产品
编 号：F150607
分子式：C26H21FN2O3
分子量：428.45
分子式：C26H21FN2O3
分子量：428.45
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1398583-31-7
产品详情
生物活性：
PF-05105679 is an orally active and selective TRPM8 antagonist with an IC50 of 103 nM. PF-05105679 has the potential for cold-related pain.
体内研究：
PF-05105679 (0.2 mg/kg for iv and 20mg/kg for oral gavage) has a T1/2 of 3.9 hours, a CL of 31 mL/min/kg, and a Vss of 7.4 L/kg for dogs. PF-05105679 (2, 20 mg/kg) has 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. Animal Model:Male beagle dogs (weight 10 to 15kg)
Dosage:0.2 mg/kg (iv) or 20 mg/kg (oral gavage)(Pharmacokinetic Analysis)
Administration:Iv or oral gavage
Result:Had a T1/2 of 3.9 hours, a CL of 31 mL/min/kg, and a Vss of 7.4 L/kg for dogs.
体外研究：
PF-05105679 demonstrates >100-fold selectivity across a range of different receptors, ion channels, and enzymes including the closely related TRPV1 and TRPA1 channels. TRPM8, also known as the cold and menthol receptor 1 (CMR1), is a member of the melastatin subfamily.
PF-05105679 is an orally active and selective TRPM8 antagonist with an IC50 of 103 nM. PF-05105679 has the potential for cold-related pain.
体内研究：
PF-05105679 (0.2 mg/kg for iv and 20mg/kg for oral gavage) has a T1/2 of 3.9 hours, a CL of 31 mL/min/kg, and a Vss of 7.4 L/kg for dogs. PF-05105679 (2, 20 mg/kg) has 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. Animal Model:Male beagle dogs (weight 10 to 15kg)
Dosage:0.2 mg/kg (iv) or 20 mg/kg (oral gavage)(Pharmacokinetic Analysis)
Administration:Iv or oral gavage
Result:Had a T1/2 of 3.9 hours, a CL of 31 mL/min/kg, and a Vss of 7.4 L/kg for dogs.
体外研究：
PF-05105679 demonstrates >100-fold selectivity across a range of different receptors, ion channels, and enzymes including the closely related TRPV1 and TRPA1 channels. TRPM8, also known as the cold and menthol receptor 1 (CMR1), is a member of the melastatin subfamily.
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