Zaldaride maleate

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Zaldaride maleate

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

109826-27-9

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议

产品名称

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 ofcalmodulin. Zaldaride maleate (CGS-9343B) inhibits CaM (calmodulin)-stimulated cAMPphosphodiesteraseactivity, with anIC₅₀of 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 inhibitsnAChR^[3].

IC₅₀& Target

IC50: 3.3 nM (calmodulin)^[1]^[2].

体内研究
(In Vivo)

Zaldaride maleate (KW 5617, P.O., 3 mg/kg) ameliorates the diarrhea in the 16, 16-dimethyl prostaglandin E₂model^[4].

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.

分子量

544.60

性状

Solid

Formula

C₃₀H₃₂N₄O₆

CAS 号

109826-27-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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