PF-05105679 是一种特异性 TRPM8 拮抗剂 (IC50 = 103 nM)。 PF-05105679 可用于冷相关疼痛的研究。
产品描述
PF-05105679 is a selective TRPM8 antagonist (IC50 = 103 nM). PF-05105679 can be used in research on cold-related pain.
体外活性
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].
体内活性
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].
Cas No.
1398583-31-7
分子式
C26H21FN2O3
分子量
428.45
储存和溶解度
DMSO:120 mg/mL (280.08 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
