in

9、 a metabolic cage containing a urine collection funnelthat is placed over an electronic balance. The balance is connected to a personal computer via a multiportcontroller and used to measure the cumulative weight of the collected urine. Every 150 s during a continuous24-h period, the computer sample

10、s and records the data for the micturition frequency and volumes. Themicturition reflex parameters that are collected includ: urine volume per micturition, maximal micturitionvolume, micturition frequency, and total urine output in the Hydroxyfasudil- or vehicle-treated animals. Eachmonitoring sessi

11、on started at 18.00 hours. Prior to being placed in the metabolic cage at the start of eachexperimental period, the animals receive either a single injection of Hydroxyfasudil (10 mg/kg) dissolved insaline or an injection of saline without the inhibitor 2.MCE has not independently confirmed the accu

12、racy of these methods. They are for reference only.户使本产品发表的科研献 Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093.See more customer validations on HYPERLINK / www.MedChemE2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEREFERENCES1. Rikitake Y, et al. Inhibition of Rho kinase (ROCK) leads to increas

13、ed cerebral blood flow and stroke protection. Stroke. 2005Oct;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. 2009Oct;16(10):842-7.3. Saito M, et al. Hydroxyfasudil ameliorates penile dysfunction in the male spontaneously hypertensive rat. Pharmacol Res. 2012Oct;66(4):325-31.Mc