208665

Calmidazolium Chloride

A cell-permeable calmodulin antagonist.

• Sinonimo/i: Calmidazolium Chloride, Compound R 24571
• Formula empirica (notazione di Hill): C₃₁H₂₃Cl₇N₂O
• Numero CAS: 57265-65-3
• Peso molecolare: 687.70
• Numero MDL: MFCD00077679
• Codice UNSPSC: 12352200

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Stato: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze
• Colore: white
• Solubilità: DMSO: 10 mg/mL; ethanol: 10 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: −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;; LBFGPQFQXRJXDI-UHFFFAOYSA-N

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

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

Avvertenza

readily adheres to glass in aqueous solution.

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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.

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable