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作靶點(diǎn): ROCK作通路: Cell Cycle/DNA Damage; Stem Cell/Wnt; TGF-beta/Smad儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)

2、體外實(shí)驗(yàn) DMSO : 31 mg/mL (100.86 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制

3、澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.5 mg/mL (1.63 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 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 您邊的抑制劑師www.MedChemE3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 0.5 mg/mL (1.63 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Hydroxyfasudil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)體外研究 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.體內(nèi)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.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.MedChemE2/3 Master of Small Molecules 您邊的抑制劑師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