208665

Calmidazolium Chloride

A cell-permeable calmodulin antagonist.

• 別名: Calmidazolium Chloride, Compound R 24571
• 実験式（ヒル表記法）: C₃₁H₂₃Cl₇N₂O
• CAS番号: 57265-65-3
• 分子量: 687.70
• MDL番号: MFCD00077679
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze
• 色: white
• 溶解性: DMSO: 10 mg/mL; ethanol: 10 mg/mL
• 輸送温度: ambient
• 保管温度: −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

詳細

詳細

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.

生物化学的／生理学的作用

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

注意

readily adheres to glass in aqueous solution.

警告

Toxicity: Standard Handling (A)

再構成

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.

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable