TC-I 2000TRPM8 blocker CAS# 1159996-20-9 |
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Quality Control & MSDS
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| Cas No. | 1159996-20-9 | SDF | Download SDF |
| PubChem ID | 57326210 | Appearance | Powder |
| Formula | C23H18F4N2O | M.Wt | 414.4 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO and to 20 mM in ethanol | ||
| Chemical Name | N-(4-fluorophenyl)-1-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-isoquinoline-2-carboxamide | ||
| SMILES | C1CN(C(C2=CC=CC=C21)C3=CC=C(C=C3)C(F)(F)F)C(=O)NC4=CC=C(C=C4)F | ||
| Standard InChIKey | ADCDUDFEGFKKQH-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C23H18F4N2O/c24-18-9-11-19(12-10-18)28-22(30)29-14-13-15-3-1-2-4-20(15)21(29)16-5-7-17(8-6-16)23(25,26)27/h1-12,21H,13-14H2,(H,28,30) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | TRPM8 channel blocker. Inhibits icilin-induced TRPM8 channel activation in rTRPM8-expressing CHO cells (IC50 = 53 nM). |
TC-I 2000 Dilution Calculator
TC-I 2000 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.4131 mL | 12.0656 mL | 24.1313 mL | 48.2625 mL | 60.3282 mL |
| 5 mM | 0.4826 mL | 2.4131 mL | 4.8263 mL | 9.6525 mL | 12.0656 mL |
| 10 mM | 0.2413 mL | 1.2066 mL | 2.4131 mL | 4.8263 mL | 6.0328 mL |
| 50 mM | 0.0483 mL | 0.2413 mL | 0.4826 mL | 0.9653 mL | 1.2066 mL |
| 100 mM | 0.0241 mL | 0.1207 mL | 0.2413 mL | 0.4826 mL | 0.6033 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Fused piperidines as a novel class of potent and orally available transient receptor potential melastatin type 8 (TRPM8) antagonists.[Pubmed:22329507]
J Med Chem. 2012 Feb 23;55(4):1593-611.
The transient receptor potential melastatin type 8 (TRPM8) is a nonselective cation channel primarily expressed in a subpopulation of sensory neurons that can be activated by a wide range of stimuli, including menthol, icilin, and cold temperatures (<25 degrees C). Antagonism of TRPM8 is currently under investigation as a new approach for the treatment of pain. As a result of our screening efforts, we identified tetrahydrothienopyridine 4 as an inhibitor of icilin-induced calcium influx in CHO cells expressing recombinant rat TRPM8. Exploration of the structure-activity relationships of 4 led to the identification of a potent and orally bioavailable TRPM8 antagonist, tetrahydroisoquinoline 87. Compound 87 demonstrated target coverage in vivo after oral administration in a rat pharmacodynamic model measuring the prevention of icilin-induced wet-dog shakes (WDS).
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