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Submit ReviewPF 05105679 is a selective TRPM8 blocker (IC50 = 103 nM) that exhibits >100-fold selectivity for TRPM8 over a panel of receptors, ion channels and enzymes, including TRPV1 and TRPA1 ion channels. PF 05105679 reduces body temperature in rats and reverses cold-induced bladder capacity reduction in guinea pigs. This compound is orally bioavailable.
Sold for research purposes under agreement from Pfizer Inc
The Chemical Probes pages of the Structural Genomics Consortium website are a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PF 05105679 is reviewed.
分子量 | 428.45 |
公式 | C26H21FN2O3 |
储存 | Store at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 1398583-31-7 |
PubChem ID | 60195662 |
InChI Key | BXNMZRPTQFVRFA-QGZVFWFLSA-N |
Smiles | C[C@H](C1=CC=C(C=C1)F)N(C(C2=CC3=C(N=C2)C=CC=C3)=O)CC4=CC(C(O)=O)=CC=C4 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Andrews et al (2015) Discovery of a selective TRPM8 antagonist with clinical efficacy in cold-related pain. ACS Med.Chem.Lett. 6 419 PMID: 25893043
Winchester et al (2014) Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans. J.Pharmacol.Exp.Ther. 351 259 PMID: 25125580
关键词: PF 05105679, PF 05105679 supplier, PF05105679, selective, transient-receptor-potential, TRPM8, ion, channels, blocks, blockers, orally, bioavailable, TRPM, 6003, Tocris Bioscience
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