PF-05105679CAS号： 1398583-31-7分子式： C26H21FN2O3分子量： 428.45描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
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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| 纯度 |
98%
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| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 可溶性/溶解性 |
DMSO:120 mg/mL (280.08 mM)
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| 生物活性 | |
| 靶点 |
TRPM8:103 nM
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| In vitro(体外研究) |
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].
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| In vivo(体内研究) |
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].
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