Zaldaride  (Synonyms: CGS-9343B free base; KW 5617 free base)

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].

IC50: 3.3 nM (calmodulin)^[1][2].

Zaldaride (P.O., 3 mg/kg) ameliorates the diarrhea in the 16, 16-dimethyl prostaglandin E₂ model^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

428.53

C₂₆H₂₈N₄O₂

109826-26-8

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]

  [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.  [Content Brief]