Zaldaride maleate

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].

Product Specifications

CAS Number

[109826-27-9]

Product Name Alternative

CGS-9343B; KW 5617

UNSPSC

12352005

Target

Calmodulin

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Metabolic Disease; Inflammation/Immunology; Neurological Disease

Assay Protocol

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

Concentration

10mM

Purity

99.7

Solubility

10 mM in H2O

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

Molecular Formula

C30H32N4O6

Molecular Weight

544.60

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.