OT-R antagonist 1|364071-17-0|(Oxytocin receptor antagonist 1)-陌孚医药/Medlife

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OT-R antagonist 1 (Synonyms: Oxytocin receptor antagonist 1)

目录号: PL08656

CAS No. :364071-17-0

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中文名称	OT-R antagonist 1
英文名称	OT-R antagonist 1
英文别名	2-Pyrrolidinecarboxamide, N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino)-1-[(2'-methyl[1,1'-bip henyl]-4-yl)carbonyl]-, (2S,4Z)-;2-PyrrolidinecarboxaMide, N-[(2S)-2-hydroxy-2-phenylethyl]-4-(MethoxyiMino)-1-[(2'-Methyl[1,1'-biphenyl]-4-yl)carbonyl]...;2-Pyrrolidinecarboxamide, N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino)-1-[(2'-methyl[1,1'-bip henyl]-4-yl)carbonyl]-, (2;Oxytocin receptor antagonist 1;OXYTOCIN RECEPTOR ANTAGONIST-I;OT-R antagonist 1;BDBM50326713;2-Pyrrolidinecarboxamide, N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino)-1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-, (2S,4Z)-;(S)-N-((S)-2-hydroxy-2-phenylethyl)-4-(methoxyimino)-1-(2''-methylbiphenylcarbonyl)pyrrolidine-2-carboxamide;(2s,4z)-n-[(2s)-2-hydroxy-2-phenylethyl]-4-(methoxyimino)-1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide
Cas No.	364071-17-0
分子式	C₂₈H₂₉N₃O₄
分子量	471.55
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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）。
生物活性	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 nM Target: oxytocin receptor in 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 >
性状	Solid
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[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.

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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