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

Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate (CGS-9343B) inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC₅₀ of 3.3 nM^[1][2]. Zaldaride maleate (CGS-9343B) 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 maleate (KW 5617, P.O., 3 mg/kg) ameliorates the diarrhea in the 16, 16-dimethyl prostaglandin E₂ model^[4].

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

544.60

C₃₀H₃₂N₄O₆

109826-27-9

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [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]