109826-26-8
Chemical Structure
Zaldaride
Synonym(s): CGS-9343B free base; KW 5617 free base
- CAS No.: 109826-26-8
- Formula:C26H28N4O2
- Molecular Weight:428.53
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
InChIKey: HTGCJAAPDHZCHL-UHFFFAOYSA-N
SMILES: O=C1NC2=C(N1C3CCN(CC4(C)OCC5=C(N6C=CC=C64)C=CC=C5)CC3)C=CC=C2
Biological Activity: Zaldaride (CGS-9343B free base) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM[1][2]. Zaldaride 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 | Zaldaride (CGS-9343B free base) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM. Zaldaride 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
