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ADX-47273

品牌
Sigma-Aldrich
CAS
851881-60-2
货号
SML2271
规格纯度
≥98% (HPLC)
价格
798.09 *本价格含增值税费
促销
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数量
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半岛bd体育手机客户端 名称:
851881-60-2
ADX-47273
ADX47273
(S)-(4-Fluorophenyl)-{3-[3-(4-fluorophenyl)-[1,2,4]oxadiazol-5-yl]-piperidin-1-yl}-methanone
(4-Fluorophenyl)[(3S)-3-[3-(4-fluorophenyl)-1,2,4-oxadiazol-5-yl]-1-piperidinyl]methanone
ADX 47273
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 说明

生化/生理作用

ADX-47273 is a brain-penetrating, potent and selective metabotropic glutamate receptor 5 (mGlu5; mGluR5) positive allosteric modulator (PAM) that enhances glutamate-stimulated Ca2+ response in rat cortical astrocytes (EC50 = 170 nM, Emax = 380%; [glutamate] = EC20 = 200 nM) via direct mGlu5 binding in a MPEP-, but not Quisqualate-, competitive manner (Ki = 4.3 μM against 2 nM MPEP; rat mGlu5 HEK293) with little mGlu5 agonist activity, no potency toward other rat/human family III GPCRs (mGlu1–8 and GABA-B), nor affinity to 56 GPCRs/transporters/enzymes/ion channels. ADX-47273 showsin vivoantipsychotic-like and procognitive efficacy in mice and ratsin vivo(1-300 mg/kg i.p.) with good pharmacokinetic properties (B/P ratio >2, bioavailability ~40%, T1/2 ~2 hrs in rats).

基本信息

经验(实验)分子式 C20H17F2N3O2
分子量 369.36
MDL编号 MFCD17167026

半岛bd体育手机客户端 性质

测定 ≥98% (HPLC)
形式 powder
旋光性 [α]/D +90 to +110°, c = 0.1 in chloroform-d
颜色 white to beige
溶解性 DMSO: 2 mg/mL, clear
储存温度 ?20℃
SMILES string FC1=CC=C(C=C1)C2=NOC([C@@H]3CN(CCC3)C(C4=CC=C(C=C4)F)=O)=N2

安全信息

储存分类代码 13 - Non Combustible Solids
WGK WGK 3
闪点(F) Not applicable
闪点(C) Not applicable

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