OT-R拮抗剂1

更新时间：2025-08-25 12:32:31

OT-R拮抗剂1结构式	常用名	OT-R拮抗剂1	英文名	OT-R antagonist 1
	CAS号	364071-17-0	分子量	471.548
	密度	1.2±0.1 g/cm3	沸点	N/A
	分子式	C₂₈H₂₉N₃O₄	熔点	N/A
	MSDS	N/A	闪点	N/A

OT-R拮抗剂1用途

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)。

中文名	OT-R拮抗剂1
英文名	OT-R antagonist 1
英文别名	更多

描述	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)。
相关类别	信号通路 >> G 蛋白偶联受体/G 蛋白 >> 催产素受体研究领域 >> 其他
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. [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.

描述

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)。

相关类别

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 催产素受体

研究领域 >> 其他

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.

[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.

密度	1.2±0.1 g/cm3
分子式	C₂₈H₂₉N₃O₄
分子量	471.548
精确质量	471.215820
LogP	2.80
InChIKey	IBXGJPAYWMFXSF-UEEONYLUSA-N
SMILES	CON=C1CC(C(=O)NCC(O)c2ccccc2)N(C(=O)c2ccc(-c3ccccc3C)cc2)C1
折射率	1.618
储存条件	2-8℃

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VER...
来源：ChEMBL
靶标：Severe acute respiratory syndrome coronavirus 2
External Id：CHEMBL4513082

实验名称：Half life in pregnant rat
来源：ChEMBL
靶标：Rattus norvegicus
External Id：CHEMBL1253128

实验名称：Oral bioavailability in pregnant rat
来源：ChEMBL
靶标：Rattus norvegicus
External Id：CHEMBL1253127

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Cac...
来源：ChEMBL
靶标：Severe acute respiratory syndrome coronavirus 2
External Id：CHEMBL4303805

实验名称：Inhibition of oxytocin-induced uterine contraction in po dosed rat
来源：ChEMBL
靶标：Rattus norvegicus
External Id：CHEMBL1253126

实验名称：SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response f...
来源：ChEMBL
靶标：Replicase polyprotein 1ab
External Id：CHEMBL4495582

实验名称：Rat OT receptor (Vasopressin and oxytocin receptors)
来源：IUPHAR-DB
靶标：OT receptor (Vasopressin and oxytocin receptors) [Rattus norvegicus]
External Id：369_Rat

实验名称：Human OT receptor (Vasopressin and oxytocin receptors)
来源：IUPHAR-DB
靶标：OT receptor (Vasopressin and oxytocin receptors) [Homo sapiens]
External Id：369_Human

实验名称：Human V1A receptor (Vasopressin and oxytocin receptors)
来源：IUPHAR-DB
靶标：V1A receptor (Vasopressin and oxytocin receptors) [Homo sapiens]
External Id：366_Human

实验名称：Selectivity ratio of Ki for human oxytocin receptor Ki for human vasopressin V2 recep...
来源：ChEMBL
靶标：N/A
External Id：CHEMBL1253111

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(4Z)-N-[(2S)-2-Hydroxy-2-phenylethyl]-4-(methoxyimino)-1-[(2'-methylbiphenyl-4-yl)carbonyl]-L-prolinamide

LS-192629