产品
编 号:F035500
分子式:C30H32N4O6
分子量:544.6
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1mg
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生物活性:
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. 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.

体内研究:
Zaldaride maleate (KW 5617, P.O., 3 mg/kg) ameliorates the diarrhea in the 16, 16-dimethyl prostaglandin E2 model.Animal Model:Male Sprague-dawley rats neighing 193-265 g.
Dosage:3-100 mg/kg.
Administration:P.O..
Result:KW-5617 at 3 to100 mg/kg 60 min before DMPGE2 challenge, significantly ameliorated the DMPGE-induced diarrhea, when this drug at 100 mg/kg (p.o. significantly reduced fecaevacuation. Pretreatment with KW-5617 at 3 to 10 mg/kg (p.o.) significantly delayed the onset of diarrhea, and this drug at 30 and 100 mg/kg (p.o. ) reduced or abolished the incidence of diarrhea.
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