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Merck
CN

371970

HA 1077, Dihydrochloride

A cell-permeable, reversible, and ATP-competitive Ca2+ antagonist with anti-vasospastic properties.

别名:

HA 1077, Dihydrochloride, Fasudil, (5-Isoquinolinesulfonyl)homopiperazine, 2HCl, PKG Inhibitor VII

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关于此项目

经验公式(希尔记法):
C14H17N3O2S · 2HCl
化学文摘社编号:
分子量:
364.29
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
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产品名称

HA 1077, Dihydrochloride, A cell-permeable, reversible, and ATP-competitive Ca2+ antagonist with anti-vasospastic properties.

SMILES string

[S](=O)(=O)(N3CCNCCC3)c1c2c(cncc2)ccc1

InChI

1S/C14H17N3O2S/c18-20(19,17-9-2-6-15-8-10-17)14-4-1-3-12-11-16-7-5-13(12)14/h1,3-5,7,11,15H,2,6,8-10H2

InChI key

NGOGFTYYXHNFQH-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze

color

white

solubility

water: 1 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

General description

A cell-permeable, reversible, and ATP-competitive Ca2+ antagonist with anti-vasospastic properties. Inhibits protein kinase A (Ki = 1.6 µM), protein kinase G (Ki = 1.6 µM), and myosin light chain kinase (Ki = 3.6 µM). Also reported to potently inhibit Rho-associated kinase (ROCK; IC50 = 10.7 µM). Prevents apoptosis and enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency.

Other Notes

Watanabe, K., et al. 2007. Nature Biotech.25, 681.
Swärd, K., et al. 2000. J. Physiol.522, 33.
Takizawa, S., et al. 1993. Eur. J. Pharmacol. 250, 431.
Seto, M., et al. 1991. Eur. J. Pharmacol.195, 267.
Shirotani, M., et al. 1991. J. Pharmacol. Exp. Ther.259, 738.
Asano, T., et al. 1990. Eur. J. Pharmacol.190, 365.
Sasaki, Y., and Sasaki, Y. 1990. Biochem. Biophys. Res. Commun.171, 1182.
Asano, T., et al. 1989. Br. J. Pharmacol. 98,1091.

Preparation Note

Following reconstitution, refrigerate (4°C). Aqueous stock solutions are stable for up to 6 months at 4°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Biochem/physiol Actions

Cell permeable: yes
Primary Target
PKA
Product competes with ATP.
Reversible: yes
Target IC50: 10.7 µM inhibiting Rho-associated kinase (ROCK)
Target Ki: .6 µM, 1.6 µM, 36 µM, inhibiting protein kinase A, protein kinase G, myosin light chain kinase, respectively

Disclaimer

Toxicity: Harmful (C)

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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