Mavatrep是一种口服有效的、具有选择性的强效 TRPV

Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (K_i=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^[1].

Mavatrep (series of decreasing concentrations from 1 μM; 25 min) inhibits capsaicin-induced Ca²⁺ influx in HEK293 cells expressing TRPV1 channels^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

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^[1].
Mavatrep (10 mg/kg; p.o.; single) exhibits substantial bioavailability in the rat (51%)^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

422.44

Solid

C₂₅H₂₁F₃N₂O

956274-94-5

Room temperature in continental US; may vary elsewhere.

DMSO : 16.67 mg/mL (39.46 mM; ultrasonic and warming and heat to 60°C)

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• 1.

  请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

  Solubility: ≥ 2.5 mg/mL (5.92 mM); Clear solution

• 2.

  请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

  Solubility: 2.5 mg/mL (5.92 mM); Suspended solution; Need ultrasonic