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TRPM8 antagonist 2

TRPM8 antagonist 2 是有效的 RPM8选择性 T 拮抗剂，IC50值为 0.2 nM，在神经性疼痛综合症中有研究价值。

CAS号

259674-19-6

分子式

C26H26N2O2

主要靶点

TRP/TRPV Channel

仅限科研使用

Cat No : CM06806

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Synonyms

验证数据展示

  • CAS No.: 259674-19-6

    TRPM8 antagonist 2
    CAS#: 259674-19-6

产品信息

TRPM8 antagonist 2 is a potent and selective TRPM8 antagonist with an IC50 of 0.2 nM. TRPM8 antagonist 2 is used in the research of neuropathic pain syndromes.

CAS号 259674-19-6
分子式 C26H26N2O2
主要靶点 TRP/TRPV Channel
主要通路 离子通道
分子量 398.5
纯度 98.00%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

TRPM8:0.2 nM

体内活性

TRPM8 antagonist 2 (1, 10, and 30 mg/kg, s.c.) exhibits a marked, dose-dependent antinociceptive activity, and inhibits wet-dog shakes (WDS)-like cold hypersensitivity in mice by 63% at 30 mg/kg. Moreover, TRPM8 antagonist 2 (0.1 and 1 μg, s.c.) attenuates Oxaliplatin (OXP)-induced cold allodynia in mice.

体外活性

TRPM8 antagonist 2 (Compound 14) is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, 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, 40 nM).

溶解度

DMSO:160 mg/mL (401.51 mM)

参考文献

1.Alessia B , Nunzio I , Carmine O , et al. Identification of a Potent Tryptophan-based TRPM8 Antagonist With in vivo Analgesic Activity[J]. Journal of Medicinal Chemistry, 2018:acs.jmedchem.8b00545-.

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