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L-371,257
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
L-371,257图片
CAS NO:162042-44-6
包装:10mg
市场价:2430元

产品介绍
L-371,257 是一种口服生物可利用的、非血脑屏障渗透剂、选择性和竞争性催产素受体 (pA2=8.4) 拮抗剂,对催产素受体 (Ki=19 nM) 和加压素 V1a 受体 (Ki=3.7) 具有高亲和力nM)。
Cas No.162042-44-6
化学名1-(1-(4-((1-acetylpiperidin-4-yl)oxy)-2-methoxybenzoyl)piperidin-4-yl)-1H-benzo[d][1,3]oxazin-2(4H)-one
Canonical SMILESO=C(C(C(OC)=C1)=CC=C1OC2CCN(C(C)=O)CC2)N3CCC(CC3)N4C5=CC=CC=C5COC4=O
分子式C28H33N3O6
分子量507.59
溶解度<5.08mg/ml in DMSO
储存条件Store at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

References:
[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.