中文名 | TRPM8 antagonist 2 |
英文名 | TRPM8 antagonist 2 |
别名 | 化合物TRPM8 ANTAGONIST 2 TRPM8 ANTAGONIST 2 游离 (S)-2-(二苄氨基)-3-(1H-吲哚-3-基)丙酸甲酯 |
英文别名 | 259674-19-6 TRPM8 Antagonist TRPM8 ANTAGONIST TRPM8 antagonist 2 Methyl N,N-dibenzyl-L-tryptophanate Methyl Na,Na-dibenzyl-L-tryptophanate L-Tryptophan, N,N-bis(phenylmethyl)-, methyl ester |
CAS | 259674-19-6 |
化学式 | C26H26N2O2 |
分子量 | 398.5 |
密度 | 1.195±0.06 g/cm3(Predicted) |
沸点 | 567.5±50.0 °C(Predicted) |
溶解度 | DMSO: 160毫克/毫升 (401.51毫米; 需要超声波) |
酸度系数 | 17.02±0.30(Predicted) |
存储条件 | under inert gas (nitrogen or Argon) at 2-8°C |
体外研究 | TRPM8 antagonist 2 (Compound 14) is a potent and selective TRPM8 antagonist, with an IC 50 of 0.2 nM, used in the research of neuropathic pain syndromes. TRPM8 antagonist 2 potently inhibits menthol-induced increase in intracellular Ca 2+ levels in Ca 2+ fluorimetric assays in HEK293 cells stably expressing the rat isoform of TRPM8 channels (IC 50 , 40 nM). |
体内研究 | TRPM8 antagonist 2 (1, 10, and 30 mg/kg, s.c.) shows a marked, dose-dependent antinociceptive activity, and inhibits wet-dog shakes (WDS)-like cold hypersensitivity in mice by 63% at 30 mg/kg. In addition, TRPM8 antagonist 2 (0.1 and 1 μg, s.c.) attenuates Oxaliplatin (OXP)-induced cold allodynia in mice. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.509 ml | 12.547 ml | 25.094 ml |
5 mM | 0.502 ml | 2.509 ml | 5.019 ml |
10 mM | 0.251 ml | 1.255 ml | 2.509 ml |
5 mM | 0.05 ml | 0.251 ml | 0.502 ml |
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