| Identification | Back Directory | [Name]
PF 05105679 | [CAS]
1398583-31-7 | [Synonyms]
PF 05105679
PF-05105679 >=98% (HPLC)
3-[[[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]benzoic acid
Benzoic acid, 3-[[[(1R)-1-(4-fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]- | [Molecular Formula]
C26H21FN2O3 | [MDL Number]
MFCD28386022 | [MOL File]
1398583-31-7.mol | [Molecular Weight]
428.45 |
| Chemical Properties | Back Directory | [Boiling point ]
669.0±55.0 °C(Predicted) | [density ]
1.308±0.06 g/cm3(Predicted) | [storage temp. ]
room temp | [solubility ]
DMSO: 10 mg/ml | [form ]
powder | [pka]
4.14±0.10(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
PF-05105679 is an orally active and selective TRPM8 antagonist with an IC50 of 103 nM. PF-05105679 has the potential for cold-related pain[1]. | [Biological Activity]
PF-05105679 is an antagonist of the TRP (transient receptor potential) channelalso known as the cold and menthol receptor 1 (CMR1)with an IC50 value of 103 nM. PF-05105679 is in clinical trials for neuropathic pain. Participants taking PF-05105679 could hold their hands in a bucket of ice water for a long time before feeling painand pain-alleviating effects matched those of oxycodone for about one hour after administration.''PF-05105679 is an antagonist of the TRP (transient receptor potential) channelalso known as the cold and menthol receptor 1 (CMR1)with an IC50 value of 103 nM. PF-05105679 is in clinical trials for neuropathic pain. Participants taking PF-05105679 could hold their hands in a bucket of ice water for a long time before feeling painand pain-alleviating effects matched those of oxycodone for about one hour after administration.
Transient receptor potential cation channel subfamily M member 8 (TRPM8) antagonistPF-05105679 [( | [in vivo]
PF-05105679 (0.2 mg/kg for iv and 20mg/kg for oral gavage) has 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].
PF-05105679 (2, 20 mg/kg) has 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[1].
| Animal Model: | Male beagle dogs (weight 10 to 15kg)[1] | | Dosage: | 0.2 mg/kg (iv) or 20 mg/kg (oral gavage)(Pharmacokinetic Analysis) | | Administration: | Iv or oral gavage | | Result: | Had a T1/2 of 3.9 hours, a CL of 31 mL/min/kg, and a Vss of 7.4 L/kg for dogs. |
| [IC 50]
TRPM8: 103 nM (IC50) | [References]
[1] Andrews MD, et al. Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain. ACS Med Chem Lett. 2015 Jan 30;6(4):419-24. DOI:10.1021/ml500479v |
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