L-371,257
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].
Product Specifications
CAS Number
162042-44-6
UNSPSC
12352005
Target
Oxytocin Receptor; Vasopressin Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein
Applications
Neuroscience-Neuromodulation
Field of Research
Endocrinology; Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/l-371-257.html
Purity
99.90
Solubility
DMSO : 8.33 mg/mL (ultrasonic)
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
Molecular Formula
C28H33N3O6
Molecular Weight
507.58
References & Citations
[1]Williams PD, et al. 1- (1-[4-[ (N-acetyl-4-piperidinyl) oxy]-2-methoxybenzoyl]piperidin-4- yl) -4H-3,1-benzoxazin-2 (1H) -one (L-371,257) : a new, orally bioavailable, non-peptide oxytocin antagonist. J Med Chem. 1995 Nov 10;38 (23) :4634-6.|[2]Tunstall BJ, et al. Oxytocin blocks enhanced motivation for alcohol in alcohol dependence and blocks alcohol effects on GABAergic transmission in the central amygdala. PLoS Biol. 2019 Apr 16;17 (4) :e2006421.|[3]Jacqueline M Ho, et al. Hindbrain oxytocin receptors contribute to the effects of circulating oxytocin on food intake in male rats. Endocrinology. 2014 Aug;155 (8) :2845-57.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
V1a Receptor
Available Sizes
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