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CAS No.: 259674-19-6

TRPM8 antagonist 2 Catalog No. CSN27198

Synonyms: TRPM8 Antagonist;HVN-74196

TRPM8 antagonist 14 is a tryptophan-derived selective TRPM8 antagonist with IC50 value of 0.2nM. It showed significant target coverage in both an icilin-induced WDS (at 1-30 mg/kg s.c.) and oxaliplatin-induced cold allodynia (at 0.1-1 μg s.c.) mice models.

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技术信息

生物活性

描述TRPM8 antagonist 14 is an effective selective TRPM8 antagonist with IC50 of 0.2 nm, which is used in the study of neuropathic pain syndrome. TRPM8 antagonist can effectively inhibit the increase of intracellular Ca2 + level induced by menthol in HEK293 cells stably expressing TRPM8 channel rat isoforms (ic50,40nm). RPM8 antagonist (1,10 and 30 mg / kg, s.c.) showed significant antinociceptive activity in a dose-dependent manner and inhibited wet dog milkshake (WDS) - like cold hypersensitivity in mice by 63% at 30 mg / kg. In addition, TRPM8 antagonist (0.1 and 1 μ g, s.c.) objective to alleviate the cold pain induced by oxaliplatin (oxp) in mice^[2]. In the wet dog shakes (WDS) assay, compound 14 (TRPM8 antagonist 14) dose-dependently blocks icilin-triggered shaking behaviors in mice. Upon local administration, compound 14 dose dependently inhibits cold allodynia evoked by the chemotherapy oxaliplatin in a murine model of peripheral neuropathy at microgram doses^[3].
参考文献

[1] Bertamino A, Iraci N, Ostacolo C, et al. Identification of a Potent Tryptophan-Based TRPM8 Antagonist With in Vivo Analgesic Activity. J Med Chem. 2018;61(14):6140-6152. doi:10.1021/acs.jmedchem.8b00545
[2] Bertamino A, Iraci N, Ostacolo C, Ambrosino P, Musella S, Di Sarno V, Ciaglia T, Pepe G, Sala M, Soldovieri MV, Mosca I, Gonzalez-Rodriguez S, Fernandez-Carvajal A, Ferrer-Montiel A, Novellino E, Taglialatela M, Campiglia P, Gomez-Monterrey I. Identification of a Potent Tryptophan-Based TRPM8 Antagonist With in Vivo Analgesic Activity. J Med Chem. 2018 Jul 26;61(14):6140-6152
[3] Journigan VB, Feng Z, Rahman S, Wang Y, Amin ARMR, Heffner CE, Bachtel N, Wang S, Gonzalez-Rodriguez S, Fernández-Carvajal A, Fernández-Ballester G, Hilton JK, Van Horn WD, Ferrer-Montiel A, Xie XQ, Rahman T. Structure-Based Design of Novel Biphenyl Amide Antagonists of Human Transient Receptor Potential Cation Channel Subfamily M Member 8 Channels with Potential Implications in the Treatment of Sensory Neuropathies. ACS Chem Neurosci. 2020 Feb 5;11(3):268-290

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5094 mL
- 12.5471 mL
- 25.0943 mL
- 5 mM
- 0.5019 mL
- 2.5094 mL
- 5.0189 mL
- 10 mM
- 0.2509 mL
- 1.2547 mL
- 2.5094 mL

技术信息

CAS号

259674-19-6

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H26N2O2

运输

蓝冰

分子量

398.50

别名

TRPM8 Antagonist;HVN-74196

溶解度

DMSO	80.0 mg/mL (200.8 mM)
Water	Insoluble
Ethanol	22.0 mg/mL (55.2 mM)

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