| Bioactivity | 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]. |
| Target | IC50: 3.3 nM (calmodulin). |
| In Vivo | Zaldaride maleate (KW 5617, P.O., 3 mg/kg) ameliorates the diarrhea in the 16, 16-dimethyl prostaglandin E2 model[4]. Animal Model: |
| Name | Zaldaride maleate |
| CAS | 109826-27-9 |
| Formula | C30H32N4O6 |
| Molar Mass | 544.60 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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. |
Zaldaride maleate
CAS: 109826-27-9 F: C30H32N4O6 W: 544.60
Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate (CGS-9
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