1. GPCR/G Protein
  2. Oxytocin Receptor
    Vasopressin Receptor
  3. L-371,257

L-371,257 

Cat. No.: HY-15010 Purity: >99.0%
Handling Instructions

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).

For research use only. We do not sell to patients.

L-371,257 Chemical Structure

L-371,257 Chemical Structure

CAS No. : 162042-44-6

Size Price Stock
10 mM * 1 mL in DMSO USD 436 Ask For Quote & Lead Time
5 mg USD 390 Ask For Quote & Lead Time

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Description

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)[1][2].

IC50 & Target

Ki: 19 nM (oxytocin receptor), 3.7 nM (vasopressin V1a receptor)[2]

In Vivo

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[3].

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

Animal Model: Six-hour fasted rats[3]
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).
Molecular Weight

507.58

Formula

C₂₈H₃₃N₃O₆

CAS No.

162042-44-6

SMILES

O=C(OC1)N(C2CCN(C(C3=C(OC)C=C(OC4CCN(C(C)=O)CC4)C=C3)=O)CC2)C5=C1C=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References
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Keywords:

L-371,257Oxytocin ReceptorVasopressin ReceptorOXTRorallybioavailablenon-blood-brainbarrierpenetrantInhibitorinhibitorinhibit

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L-371,257
Cat. No.:
HY-15010
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