货号	规格	价格	上海	北京	珠海	重庆	武汉
S85103-1mg	≥98%	￥2390.00 S85103-1mg ￥2390.00 3-5天	0 货期：3-5天	-	-	-	-
S85103-5mg促销	≥98%	￥9500.00 ￥5800.00 S85103-5mg ￥5800.00 3-5天	0 货期：3-5天	-	-	-	-
S85103-10mg促销	≥98%	￥15800.00 ￥11000.00 S85103-10mg ￥11000.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

OT-R antagonist 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM). OT-R antagonist 1 is a new effective and selective nonpeptide low molecular weight OT-R antagonist.

体外研究：

OT-R antagonist 1 inhibits IP3-Synthesis, rat OT-R (IC50=0.03 uM). OT-R antagonist 1 inhibits phosphodiesterase IV (IC50 = 6.1 μM, a value about 300-fold higher than the affinity for 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. OT-R antagonist 1 displays a very clean selectivity profile with specific interaction with OT-R. Selectivity against vasopressin receptor subtypes is >6-fold for V1a and >350-fold for V2 and V1b

体内研究：

OT-R antagonist 1 significantly inhibits spontaneous uterine contractions in pregnant rats near term when administered intravenously or orally. Oxytocininduced contraction of isolated rat uterine strips is blocked by OT-R antagonist 1 (pA2 = 7.82). OT-R antagonist 1(single administration; i.v. or oral routes) causes dose-dependent inhibition of contractions elicited by repeated injections of oxytocin (ED50 = 3.5 mg/kg i.v. and 89 mg/kg p.o., respectively), in anesthetized nonpregnant rats

参考文献：

1. Serge Halazy, et al. Pharmaceutically active pyrrolidine derivatives as bax inhibitors. WO/2001072705/A1. 2. William Nadler, et al. Method for preparing pyrrolidine oximes. WO/2005082848/A2. 3. Serge Halazy, et al. Pharmaceutically active pyrrolidine derivatives as bax inhibitors.WO/2001074769/A1. 4. 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.

溶解性：

10 mM in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.121 ml	10.603 ml	21.207 ml
5 mM	0.424 ml	2.121 ml	4.241 ml
10 mM	0.212 ml	1.06 ml	2.121 ml
50 mM	0.042 ml	0.212 ml	0.424 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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