Zaldaride maleate CGS-9343B; KW 5617|cas:109826-27-9|西域试剂

Zaldaride maleate CGS-9343B; KW 5617,98.0%

产品编号：Bellancom-105118A| CAS NO：109826-27-9| 分子式：C₃₀H₃₂N₄O₆| 分子量：544.60

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货号	价格	库存与货期
Bellancom-105118A	￥5200.00	杭州北京（现货）
Bellancom-105118A	￥8100.00	杭州北京（现货）
Bellancom-105118A	￥15000.00	杭州北京（现货）

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Zaldaride maleate CGS-9343B; KW 5617

产品介绍

Zaldaride maleate (CGS-9343B) 是一个有效的、有口服活性的、选择性的钙调蛋白 (calmodulin) 的抑制剂，可抑制钙调蛋白刺激cAMP磷酸二酯酶的活性，IC₅₀ 值为 3.3 nM。Zaldaride maleate (CGS-9343B) 可抑制雌激素诱导的 ER 转录激活，可逆地阻断 PC12 细胞中电压激活的的 Na⁺、Ca²⁺和 K⁺电流，抑制 nAChR。

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.

体外研究

体内研究

Zaldaride maleate (KW 5617, P.O., 3 mg/kg) ameliorates the diarrhea in the 16, 16-dimethyl prostaglandin E₂ model^[4].

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

Animal Model:	Male Sprague-dawley rats neighing 193-265 g^[4].
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.

体内研究

Zaldaride maleate (KW 5617, P.O., 3 mg/kg) ameliorates the diarrhea in the 16, 16-dimethyl prostaglandin E₂ model^[4].

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

Animal Model:	Male Sprague-dawley rats neighing 193-265 g^[4].
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.