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- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Hydroxyfasudil Hydrochloride
- 库存：
999
- 供应商：
北京索莱宝科技有限公司
- CAS号：
155558-32-0
- 规格：
1mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mg | 产品价格： | ¥270.00 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ¥690.00 |
| 规格： | 10mg | 产品价格： | ¥1040.00 |
| 规格： | 25mg | 产品价格： | ¥2028.00 |
| 规格： | 50mg | 产品价格： | ¥3190.00 |
| 规格： | 100mg | 产品价格： | ¥4690.00 |
| CAS | 155558-32-0 |
| 英文名称 | Hydroxyfasudil Hydrochloride |
| 别名 | 羟基法舒地尔盐酸盐; HA-1100 hydrochloride;HA 1100 hydrochloride;HA1100 hydrochloride |
| 分子式 | C14H18ClN3O3S |
| 分子量 | 343.83 |
| 规格 | 1mg ; 5mg ; 10mg ; 25mg ; 50mg ; 100mg |
| 溶解性 | Soluble in DMSO ≥3mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 | 冷藏运输 |
| EC | 683-374-3 |
| MDL | MFCD06411567 |
| SMILES | C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CNC3=O.Cl |
| InChIKey | XWWFOUVDVJGNNG-UHFFFOYSA-N |
| InChI | InChI=1S/C14H17N3O3S.ClH/c18-14-12-3-1-4-13(11(12)5-7-16-14)21(19，20)17-9-2-6-15- 8-10-17;/h1，3-5，7，15H，2，6，8-10H2，(H，16，18);1H |
| PubChem CID | 11371328 |
| 靶点 | ROCK |
| 通路 | Cytoskeleton; Cell Cycle;TGF-beta/Smad;Stem Cells |
| 背景说明 | Hydroxyfasudil hydrochloride 是一种 ROCK 抑制剂，可抑制 ROCK1 和 ROCK2 的活性。 |
| 生物活性 | Hydroxyfasudil hydrochloride is a ROCK inhibitor， with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2， respectively.[1-3] |
| In Vitro | Hydroxyfasudil hydrochloride is a ROCK inhibitor， with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2， respectively. Hydroxyfasudil also less potently inhibits PKA， with an IC50 of 37 μM， 50-fold higher than those of the ROCKs. Hydroxyfasudil increases eNOS mRNA levels， with an EC50 value of 0.8 ± 0.3 μM. Hydroxyfasudil (0-100 μM) concentration-dependently increases eNOS activity and stimulates NO production in human aortic endothelial cells (HAEC). Hydroxyfasudil (10 μM) increases the half-life of eNOS mRNA from 13 to 16 hours， but does not affect eNOS promoter activity at concentrations from 0.1 to 100 μM[1]. |
| In Vivo | Hydroxyfasudil (10 mg/kg， i.p.) significantly increases both the average and maximal voided volumes in SD rats. 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， 10 mg/kg， i.p) significantly ameliorates decreased penile cGMP contents in rats[3]. |
| 动物实验 | Micturition behavior is studied after intraperitoneal injection of either Hydroxyfasudil (10 mg/kg) 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 includ: 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 receive either a single injection of Hydroxyfasudil (10 mg/kg) dissolved in saline or an injection of saline without the inhibitor[2]. |
| 数据来源文献 | [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. |
| 单位 | 瓶 |
| 表格1 | |*|1mg|5mg|10mg|$$|1mM|2.9084mL|14.5421mL|29.0841mL|$$|5mM|0.5817mL|2.9084mL|5.8168mL|$$|10mM|0.2908mL|1.4542mL|2.9084mL| |
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文献和实验Guanidine Hydrochloride Purification of Proteins From SDS
Pepstatin A (2.0 mg/ml)10 ml Leupeptin (1.0 mg/ml)10 ml Aprotinin (5.0 mg/ml)(Protease Inhibitor Cocktail Sigma #P8340)Denaturation Buffer6 M guanidine hydrochloride 57.3 g G-HCl20 mM Hepes 7.9 2 ml 1M Hepes pH 7.910 mM KCl 0.074 g KCl0.5 mM DTT 100 ml 0.5 M
Guanidine Hydrochloride Purification of Proteins From SDS PAGE
(Sigma #P7626) 10 ml Pepstatin A (2.0 mg/ml) 10 ml Leupeptin (1.0 mg/ml) 10 ml Aprotinin (5.0 mg/ml) (Protease Inhibitor Cocktail Sigma #P8340) Denaturation Buffer 6 M guanidine hydrochloride 57.3 g G-HCl 20 mM Hepes 7.9 2 ml 1M Hepes pH 7.9 10 mM
Packed column subcritical and/or supercritical fluid chromatography (p-sub or pSFC) has been used as a powerful chiral separation technique, whereby a mobile phase produces low viscosity, a high diffusion coefficient, and a solvating power. P
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