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. |
Solubility Information | DMSO : 120 mg/mL (280.08 mM), Sonication is recommended.
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Keywords | Inhibitor | TRPM8 | subfamily | cold-related | orally | clinical | menthol | TRP Channel | pain | PF-05105679 | Transient receptor potential channels | PF 05105679 | inhibit | cold | CMR1 | PF05105679 | melastatin |
Inhibitors Related | (+)-Camphor | AP 18 | Methyl syringate | Caffeic Acid | Oleoyl Serotonin | (-)-Menthol | Camphor | Pregnenolone | Probenecid | 1,4-Cineole | Methyl salicylate | SKF-96365 hydrochloride |
Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Drug Library |