Hydroxyfasudil-hydrochloride-HA-1100-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEHydroxyfasudil hydrochlorideCat. No.: HY-13911ACAS No.: 155558-32-0Synonyms: HA-1100 hydrochloride; HA 1100 hydrochloride; HA1100hydrochloride分式: CHClNOS分量: 343.83作靶點(diǎn): ROCK作通路: Cell Cycle/DNA Damage; Stem Cell/Wnt; TGF-beta/Smad

2、儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 30 mg/mL (87.25 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.9084 mL 14.5421 mL 29.0841 mL5 mM 0.5817 mL 2.9084 mL 5.8168 mL10 mM 0.2908 mL 1.4542 mL 2.9084 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)

3、備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Hydroxyfasudil hydrochloride種 ROCK 抑制劑，可抑制 ROCK1 和 ROCK2 的活性，IC50 值分別為 0.73和 0.72 M。IC50 & Target ROCK2 ROCK1 PKA0.72 M (IC50) 0.73 M (IC50) 37 M (IC50)1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 Hydroxyfasudil hydrochloride is a ROCK inhibitor, wit

4、h 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 thoseof the ROCKs. Hydroxyfasudil increases eNOS mRNA levels, with an EC50 value of 0.8 0.3 M.Hydroxyfasudil (0-100 M) concentration-dependently incr

5、eases eNOS activity and stimulates NO productionin human aortic endothelial cells (HAEC). Hydroxyfasudil (10 M) increases the half-life of eNOS mRNA from13 to 16 hours, but does not affect eNOS promoter activity at concentrations from 0.1 to 100 M 1.體內(nèi)研究 Hydroxyfasudil (10 mg/kg, i.p.) significantly

6、 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).Furthermore, Hydroxyfasudil (3,

7、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 a metabolic cage containing a

8、 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 samples and records the data for the

9、 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 session started at 18.00 hours. Pri

10、or 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 accuracy of these methods. They ar

11、e for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Rikitake Y, et al. Inhibition of Rho kinase (ROCK) leads to increased cerebral blood flow and stroke protection. Stroke. 2005Oct;36(10):2251-7. Ep

12、ub 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.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.MedChemECaution