208665

Calmidazolium Chloride

A cell-permeable calmodulin antagonist.

• Sinónimos: Calmidazolium Chloride, Compound R 24571
• Fórmula empírica (notación de Hill): C₃₁H₂₃Cl₇N₂O
• Número de CAS: 57265-65-3
• Peso molecular: 687.70
• MDL number: MFCD00077679
• UNSPSC Code: 12352200

Propiedades

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze
• color: white
• solubility: DMSO: 10 mg/mL; ethanol: 10 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• InChI: 1S/C31H24Cl6N2O.Cl/c32-23-6-1-20(2-7-23)31(21-3-8-24(33)9-4-21)39-14-13-38(19-39)17-30(27-12-11-26(35)16-29(27)37)40-18-22-5-10-25(34)15-28(22)36;/h1-16,30-31H,17-19H2;
• InChI key: LBFGPQFQXRJXDI-UHFFFAOYSA-N

Descripción

General description

A cell-permeable calmodulin antagonist. An analog of sepazonium that is at least 150 times more potent than Trifluoperazine (Cat. No. 642150) as an inhibitor of brain Ca²⁺-calmodulin-dependent phosphodiesterase (IC₅₀ = 10 nM). Inhibits voltage-gated Ca²⁺ channels and stimulates the release of nitric oxide in neuroblastoma cells. Also, acts as a strong inhibitor of calcium-dependent Ca²⁺-ATPase in erythrocytes. Known to prolong cardiac refractory period in vivo.

A cell-permeable calmodulin antagonist. At least 150 times more potent than Trifluoperazine (Cat. No. 642150) as an inhibitor of brain calmodulin-dependent phosphodiesterase (IC₅₀ = 10 nM). An inhibitor of voltage-gated Ca²⁺ channels. Stimulates the release of nitric oxide in neuroblastoma cells. Also acts as a strong non-competitive inhibitor of skeletal muscle sarcoplasmic reticulum Ca²⁺-ATPase (K_i = 60 nM). Known to prolong cardiac refractoriness in vivo.

Note: easily adheres to glass in aqueous solution.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
brain calmodulin-dependent phosphodiesterase

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 10 nM against brain calmodulin-dependent phosphodiesterase

Caution

readily adheres to glass in aqueous solution.

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C) for long term storage or refrigerate (4°C) for short-term storage. DMSO stock solutions are stable for up to 2 months -20°C.

Other Notes

Hu, J., and El-Fakahany, E.E. 1993. NeuroReport. 4, 198.
Nakazawa, K., et al. 1993. Br. J. Pharmacol. 109, 137.
Yuasa, T., and Muto, S. 1992. Arch. Biochem. Biophys.296, 175.
Ichikawa, M., et al. 1991. J. Membrane Biol.120, 211.
Silver, P.J., et al. 1989. Cardiovasc. Drug Ther. 3, 675.
Anderson, K.W., et al. 1984. J. Biol. Chem.259, 11487.
Gietzen, L., et al. 1982. Biochem. J. 207, 541.
Van Belle, H. 1981. Cell Calcium2, 483.
Levin, R.N., and Weiss, B. 1979. J. Pharmacol. Exp. Therap.208, 454.

Legal Information

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

Información de seguridad

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable