L-371,257

Research use only, not for human use.

L-371,257 is a competitive antagonist of oxytocin receptor with pA2 of 8.4 and Ki of 19 nM. L-371,257 shows a Ki of 3.7 nM for vasopressin receptor 1a.

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 : 8.33 mg/mL (16.41 mM; Ultrasonic )

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

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(-20℃)

With Ice Pack

≥ 2 years