109826-27-9
Chemical Structure
Zaldaride maleate
Synonym(s): CGS-9343B; KW 5617
- CAS No.: 109826-27-9
- Formula:C30H32N4O6
- Molecular Weight:544.60
IUPAC Name: 1-(1-((4-methyl-4H,6H-benzo[e]pyrrolo[2,1-c][1,4]oxazepin-4-yl)methyl)piperidin-4-yl)-1,3-dihydro-2H-benzo[d]imidazol-2-one maleate
InChIKey: NGODOSILXOFQPH-BTJKTKAUSA-N
SMILES: O=C(O)/C=C\C(O)=O.CC1(C2=CC=CN2C3=CC=CC=C3CO1)CN4CCC(N5C6=C(C=CC=C6)NC5=O)CC4
Biological Activity: Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM[1][2]. Zaldaride maleate prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na+, Ca2+ and K+ currents in PC12 cells and inhibits nAChR[3].
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Zaldaride maleate | 99.7% | Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM. Zaldaride maleate prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na+, Ca2+ and K+ currents in PC12 cells and inhibits nAChR. | ||||||||||||||||||||
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- [1]. Norman JA, et al. CGS 9343B, a novel, potent, and selective inhibitor of calmodulin activity. Mol Pharmacol. 1987 May;31(5):535-40. [Content Brief]
- [2]. Neuhaus R, et al. Inhibition of membrane currents and rises of intracellular Ca2+ in PC12 cells by CGS 9343B, a calmodulin inhibitor. Eur J Pharmacol. 1992 Jun 5;226(2):183-5. [Content Brief]
- [3]. Li L, et al. Calmodulin regulates the transcriptional activity of estrogen receptors. Selective inhibition of calmodulin function in subcellular compartments. J Biol Chem. 2003 Jan 10;278(2):1195-200. [Content Brief]
Keywords
