1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. TRP Channel
  3. PF-05105679

PF-05105679 

Cat. No.: HY-115506
Handling Instructions

PF-05105679 is an orally active and selective TRPM8 antagonist with an IC50 of 103 nM. TRPM8, also known as the cold and menthol receptor 1 (CMR1), is a member of the melastatin subfamily. PF-05105679 is used for clinical efficacy in cold-related pain.

For research use only. We do not sell to patients.

PF-05105679 Chemical Structure

PF-05105679 Chemical Structure

CAS No. : 1398583-31-7

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Description

PF-05105679 is an orally active and selective TRPM8 antagonist with an IC50 of 103 nM. TRPM8, also known as the cold and menthol receptor 1 (CMR1), is a member of the melastatin subfamily. PF-05105679 is used for clinical efficacy in cold-related pain[1].

IC50 & Target[1]

TRPM8

103 nM (IC50)

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[1].

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.
Molecular Weight

428.45

Formula

C₂₆H₂₁FN₂O₃

CAS No.

1398583-31-7

SMILES

O=C(O)C1=CC=CC(CN([[email protected]@H](C2=CC=C(F)C=C2)C)C(C3=CC4=CC=CC=C4N=C3)=O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

PF-05105679PF05105679PF 05105679TRP ChannelTransient receptor potential channelsorallyTRPM8coldmentholCMR1melastatinsubfamilyclinicalcold-relatedpainInhibitorinhibitorinhibit

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PF-05105679
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HY-115506
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