Description
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.
Product information
CAS Number: 1398583-31-7
Molecular Weight: 428.45
Formula: C26H21FN2O3
Chemical Name: 3-({N-[(1R)-1-(4-fluorophenyl)ethyl]-1-(quinolin-3-yl)formamido}methyl)benzoic acid
Smiles: C[C@H](C1C=CC(F)=CC=1)N(CC1=CC(=CC=C1)C(O)=O)C(=O)C1=CN=C2C=CC=CC2=C1
InChiKey: BXNMZRPTQFVRFA-QGZVFWFLSA-N
InChi: InChI=1S/C26H21FN2O3/c1-17(19-9-11-23(27)12-10-19)29(16-18-5-4-7-21(13-18)26(31)32)25(30)22-14-20-6-2-3-8-24(20)28-15-22/h2-15,17H,16H2,1H3,(H,31,32)/t17-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
PF-05105679 demonstrates >100-fold selectivity across a range of different receptors, ion channels, and enzymes including the closely related TRPV1 and TRPA1 channels. TRPM8, also known as the cold and menthol receptor 1 (CMR1), is a member of the melastatin subfamily.
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. 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.
Products are for research use only. Not for human use.
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