| CAS: | 851881-60-2 | |
| 分子式: | C20H17F2N3O2 | |
| 分子量: | 369.36 | |
| 中文名称: |
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| 英文名称: |
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| 用途: | ADX-47273是mGluR5正变构调节剂(PAM),EC50值为170nM。 |
| 货号 | 品牌 | 产品名称 | 规格 | 包装、参考价格 | |||||||||||||||||||||||||||||||
| A793190 | MACKLIN | ADX47273 | 10mM in DMSO | 484元/1ml; | 咨询 | ||||||||||||||||||||||||||||||
储存:-20°C | |||||||||||||||||||||||||||||||||||
| A860964 | MACKLIN | ADX47273 | >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 | |||||||||||||||||||||||||||||||||||
| SML2271 | Sigma-Aldrich | ADX-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
产品性质
安全信息
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