162042-44-6

Basic information

• Product Name: L371,257
• Synonyms: L371,257;1-[4-[(1-Acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]-4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidine;1-[1-[4-(1-acetylpiperidin-4-yl)oxy-2-methoxybenzoyl]piperidin-4-yl]-4H-3,1-benzoxazin-2-one
• CAS NO: 162042-44-6
• Molecular Formula: C28H33N3O6
• Molecular Weight: 507.584
• Mol File: 162042-44-6.mol
• Article Data: 1

Chemical Properties

• Boiling Point: 728.9±60.0 °C(Predicted)
• Appearance: /
• Density: 1.282±0.06 g/cm3(Predicted)
• Storage Temp.: Store at RT
• PKA: 0.73±0.20(Predicted)
• CAS DataBase Reference: L371,257(CAS DataBase Reference)
• NIST Chemistry Reference: L371,257(162042-44-6)
• EPA Substance Registry System: L371,257(162042-44-6)

Safety Data

• Hazardous Substances Data: 162042-44-6(Hazardous Substances Data)

Usage

Description

L371,257 is a potent antagonist that effectively counteracts oxytocin-induced contractions in the rat uterus, both in vitro and in vivo. It is characterized by its significant oral bioavailability in rats, making it a valuable compound for research and potential therapeutic applications.

Uses

Used in Pharmaceutical Research:
L371,257 is used as a research compound for studying the effects of oxytocin on uterine contractions. Its antagonistic properties allow scientists to investigate the role of oxytocin in various physiological processes and conditions, such as labor and postpartum hemorrhage.
Used in Drug Development:
L371,257 is used as a starting point for the development of new drugs targeting oxytocin receptors. Its antagonistic activity and oral bioavailability make it a promising candidate for the creation of medications aimed at treating conditions related to uterine contractions, such as preterm labor and other gynecological disorders.
Used in Preclinical Studies:
L371,257 is used as a preclinical tool to evaluate the efficacy and safety of potential therapeutic agents targeting oxytocin receptors. Its ability to block oxytocin-induced contractions in rats provides a valuable model for assessing the potential benefits and risks of new drugs in a controlled environment before proceeding to human trials.

Biological Activity

Potent, high affinity human oxytocin (OT) receptor antagonist (K i = 4.6 nM) that displays > 800-fold selectivity over human arginine vasopressin receptors V 1a and V 2 . Antagonizes oxytocin-induced contractions in isolated rat uterine tissue (pA 2 = 8.44) and in anesthetised rats following intravenous and intraduodenal administration. Orally active.

Upstream product

• 108-24-7 acetic anhydride 
• 5344-90-1 2-Aminobenzyl alcohol 
• 2150-47-2 methyl 2,4-dihydroxybenzoate 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 
• 109384-19-2 t-butyl 4-hydroxy piperidine-1-carboxylate 
• 162045-29-6 1-(tert-Butoxycarbonyl)-4-[(2-hydroxymethylphenyl)amino]piperidine 
• 162045-36-5 4-(N-t-Butoxycarbonyl-4-piperidinyloxy)-2-hydroxybenzoic acid methyl ester 
• 162045-38-7 4-(N-t-Butoxycarbonyl-4-piperidinyloxy)-2-methoxy-benzoic acid 
• 162045-37-6 4-(N-t-Butoxycarbonyl-4-piperidinyloxy)-2-methoxybenzoic acid methyl ester 
• 162045-30-9 1-(N-t-butyloxy-carbonyl-4-piperidinyl)-4H-3,1-benzoxazin-2(1H)-one 
• 162045-31-0 1-piperidin-4-yl-1,4-dihydro-2H-3,1-benzoxazin-2-one hydrochloride 
• 162042-41-3 4-{3-Methoxy-4-[4-(2-oxo-4H-benzo[d][1,3]oxazin-1-yl)-piperidine-1-carbonyl]-phenoxy}-piperidine-1-carboxylic acid tert-butyl ester 

Relevant articles and documents

1--2-methoxybenzoyl>piperidin-4-yl>-4H-3,1-benzoxazin-2(1H)-one (L-371,257): A New, Orally Bioavailable, Non-Peptide Oxytocin Antagonist

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