S85646 |
Methoxy-PEPy |
源叶(MedMol) | 98% |
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- 产品描述: Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM. IC50 value: 1 nM Target: mGlu5R inhibitor Administration of [3H]methoxy-PEPy (50 microCi/kg i.v.) to mGlu5 receptor-deficient mice revealed binding at background levels in forebrain, whereas wild-type mice exhibited 14-fold higher binding in forebrain relative to cerebellum . The calcium transients stimulated by these agonists were potently inhibited by reference allosteric mGlu5 antagonists - 2-methyl-6-(phenylethynyl)pyridine (MPEP), 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) and 3-methoxy-5-(pyridine-2-ylethynyl)pyridine (methoxy-PEPy) (IC(50) ranges: 0.8-66 nM)
- 靶点: mGlu5 Receptor:1 nM (IC50);GluR
- 参考文献:
1. Cosford ND, et al. [3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor. Bioorg Med Chem Lett. 2003 Feb 10;13(3):351-4. 2. Anderson JJ, et al. In vivo receptor occupancy of mGlu5 receptor antagonists using the novel radioligand [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine). Eur J Pharmacol. 2003 Jul 18;473(1):35-40. 3. Salisbury BG, et al. Inducible expression and pharmacological characterization of the mouse metabotropic glutamate 5b receptor. Eur J Pharmacol. 2008 Jan 28;579(1-3):34-9.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 4.757 ml 23.783 ml 47.567 ml 5 mM 0.951 ml 4.757 ml 9.513 ml 10 mM 0.476 ml 2.378 ml 4.757 ml 50 mM 0.095 ml 0.476 ml 0.951 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)