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[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].

Product Specifications

CAS Number

[109826-26-8]

Product Name Alternative

CGS-9343B (free base) ; KW 5617 (free base)

UNSPSC

12352005

Target

Calmodulin

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease; Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/zaldaride.html

Smiles

O=C1NC2=C(N1C3CCN(CC4(C)OCC5=C(N6C=CC=C64)C=CC=C5)CC3)C=CC=C2

Molecular Formula

C26H28N4O2

Molecular Weight

428.53

References & Citations

[1]Norman JA, et al. CGS 9343B, a novel, potent, and selective inhibitor of calmodulin activity. Mol Pharmacol. 1987 May;31 (5) :535-40.|[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.|[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.|[4]Aikawa N, et al. Effects of KW-5617 (zaldaride maleate), a potent and selective calmodulin inhibitor, on secretory diarrhea and on gastrointestinal propulsion in rats. Jpn J Pharmacol. 1998 Feb;76 (2) :199-206.