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OT-R antagonist 1
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。
OT-R antagonist 1图片
CAS NO:364071-17-0
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
OT-R antagonist 1是一种新型有效的选择性非肽类OT-R拮抗剂, 抑制催产素诱发的细胞内Ca2+活动(IC50=8nM)。
Cas No.364071-17-0
别名Oxytocin receptor antagonist 1
Canonical SMILESO=C([C@H](C/1)N(C(C2=CC=C(C3=CC=CC=C3C)C=C2)=O)CC1=N/OC)NC[C@@H](O)C4=CC=CC=C4
分子式C28H29N3O4
分子量471.55
溶解度Soluble in DMSO
储存条件Store at -20°C
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

OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist. OT-R antagonist 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM).IC50 value: 8 nMTarget: oxytocin receptorin vitro: OT-R antagonist 1 inhibitis IP3-Synthesis, rat OT-R (IC50=0.03 uM). [4] OT-R antagonist 1 inhibits phosphodiesterase IV with IC50 = 6.1 μM, a value about 300-fold higher than the affinity for OT-R. OT-R antagonist 1 shows a very clean selectivity profile with specific interaction with OT-R. OT-R antagonist 1 competitively inhibits binding of [3H]oxytocin and the peptide antagonist 125I-ornithine vasotocin analog to human and rat oxytocin receptor expressed in human embryonic kidney 293-EBNA or Chinese hamster ovary cells with nanomolar potency. Selectivity against vasopressin receptor subtypes is >6-fold for V1a and >350-fold for V2 and V1b. [1]in vivo: Oxytocininduced contraction of isolated rat uterine strips is blocked by OT-R antagonist 1 (pA2 = 7.82). In anesthetized nonpregnant rats, single administration of OT-R antagonist 1 by i.v. or oral routes causes dose-dependent inhibition of contractions elicited by repeated injections of oxytocin with ED50 = 3.5 mg/kg i.v. and 89 mg/kg p.o., respectively. OT-R antagonist 1 significantly inhibits spontaneous uterine contractions in pregnant rats near term when administered intravenously or orally. [1]

[1]. Serge Halazy, et al. Pharmaceutically active pyrrolidine derivatives as bax inhibitors. WO/2001072705/A1. [2]. Cirillo R, et al. Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor. J Pharmacol Exp Ther. 2003 Jul;306(1):253-61. [3]. William Nadler, et al. Method for preparing pyrrolidine oximes. WO/2005082848/A2. [4]. Serge Halazy, et al. Pharmaceutically active pyrrolidine derivatives as bax inhibitors.WO/2001074769/A1.