1398583-31-7
1398583-31-7 structure
- Name: PF 05105679
- Chemical Name: 3-({[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino}methyl)benzoic acid
- CAS Number: 1398583-31-7
- Molecular Formula: C26H21FN2O3
- Molecular Weight: 428.455
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
- Create Date: 2018-06-26 05:39:13
- Modify Date: 2024-01-16 06:44:39
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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].
| Name | 3-({[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino}methyl)benzoic acid |
|---|---|
| Synonyms |
Benzoic acid, 3-[[[(1R)-1-(4-fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]-
3-({[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino}methyl)benzoic acid |
| 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]. |
|---|---|
| Related Catalog | |
| Target |
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. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 669.0±55.0 °C at 760 mmHg |
| Molecular Formula | C26H21FN2O3 |
| Molecular Weight | 428.455 |
| Flash Point | 358.4±31.5 °C |
| Exact Mass | 428.153625 |
| LogP | 4.57 |
| Vapour Pressure | 0.0±2.1 mmHg at 25°C |
| Index of Refraction | 1.661 |
| Storage condition | -20°C |
