Zaldaride maleate - CAS:109826-27-9

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

目录号 : KM2627 CAS No. : 109826-27-9 纯度 : ≥98%

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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。

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50mg	询价	In-stock

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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, Ca 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.

分子式

C₂₆H₂₈N₄O₂^.C₄H₄O₄

分子量

544.60

CAS号

109826-27-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

纯度： ≥98%

Data Sheet

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