产品
编 号：F538577
分子式：C25H21F3N2O
分子量：422.44
分子式：C25H21F3N2O
分子量：422.44
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 956274-94-5
产品详情
生物活性：
Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain.
体内研究：
Mavatrep (1, 3, 10, 30 mg/kg; p.o.; single) shows complete reversal of thermal hypersensitivity both in CFA model of inflammatory of pain and (0.1, 0.3, 1, 3, 10 mg/kg) carrageenan model of inflammatory pain.Mavatrep (10 mg/kg; p.o.; single) exhibits substantial bioavailability in the rat (51%).Animal Model:Male Sprague-Dawley rats (195-350 g; CFA model of inflammatory of pain).
Dosage:10 mg/kg
Administration:Oral administration, single.
Result:Significantly reversed CFA-induced thermal hypersensitivity, beginning 30 min after administration and lasting for at least 3 h.
Animal Model:Male Sprague-Dawley rats (195-350 g; CFA model of inflammatory of pain).
Dosage:1, 3, 10, 30 mg/kg
Administration:Oral administration, single.
Result:Exhibited complete reversal of thermal hypersensitivity, with ED50 and ED80 values of 1.8 and 7.8 mg/kg, and the corresponding plasma levels were 41.9 and 270.8 ng/mL, respectively.
Animal Model:Male Sprague-Dawley rats (195-350 g; carrageenan model of inflammatory pain).
Dosage:0.1, 0.3, 1, 3, 10 mg/kg
Administration:Oral administration, single.
Result:Completely reversed carrageenan-induced thermal hypersensitivity, with ED50 and ED80 values of 0.18 and 0.48 mg/kg, and the corresponding plasma levels were 3.8 and 9.2 ng/mL, respectively.
Animal Model:Male Sprague-Dawley rats (195-350 g).
Dosage:2 mg/kg (for i.v.); 10 mg/kg (for p.o.). (Dissolved in 20% HPβCD)
Administration:Oral administration, single.
Result:1.19Pharmacokinetic Parameters of Mavatrep in male Sprague-Dawley rats.IV (2 mg/kg)PO (10 mg/kg)
CL (mL/min/kg)Vss (L/kg)T1/2 (h)Cmax (ng/mL)AUCmax (ng?h/mL)T1/2 (h)F (%)
33103.442142033.851
体外研究：
Mavatrep (series of decreasing concentrations from 1 μM; 25 min) inhibits capsaicin-induced Ca2+ influx in HEK293 cells expressing TRPV1 channels.
Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain.
体内研究：
Mavatrep (1, 3, 10, 30 mg/kg; p.o.; single) shows complete reversal of thermal hypersensitivity both in CFA model of inflammatory of pain and (0.1, 0.3, 1, 3, 10 mg/kg) carrageenan model of inflammatory pain.Mavatrep (10 mg/kg; p.o.; single) exhibits substantial bioavailability in the rat (51%).Animal Model:Male Sprague-Dawley rats (195-350 g; CFA model of inflammatory of pain).
Dosage:10 mg/kg
Administration:Oral administration, single.
Result:Significantly reversed CFA-induced thermal hypersensitivity, beginning 30 min after administration and lasting for at least 3 h.
Animal Model:Male Sprague-Dawley rats (195-350 g; CFA model of inflammatory of pain).
Dosage:1, 3, 10, 30 mg/kg
Administration:Oral administration, single.
Result:Exhibited complete reversal of thermal hypersensitivity, with ED50 and ED80 values of 1.8 and 7.8 mg/kg, and the corresponding plasma levels were 41.9 and 270.8 ng/mL, respectively.
Animal Model:Male Sprague-Dawley rats (195-350 g; carrageenan model of inflammatory pain).
Dosage:0.1, 0.3, 1, 3, 10 mg/kg
Administration:Oral administration, single.
Result:Completely reversed carrageenan-induced thermal hypersensitivity, with ED50 and ED80 values of 0.18 and 0.48 mg/kg, and the corresponding plasma levels were 3.8 and 9.2 ng/mL, respectively.
Animal Model:Male Sprague-Dawley rats (195-350 g).
Dosage:2 mg/kg (for i.v.); 10 mg/kg (for p.o.). (Dissolved in 20% HPβCD)
Administration:Oral administration, single.
Result:1.19Pharmacokinetic Parameters of Mavatrep in male Sprague-Dawley rats.IV (2 mg/kg)PO (10 mg/kg)
CL (mL/min/kg)Vss (L/kg)T1/2 (h)Cmax (ng/mL)AUCmax (ng?h/mL)T1/2 (h)F (%)
33103.442142033.851
体外研究：
Mavatrep (series of decreasing concentrations from 1 μM; 25 min) inhibits capsaicin-induced Ca2+ influx in HEK293 cells expressing TRPV1 channels.
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