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
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
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.
N-Bromosuccinimide Price
- Product number
- PZ0245
- Product name
- PF-05105679
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $104.06
- Updated
- 2025/07/31
- Product number
- PZ0245
- Product name
- PF-05105679
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $411.82
- Updated
- 2025/07/31
- Product number
- 29489
- Product name
- PF-05105679
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 29489
- Product name
- PF-05105679
- Packaging
- 5mg
- Price
- $116
- Updated
- 2024/03/01
- Product number
- 29489
- Product name
- PF-05105679
- Packaging
- 10mg
- Price
- $184
- Updated
- 2024/03/01
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 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. |
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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