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CAS: 851881-60-2
分子式: C20H17F2N3O2
分子量: 369.36
中文名称: 
(S)-(4-氟苯基)-3-[3-(4-氟苯基)-[1,2,4]二唑-5-基]哌啶-1-基甲酮
英文名称: 
adx47273
用途: ADX-47273是mGluR5正变构调节剂(PAM),EC50值为170nM。
推荐供应商
货号品牌产品名称规格包装、参考价格
A793190MACKLINADX4727310mM in DMSO484元/1ml;   咨询
储存:-20°C
A860964MACKLINADX47273>98%287元/5mg;   451元/10mg;   1450元/50mg;   咨询
储存:-20℃
状态:白色粉末
折射率:white solid
SML2271Sigma-AldrichADX-47273≥98% (HPLC)798.09元/5 MG;   3224.81元/25 MG;   咨询

产品说明

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 shows in vivo antipsychotic-like and procognitive efficacy in mice and rats in 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

产品性质

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 stringFC1=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
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
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