ChemicalBook > CAS DataBase List > PF 05105679

PF 05105679

Product Name: PF 05105679
CAS No.: 1398583-31-7
Chemical Name: PF 05105679
Synonyms: PF 0510567;PF 05105679;PF-05105679【PZ0245】;PF-05105679 >=98% (HPLC);PF-05105679, 10 mM in DMSO;(R)-3-((N-(1-(4-Fluorophenyl)ethyl)quinoline-3-carboxamido)methyl)benzoic acid;3-[[[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]benzoic acid;Benzoic acid, 3-[[[(1R)-1-(4-fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]-;Inhibitor,TRPM8,PF05105679,subfamily,cold-related,orally,clinical,menthol,TRP Channel,PF-05105679,pain,Transient receptor potential channels,PF 05105679,inhibit,cold,CMR1,melastatin
CBNumber: CB43146354
Molecular Formula: C26H21FN2O3
Formula Weight: 428.45
MOL File: 1398583-31-7.mol

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PF 05105679 Property

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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: PZ0245
Product name: PF-05105679
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $104.06
Updated: 2025/07/31

Sigma-Aldrich

Product number: PZ0245
Product name: PF-05105679
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $411.82
Updated: 2025/07/31

Cayman Chemical

Product number: 29489
Product name: PF-05105679
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 29489
Product name: PF-05105679
Packaging: 5mg
Price: $116
Updated: 2024/03/01

Cayman Chemical

Product number: 29489
Product name: PF-05105679
Packaging: 10mg
Price: $184
Updated: 2024/03/01

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PF 05105679 Chemical Properties,Usage,Production

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) channel, also 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 pain, and pain-alleviating effects matched those of oxycodone for about one hour after administration.', 'PF-05105679 is an antagonist of the TRP (transient receptor potential) channel, also 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 pain, and pain-alleviating effects matched those of oxycodone for about one hour after administration.
Transient receptor potential cation channel subfamily M member 8 (TRPM8) antagonist, PF-05105679 [(R)-3-[(1-(4-fluorophenyl)ethyl)(quinolin-3-ylcarbonyl)amino]methylbenzoic acid] acts as a clinical tool to assess the function of TRPM8 in modulating the body temperature. It also helps to determine its role in the treatment of pain in humans.

in vivo

PF-05105679 (0.2 mg/kg for iv and 20mg/kg for oral gavage) has a T_1/2 of 3.9 hours, a CL of 31 mL/min/kg, and a V_ss of 7.4 L/kg for dogs^[1].
PF-05105679 (2, 20 mg/kg) has a T_1/2 of 3.6 hours, a CL of 19.8 mL/min/kg, and a V_ss 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 T_1/2 of 3.9 hours, a CL of 31 mL/min/kg, and a V_ss 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

PF 05105679 Preparation Products And Raw materials

Raw materials

Preparation Products

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PF 05105679 Suppliers

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PF 05105679

3-[[[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]benzoic acid

Benzoic acid, 3-[[[(1R)-1-(4-fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]-

PF-05105679 >=98% (HPLC)

Inhibitor,TRPM8,PF05105679,subfamily,cold-related,orally,clinical,menthol,TRP Channel,PF-05105679,pain,Transient receptor potential channels,PF 05105679,inhibit,cold,CMR1,melastatin

(R)-3-((N-(1-(4-Fluorophenyl)ethyl)quinoline-3-carboxamido)methyl)benzoic acid

PF-05105679, 10 mM in DMSO

PF 0510567

PF-05105679【PZ0245】

1398583-31-7