A TRPM8 antagonist
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PF-05105679

Item No. 29489

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[[(1R)-1-(4-fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]-benzoic acid
CAS Number
1398583-31-7
Molecular Formula
C26H21FN2O3
Formula Weight
428.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mg/ml
λmax
232 nm
SMILES
O=C(N([C@@H](C1=CC=C(F)C=C1)C)CC2=CC=CC(C(O)=O)=C2)C3=CC4=C(C=CC=C4)N=C3
InChi Code
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
InChi Key
BXNMZRPTQFVRFA-QGZVFWFLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $128

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    10 mg

    $203

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    Product Description

    PF-05105679 is an antagonist of transient receptor potential melastatin 8 (TRPM8; IC50 = 103 nM for inhibition of voltage-activated currents in HEK293 cells expressing the human receptor).1 It is greater than 100-fold selective for TRPM8 over a panel of 90 receptors, ion channels, and enzymes. PF-05105679 inhibits calcium flux induced by cold or the TRPM8 agonist WS-12 in HEK293 cells expressing the human TRPM8 (IC50s = 480 and 181 nM, respectively). Intravenous infusion of PF-05105679 (46.67 μg/kg per minute) reverses cold-induced reductions in bladder capacity in anesthetized guinea pigs. It decreases the core body temperature in rats when administered at doses of 100 and 300 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Winchester, W.J., Gore, K., Glatt, S., et al. Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans. J. Pharmacol. Exp. Ther. 351(2), 259-269 (2014).