TRPM8-antagonist-2 - TRP Channel Antagonist - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETRPM8 antagonist 2Cat. No.: HY-112430CAS No.: 259674-19-6分式: CHNO分量: 398.5作靶點: TRP Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 D

2、MSO : 160 mg/mL (401.51 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.5094 mL 12.5471 mL 25.0941 mL5 mM 0.5019 mL 2.5094 mL 5.0188 mL10 mM 0.2509 mL 1.2547 mL 2.5094 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性

3、，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.67 mg/mL (6.70 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.67 mg/mL (6.70 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn

4、oilSolubility: 2.67 mg/mL (6.70 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 TRPM8 antagonist 2種有效的，選擇性的 TRPM8 拮抗劑，IC50 值為 0.2 nM，可于研究神經(jīng)性疼痛綜合癥。IC50 & Target IC50: 0.2 nM (TRPM8) 1體外研究 TRPM8 antagonist 2 (Compound 14) is a potent and selective TRPM8 antag

5、onist, with an IC50 of 0.2 nM,used in the research of neuropathic pain syndromes. TRPM8 antagonist 2 potently inhibits menthol-inducedincrease in intracellular Ca2+ levels in Ca2+ fluorimetric assays in HEK293 cells stably expressing the ratisoform of TRPM8 channels (IC50, 40 nM) 1.體內(nèi)研究 TRPM8 antago

6、nist 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 g, s.c.) attenuates Oxaliplatin (OXP)-induced cold allodynia in mice 1.PROTOCO

7、LAnimal Mice 1Administration 1 Icilin, a TRPM8 agonist, is dissolved in 20% DMSO and 1% Tween 80 in distilled water and injectedintraperitoneally (i.p.) in a volume of 10 mL/kg. Each animal is acclimatized for 30 min for two consecutivedays before icilin administration. TRPM8 antagonist 2 (compound

8、14) stock is prepared in DMSO and dilutedin saline for injections. Gabapentin is dissolved in saline and administered s.c. at the dose of 25 mg/kg 60min prior to icillin injection. Control animals receive the vehicle injection 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Bertamino A, et al. Identification of a Potent Tryptophan-Based TRPM8 Antagonist With in Vivo Analgesic Activity. J Med Chem. 2018Jul 10. doi: 10.1021/acs.jmedchem.8b00545.McePdfHeightCaution: Product has not been fully validated for medical a