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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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P287705-5mg | 5mg | In stock | $117.90 | |
P287705-10mg | 10mg | In stock | $197.90 | |
P287705-25mg | 25mg | In stock | $385.90 | |
P287705-50mg | 50mg | In stock | $593.90 | |
P287705-100mg | 100mg | In stock | $890.90 |
Selective TRPM8 blocker
Synonyms | CS-0087256 | PF 05105679 | (R)-3-((N-(1-(4-fluorophenyl)ethyl)quinoline-3-carboxamido)methyl)benzoic acid | SCHEMBL12487950 | PF05105679 | PF-05105679 | 1398583-31-7 | AKOS030210975 | Benzoic acid, 3-((((1R)-1-(4-fluorophenyl)ethyl)(3-quinolinylcarbonyl)a |
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Specifications & Purity | Moligand™, ≥98%(HPLC) |
Biochemical and Physiological Mechanisms | Selective TRPM8 blocker (IC50= 103 nM). Exhibits >100-fold selectivity for TRPM8 over a panel of receptors, ion channels and enzymes, including TRPV1 and TRPA1 ion channels. Reduces body temperature in rats and reverses cold-induced bladder capacity reduc |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | CHANNEL BLOCKER |
Mechanism of action | Channel blocker of TRPM8 |
Product Description | Introduction: 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. |
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IUPAC Name | 3-[[[(1R)-1-(4-fluorophenyl)ethyl]-(quinoline-3-carbonyl)amino]methyl]benzoic acid |
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INCHI | InChI=1S/C26H21FN2O3/c1-17(19-9-11-23(27)12-10-19)29(16-18-5-4-7-21(13-18)26(31)32)25(30)22-14-20-6-2-3-8-24(20)28-15-22/h2-15,17H,16H2,1H3,(H,31,32)/t17-/m1/s1 |
InChi Key | BXNMZRPTQFVRFA-QGZVFWFLSA-N |
Canonical SMILES | CC(C1=CC=C(C=C1)F)N(CC2=CC(=CC=C2)C(=O)O)C(=O)C3=CC4=CC=CC=C4N=C3 |
Isomeric SMILES | C[C@H](C1=CC=C(C=C1)F)N(CC2=CC(=CC=C2)C(=O)O)C(=O)C3=CC4=CC=CC=C4N=C3 |
Alternate CAS | 1398583-31-7 |
PubChem CID | 60195662 |
Molecular Weight | 428.45 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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K2211474 | Certificate of Analysis | Jul 30, 2022 | P287705 |
K2211477 | Certificate of Analysis | Jul 30, 2022 | P287705 |
K2211480 | Certificate of Analysis | Jul 30, 2022 | P287705 |
K2211481 | Certificate of Analysis | Jul 30, 2022 | P287705 |
K2211482 | Certificate of Analysis | Jul 30, 2022 | P287705 |
Solubility | Solvent:DMSO, Max Conc. mg/mL: 42.84, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 42.84, Max Conc. mM: 100 |
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Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H302:Harmful if swallowed |
Precautionary Statements | P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P270:Do not eat, drink or smoke when using this product. P330:Rinse mouth. P301+P317:IF SWALLOWED: Get medical help. |
RIDADR | NONHforallmodesoftransport |
1. Andrews MD, Af Forselles K, Beaumont K, Galan SR, Glossop PA, Grenie M, Jessiman A, Kenyon AS, Lunn G, Maw G et al.. (2015) Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain.. ACS Med Chem Lett, 6 (4): (419-24). [PMID:25893043] |