371970

HA 1077, Dihydrochloride

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

• Synonyma: HA 1077, Dihydrochloride, Fasudil, (5-Isoquinolinesulfonyl)homopiperazine, 2HCl, PKG Inhibitor VII
• Empirický vzorec (Hillův zápis): C₁₄H₁₇N₃O₂S · 2HCl
• Číslo CAS: 103745-39-7
• Molekulová hmotnost: 364.29
• MDL number: MFCD00866182
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze

Vlastnosti

• Quality Segment: 100
• 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
• 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

Popis

General description

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.

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

Preparation Note

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

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.

Legal Information

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

Disclaimer

Toxicity: Harmful (C)

Bezpečnostní informace

• Skladovací třída: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable