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mavatrep
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
mavatrep图片
CAS NO:956274-94-5
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
JNJ-39439335
产品介绍
Mavatrep (JNJ-39439335) 是一种口服有效的、具有选择性的强效TRPV1拮抗剂,对hTRPV1通道具有高亲和力 (Ki=6.5 nM)。Mavatrep 能拮抗辣椒素诱导的 Ca2+流入,其IC50值为4.6 nM。Mavatrep 可用于某些神经病理性疼痛的研究。
生物活性

Mavatrep (JNJ-39439335) is an orally active, selective and potentTRPV1antagonist with high affinity forhTRPV1channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca2+influx with anIC50value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain[1].

体外研究
(In Vitro)

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

Cell Viability Assay[1]

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 IC50value of 4.6 nM.
体内研究
(In Vivo)

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].

Animal Model:Male Sprague-Dawley rats (195-350 g; CFA model of inflammatory of pain)[1].
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)[1].
Dosage:1, 3, 10, 30 mg/kg
Administration:Oral administration, single.
Result:Exhibited complete reversal of thermal hypersensitivity, with ED50and ED80values 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)[1].
Dosage:0.1, 0.3, 1, 3, 10 mg/kg
Administration:Oral administration, single.
Result:Completely reversed carrageenan-induced thermal hypersensitivity, with ED50and ED80values 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)[1].
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[1].
IV (2 mg/kg)PO (10 mg/kg)
CL (mL/min/kg)Vss(L/kg)T1/2(h)Cmax(ng/mL)AUCmax(ngoh/mL)T1/2(h)F (%)
33103.442142033.851
Clinical Trial
分子量

422.44

性状

Solid

Formula

C25H21F3N2O

CAS 号

956274-94-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

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

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3672 mL11.8360 mL23.6720 mL
5 mM0.4734 mL2.3672 mL4.7344 mL
10 mM0.2367 mL1.1836 mL2.3672 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 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

    此方案可获得 ≥ 2.5 mg/mL (5.92 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

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

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

    此方案可获得 2.5 mg/mL (5.92 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。