| 货号 | 2448/50 |
| 别名 | 6-Amino-N-cyclohexyl-N,3-dimethylth |
| 供应商 | Tocris |
| 生物活性 | Non-competitive antagonist with high affinity and selectivity for mGlu1 receptors (Ki = 19 nM); inactive at other mGlu receptor subtypes (mGlu2-7), ionotropic receptors and glutamate transporters (IC50 > 10 μM). Inhibits glutamate-induced IP production more potently than CPCCOEt (IC50 values are 16 nM and 6.3 μM respectively), and is orally active in vivo, demonstrating an antinociceptive effect in hyperalgesic mice. Desmethyl derivative (Cat. No. 2447) also available. |
| 运输条件 | Blue Ice |
| 存放说明 | 4℃ |
| 纯度 | >99 % |
| 计算分子量 | 378.92 |
| 分子式 | C18H22N4OS.HCl |
| 可溶性/溶解性 | Soluble to 100 mM in water |
| CAS号 | 748758-45-4 |
| 参考文献 | Emeryet al (2010) The protective signaling of metabotropic glutamate receptor 1 is mediated by sustained, β-arrestin-1-dependent ERK phosphorylation. J.Biol.Chem. 285 26041. PMID: 20566651. Koharaet al (2005) Radioligand binding properties and pharmacological characterization of 6-Amino-N-cyclohexyl-N,3-dimethyl-thiazolo[3,2-a]-benzimidazole-2-carboxamide (YM-298198), a high-affinity, selective and noncompetitive antagonist of metabotropic glutamate receptor type 1. J.Pharmacol.Exp.Ther. 315 163. PMID: 15976016. |