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. |
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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 (%) | | 33 | 10 | 3.4 | | 421 | 4203 | 3.8 | 51 |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 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 | 1 mM | 2.3672 mL | 11.8360 mL | 23.6720 mL | | 5 mM | 0.4734 mL | 2.3672 mL | 4.7344 mL | | 10 mM | 0.2367 mL | 1.1836 mL | 2.3672 mL |
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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
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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。 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。 *以上所有助溶剂都可在本网站选购。
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