371970

HA 1077, Dihydrochloride

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

• Sinónimos: HA 1077, Dihydrochloride, Fasudil, (5-Isoquinolinesulfonyl)homopiperazine, 2HCl, PKG Inhibitor VII
• Fórmula empírica (notación de Hill): C₁₄H₁₇N₃O₂S · 2HCl
• Número de CAS: 103745-39-7
• Peso molecular: 364.29
• Número MDL: MFCD00866182
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥98% (HPLC)
• Formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze
• color: white
• solubilidad: water: 1 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 2-8°C
• cadena SMILES: [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
• Clave InChI: NGOGFTYYXHNFQH-UHFFFAOYSA-N

Descripción

Descripción general

A cell-permeable, reversible, and ATP-competitive Ca²⁺ antagonist with anti-vasospastic properties. Inhibits protein kinase A (K_i = 1.6 µM), protein kinase G (K_i = 1.6 µM), and myosin light chain kinase (K_i = 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.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
PKA

Product competes with ATP.

Reversible: yes

Target IC₅₀: 10.7 µM inhibiting Rho-associated kinase (ROCK)

Target K_i: .6 µM, 1.6 µM, 36 µM, inhibiting protein kinase A, protein kinase G, myosin light chain kinase, respectively

Advertencia

Toxicity: Harmful (C)

Reconstitución

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

Otras notas

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.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable