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PF-05105679

Catalog No. T16483 CAS 1398583-31-7

PF-05105679 is a selective TRPM8 antagonist (IC50 = 103 nM). PF-05105679 can be used in research on cold-related pain.

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PF-05105679, CAS 1398583-31-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 41.00
2 mg	In stock	$ 59.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 163.00
25 mg	In stock	$ 322.00
50 mg	In stock	$ 497.00
100 mg	In stock	$ 747.00
200 mg	In stock	$ 987.00
500 mg	In stock	$ 1,520.00
1 mL * 10 mM (in DMSO)	In stock	$ 97.00

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Purity: 99.82%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PF-05105679 is a selective TRPM8 antagonist (IC50 = 103 nM). PF-05105679 can be used in research on cold-related pain.
Targets&IC50	TRPM8:103 nM
In vitro	PF-05105679 shows >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 (2, 20 mg/kg) shows 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. PF-05105679 (0.2 mg/kg for iv and 20mg/kg for oral gavage) displays 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].

Molecular Weight	428.45
Formula	C26H21FN2O3
CAS No.	1398583-31-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 120 mg/mL (280.08 mM), Sonification is recommended.

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Neuronal Signaling Compound Library Bioactive Compounds Library Max ReFRAME Related Library Bioactive Compound Library Ion Channel Inhibitor Library Clinical Compound Library

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Piromelatine TRPC6-PAM-C20 Linoleoyl Ethanolamide Methyl syringate cim0216 AS1269574 AMG2850 SB 452533

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Keywords

PF-05105679 1398583-31-7 Membrane transporter/Ion channel TRP/TRPV Channel Inhibitor TRPM8 subfamily cold-related orally clinical menthol TRP Channel pain Transient receptor potential channels PF 05105679 inhibit cold CMR1 PF05105679 melastatin inhibitor

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