2. GPCR/G Protein
  3. Oxytocin Receptor
  4. Epelsiban

Epelsiban (GSK 557296) 是一种有效的，选择性的，可口服的催产素受体 (oxytocin receptor) 抑制剂，对人催产素受体的 pKi 值为 9.9。

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Epelsiban Chemical Structure

Epelsiban Chemical Structure

CAS No. : 872599-83-2

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Epelsiban 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.

IC50 & Target

pKi: 9.9 (human oxytocin receptor)[1]
IC50: 192 nM (human oxytocin receptor)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
9.2 nM
Compound: GSK-557296
Antagonist activity at human OTR expressed in HEK293 cells assessed as decrease in calcium flux measured after 10 mins in presence of vasopressin by Fluo-4 dye based microplate reader based assay
Antagonist activity at human OTR expressed in HEK293 cells assessed as decrease in calcium flux measured after 10 mins in presence of vasopressin by Fluo-4 dye based microplate reader based assay
[PMID: 31223461]
体外研究
(In Vitro)

Epelsiban is a potent oxytocin receptor, with a pKi of 9.9 for human oxytocin receptor, >31000-fold selectivity over all three human vasopressin receptors hV1aR (pKi, <5.2), hV2R (pKi, <5.1), and hV1bR (pKi, 5.4), and shows no significant P450 inhibition[1].

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

Epelsiban 相关抗体:
体内研究
(In Vivo)

Epelsiban shows an IC50 of 192 nM for oxytocin receptor in rats. Epelsiban has low levels of intrinsic clearance against the microsomes of rat, dog, and cynomolgus monkey, good bioavailability (55%), but is negative in the genotoxicity screens with a satisfactory oral safety profile in female rats[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
NCT NumberSponsorConditionStart DatePhase
NCT01669083GlaxoSmithKline
Embryo Transfer
August 16, 2012Phase 1
NCT01021553GlaxoSmithKline
Premature Ejaculation
December 23, 2009Phase 2
NCT02213029GlaxoSmithKline
Embryo Transfer
August 28, 2014Phase 1
分子量

518.65

Formula

C30H38N4O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Epelsiban 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

Keywords:

Epelsiban872599-83-2GSK 557296GSK557296GSK-557296Oxytocin ReceptorOXTRInhibitorinhibitorinhibit

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目录号：
HY-105018
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