TRPM8 antagonist 2 ≥98%
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| 包装规格: | 5mg 10mg 50mg 100mg in glass bottle |
| 溶解性: | 溶于DMSO(160mg/ml 超声) |
| 产品描述: | 基本信息 产品编号: T11144 产品名称: TRPM8 antagonist 2 CAS: 259674-19-6 储存条件 粉末 -20℃ 四年 分子式: C26H26N2O2 溶于液体 -80℃ 6个月 分子量: 398.50 -20℃ 1个月 化学名: methyl (2S)-2-(dibenzylamino)-3-(1H-indol-3-yl)propanoate Solubility (25°C): 体外: DMSO 80mg/mL (200.75mM) Ethanol 22mg/mL (55.2mM) Water Insoluble 体内(现配现用): <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 制备储备液 浓度 溶液体积 质量 1mg 5mg 10mg 1mM 2.5094mL 12.5471mL 25.0941mL 5mM 0.5019mL 2.5094mL 5.0188mL 10mM 0.2509mL 1.2547mL 2.5094mL 50mM 0.0502mL 0.2509mL 0.5019mL 生物活性 产品描述 一种有效的,选择性的TRPM8拮抗剂。 靶点 TRPM8(Cell-free assay) 0.2nM 体外研究 TRPM8 antagonist 2 (Compound 14) is a potent and selective TRPM8 antagonist,with an IC50 of 0.2nM,used in the research of neuropathic pain syndromes.TRPM8 antagonist 2 potently inhibits menthol-induced increase in intracellular Ca2+ levels in Ca2+ fluorimetric assays in HEK293 cells stably expressing the rat isoform of TRPM8 channels (IC50,40nM). 体内研究 TRPM8 antagonist 2 (1,10,and 30mg/kg,s.c.) shows a marked,dose-dependent antinociceptive activity,and inhibits wetdog shakes (WDS)-like cold hypersensitivity in mice by 63% at 30mg/kg.In addition,TRPM8 antagonist 2 (0.1 and 1μg,s.c.) attenuates Oxaliplatin (OXP)-induced cold allodynia in mice. 推荐实验方法(仅供参考) 动物实验: Mice Icilin,a TRPM8 agonist,is dissolved in 20% DMSO and 1% Tween 80 in distilled water and injected intraperitoneally (i.p.) in a volume of 10mL/kg.Each animal is acclimatized for 30 min for two consecutive days before icilin administration.TRPM8 antagonist 2 (compound 14) stock is prepared in DMSO and diluted in saline for injections.Gabapentin is dissolved in saline and administered s.c.at the dose of 25mg/kg 60 min prior to icillin injection.Control animals receive the vehicle injection. |
| 保存条件: | -20℃ |
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