L-371,257

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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).

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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).

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GPCR/G Protein

Orexin Receptor

Oxytocin Receptor | Vasopressin Receptor

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162042-44-6

507.58

C28H33N3O6

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 8.33 mg/mL (16.41 mM; 超声助溶 )

COc1cc(OC2CCN(CC2)C(C)=O)ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2ccccc12

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(-20℃)

With Ice Pack

≥ 2 years