| Name | PF-05105679 |
| Description | PF-05105679 is a selective TRPM8 antagonist (IC50 = 103 nM). PF-05105679 can be used in research on cold-related pain. |
| In vitro | PF-05105679 shows >100-fold selectivity across a range of different receptors, ion channels, and enzymes including the closely related TRPV1 and TRPA1 channels[1]. |
| In vivo | PF-05105679 (2, 20 mg/kg) shows a T1/2 of 3.6 hours, a CL of 19.8 mL/min/kg, and a Vss of 6.2 L/kg for rats. PF-05105679 (0.2 mg/kg for iv and 20mg/kg for oral gavage) displays a T1/2 of 3.9 hours, a CL of 31 mL/min/kg, and a Vss of 7.4 L/kg for dogs[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (9.34 mM), Sonication is recommended. DMSO : 120 mg/mL (280.08 mM), Sonication is recommended.
|
| Keywords | TRPVChannel | TRPV Channel | TRPM8 | TRPChannel | TRP Channel | Transient receptor potential channels | subfamily | PF-05105679 | PF05105679 | PF 05105679 | pain | orally | menthol | melastatin | Inhibitor | inhibit | cold-related | cold | CMR1 | clinical |
| Inhibitors Related | (+)-Camphor | Fingolimod hydrochloride | Caffeic Acid | Oleoyl Serotonin | (-)-Menthol | Camphor | Pregnenolone | Probenecid | 1,4-Cineole | Capsaicin | trans-Cinnamaldehyde | Methyl salicylate |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Clinical Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Ion Channel Targeted Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library |