PF 05105679

Discontinued Product

6003 has been discontinued.

View all TRPM Channels products.
说明: Selective TRPM8 blocker
化学名: 3-[[[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]benzoic acid
纯度: ≥98% (HPLC)
说明书
引用文献
评论

生物活性 for PF 05105679

PF 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.

许可信息

Sold for research purposes under agreement from Pfizer Inc

External Portal Information for PF 05105679

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.

技术数据 for PF 05105679

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 for PF 05105679

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

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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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