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

PF-05105679 

Cat. No.: HY-115506 Purity: 99.95%
COA Handling Instructions

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.

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. PF-05105679 has the potential for 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].
TRPM8, also known as the cold and menthol receptor 1 (CMR1), is a member of the melastatin subfamily[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

428.45

Formula

C26H21FN2O3

CAS No.
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (291.75 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3340 mL 11.6700 mL 23.3399 mL
5 mM 0.4668 mL 2.3340 mL 4.6680 mL
10 mM 0.2334 mL 1.1670 mL 2.3340 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.95%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
PF-05105679
Cat. No.:
HY-115506
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