Mavatrep JNJ-39439335|cas:956274-94-5|西域试剂

Mavatrep JNJ-39439335,99.60%

产品编号：Bellancom-16935| CAS NO：956274-94-5| 分子式：C₂₅H₂₁F₃N₂O| 分子量：422.44

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-16935	￥2500.00	杭州北京（现货）
Bellancom-16935	￥4000.00	杭州北京（现货）
Bellancom-16935	￥8500.00	杭州北京（现货）
Bellancom-16935	￥13600.00	杭州北京（现货）
Bellancom-16935	￥22000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Mavatrep 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 (K_i=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 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.

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.

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

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.

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

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

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:

1.19 Pharmacokinetic Parameters of Mavatrep in male Sprague-Dawley rats.

IV (2 mg/kg)			PO (10 mg/kg)
CL (mL/min/kg)	V_ss (L/kg)	T_1/2 (h)		C_max (ng/mL)	AUC_max (ng•h/mL)	T_1/2 (h)	F (%)
33	10	3.4		421	4203	3.8	51

体内研究

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

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:

1.19 Pharmacokinetic Parameters of Mavatrep in male Sprague-Dawley rats.

IV (2 mg/kg)			PO (10 mg/kg)
CL (mL/min/kg)	V_ss (L/kg)	T_1/2 (h)		C_max (ng/mL)	AUC_max (ng•h/mL)	T_1/2 (h)	F (%)
33	10	3.4		421	4203	3.8	51

体内研究

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

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:

1.19 Pharmacokinetic Parameters of Mavatrep in male Sprague-Dawley rats.

IV (2 mg/kg)			PO (10 mg/kg)
CL (mL/min/kg)	V_ss (L/kg)	T_1/2 (h)		C_max (ng/mL)	AUC_max (ng•h/mL)	T_1/2 (h)	F (%)
33	10	3.4		421	4203	3.8	51

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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-CD in 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 μL 20% 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