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  3. GPCR/G Protein | G 蛋白偶联受体/G 蛋白
  4. GPCR/G Protein——Oxytocin Receptor
L-371,257
目录号 : KM7896 CAS No. : 162042-44-6 纯度 : 98%
Data Sheet 产品使用指南

L-371,257 是一种口服生物有效的，不能透过血脑屏障的，竞争性的，选择性催产素受体 (oxytocin receptor) 拮抗剂 (pA2=8.4)，对催产素受体 (Ki=19 nM) 和血管加压素 V1a 受体 (vasopressin V1a receptor，Ki=3.7 nM) 具有高亲和力。

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生物活性

L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM).

体内研究

Systemic administration of nonpenetrant oxytocin receptor antagonist L-371,257 (0.5 and 1.0 mg/kg; i.p. injection) stimulates weight gain in rats.

Animal Model: Six-hour fasted rats
Dosage: 0.5 and 1.0 mg/kg
Administration: Intraperitoneal injection (a single) 30-45 minutes prior to the start of the dark cycle and access to food; Intraperitoneal injection (given repeatedly) over 6 days.
Result: A single injection significantly stimulated weight gain at 0.5 and 1.0 mg/kg relative to vehicle treatment.
When given repeatedly over 6 days, 0.5 mg/kg significantly stimulated body weight gain (10.5±2.2 g) relative to vehicle treatment (4.7±2.7 g).
分子式
C28H33N3O6
分子量
507.58
CAS号
162042-44-6
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
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