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About This Item
Empirical Formula (Hill Notation):
C31H23Cl7N2O
CAS Number:
Molecular Weight:
687.70
UNSPSC Code:
12352200
MDL number:
Quality Level
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
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 (Ki = 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
brain calmodulin-dependent phosphodiesterase
Product does not compete with ATP.
Reversible: no
Target IC50: 10 nM against brain calmodulin-dependent phosphodiesterase
Preparation Note
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.
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
Disclaimer
Toxicity: Standard Handling (A)
readily adheres to glass in aqueous solution.
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Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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Corentin Léger et al.
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Global Trade Item Number
| SKU | GTIN |
|---|---|
| 208665-10MG | 07790788048488 |