Mavatrep

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种选择性高亲和力 TRPV1 拮抗剂，IC50 为 4.6 nM（抑制辣椒素诱导的 Ca(2+) 内流）。

A selective, high-affinity TRPV1 antagonist with IC50 of 4.6 nM (inhibition of capsaicin-induced Ca(2+) influx); exhibits potent in vitro functional activity and robust oral efficacy in multiple models of inflammatory pain.Pain Phase 1 Clinical.

Mavatrep (series of decreasing concentrations from 1 μM; 25 min) inhibits capsaicin-induced Ca2+ influx in HEK293 cells expressing TRPV1 channels.:Cell Viability Assay Cell Line:HEK293 cells (stably expressing TRPV1 channels) Concentration:Series of decreasing concentrations from 1 μM Incubation Time:25 min Result:Inhibited capsaicin-induced Ca2+ influx with an IC50 value of 4.6 nM.

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.

JNJ-39439335

Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRP/TRPV Channel

Neurological Disease

Pain

956274-94-5

422.4423

C25H21F3N2O

>98% (HPLC)

DMSO: ≥ 28 mg/mL

OC(C)(C)C1=CC=CC=C1C2=CC=C3N=C(/C=C/C4=CC=C(C(F)(F)F)C=C4)NC3=C2

Benzenemethanol, α,α-dimethyl-2-[2-[(1E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-1H-benzimidazol-6-yl]-

(-20℃)

With Ice Pack

≥ 2 years