产品说明书

Retosiban

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Chemical Structure| 820957-38-8 同义名 : GSK 221149;GSK 221149A
CAS号 : 820957-38-8
货号 : A656414
分子式 : C27H34N4O5
纯度 : 99+%
分子量 : 494.583
MDL号 : MFCD19443707
存储条件：

粉末

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(212.3 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Retosiban is an oral active, potent and selective, sub-nanomolar (Ki = 0.65 nM) oxytocin receptor antagonist with > 1400-fold selectivity over the related vasopressin receptors. Retosiban inhibits the procontractile effect of stretch on human myometrium and prevent stretch-induced stimulation of human myometrial contractility.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.02mL

0.40mL

0.20mL

10.11mL

2.02mL

1.01mL

20.22mL

4.04mL

2.02mL
参考文献

[1]Stier B, Fossler M, et al. Effect of Retosiban on Cardiac Repolarization in a Randomized, Placebo- and Positive-controlled, Crossover Thorough QT/QTc Study in Healthy Men and Women. Clin Ther. 2015 Jul 1;37(7):1541-54.

[2]Liddle J, Allen MJ, et al. The discovery of GSK221149A: a potent and selective oxytocin antagonist. Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4.