Zaldaride maleate (Synonyms:CGS-9343B; KW 5617)
目录号 : KM2627 CAS No. : 109826-27-9 纯度 : ≥98%

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。

规格 价格 是否有货 数量
5mg
In-stock
10mg 询价 In-stock
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
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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