产品描述

Fasudil Hydrochloride is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

靶点活性

MLCK    PKA    PKC    PKG    ROCK2

激酶实验

Cyclic AMP-dependent protein kinase activity is assayed in a reaction mixture containing, in a final volume of 0.2 mL, 50 mM Tris-HCl (pH 7.0), 10 mM magnesium acetate, 2 mM EGTA, 1 μM cyclic AMP or absence of cyclic AMP, 3.3 to 20 μM [r-32P] ATP (4×105 c.p.m.), 0.5 μg of the enzyme, 100 μg of histone H2B and compound. The mixture is incubated at 30°C for 5 min. The reaction is terminated by adding 1mL of ice-cold 20% trichloroacetic acid after adding 500 μg of bovine serum albumin as a carrier protein. The sample is centrifuged at 3000 r.p.m. for 15min, the pellet is resuspended in ice-cold 10% trichloro-acetic acid solution and the centrifugation-resuspension cycle is repeated three times. The final pellet is dissolved in 1 mL of 1 N NaOH and radioactivity is measured with a liquid scintillation counter.

别名

盐酸法舒地尔 , AT-877 , Fasudil HCl , HA-1077 , Fasudil (HA-1077) HCl , HA-1077 hydrochloride

纯度

98%

分子量

327.83

分子式

C14H18ClN3O2S

CAS No.

105628-07-7

存储

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

溶解度

DMSO: 24.6 mg/mL (75 mM)

water: 32.8 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

溶液 1

Saline: 30 mg/mL

参考文献

1. Ono-Saito N, et al. Pharmacol Ther, 1999, 82(2-3), 123-131.

2. Asano T, et al. J Pharmacol Exp Ther, 1987, 241(3), 1033-1040.

3. Asano T, et al. Br J Pharmacol, 1989, 98(4), 1091-1100.

4. Negoro N, et al. Biochem Biophys Res Commun, 1999, 262(1), 211-215.

5. Fukushima M, et al. Liver Int, 2005, 25(4), 829-838.

6. Zhang J, et al. Clin Chim Acta, 2009, 401(1-2), 76-80.

Note

For research use only.