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SHR1653 Sale

目录号 : GC37635

SHR1653是强效的、选择性的、能透过大脑的催产素受体 (OTR) 的拮抗剂,对hOTR 的 IC50 值为 15 nM。

SHR1653 Chemical Structure

Cas No.:2231770-73-1

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Sample solution is provided at 25 µL, 10mM.

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产品描述

SHR1653 is a highly potent, selective and brain penetrated oxytocin receptor (OTR) antagonist, with an IC50 of 15 nM for hOTR[1]. IC50: 15 nM (hOTR)[1].

[1]. Li X, et al. Discovery of SHR1653, a Highly Potent and Selective OTR Antagonist with Improved Blood-Brain Barrier Penetration. ACS Med Chem Lett. 2019 May 29;10(6):996-1001.

Chemical Properties

Cas No. 2231770-73-1 SDF
Canonical SMILES COC1=CC=C(N2C(N3C[C@@]4(C5=CC=C(F)C=C5Cl)C[C@@]4([H])C3)=NN=C2COC)C=N1
分子式 C21H21ClFN5O2 分子量 429.88
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.3262 mL 11.6312 mL 23.2623 mL
5 mM 0.4652 mL 2.3262 mL 4.6525 mL
10 mM 0.2326 mL 1.1631 mL 2.3262 mL
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Research Update

Discovery of SHR1653, a Highly Potent and Selective OTR Antagonist with Improved Blood-Brain Barrier Penetration

ACS Med Chem Lett 2019 May 29;10(6):996-1001.PMID:31223461DOI:PMC6580551

The oxytocin receptor (OTR) plays a major role in the control of male sexual responses. Antagonists of the OTR have been reported to inhibit ejaculation in animal models and serve as a potential treatment for premature ejaculation (PE). Herein, we describe a novel scaffold featuring an aryl substituted 3-azabicyclo [3.1.0] hexane structure. The lead compound, SHR1653, was shown to be a highly potent OTR antagonist, which exhibited excellent selectivity over V1AR, V1BR, and V2R. This novel molecule was shown to have a favorable pharmacokinetic profile across species, as well as robust in vivo efficacy in a rat uterine contraction model. Interestingly, SHR1653 exhibited excellent blood-brain barrier penetration, which might be beneficial for the treatment of CNS-related PE.