计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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 Ca 2+ influx with an IC 50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain.
In Vitro
Mavatrep (series of decreasing concentrations from 1 μM; 25 min) inhibits capsaicin-induced Ca 2+ influx in HEK293 cells expressing TRPV1 channels. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: HEK293 cells (stably expressing TRPV1 channels) Concentration: Series of decreasing concentrations from 1 μM Incubation Time: 25 min Result: Inhibited capsaicin-induced Ca 2+ influx with an IC 50 value of 4.6 nM.
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%) . MCE 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 ED 50 and ED 80 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 ED 50 and ED 80 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
规格
别名
马瓦特雷普
规格或纯度
10mM in DMSO
英文名称
Mavatrep
生化机理
Mavatrep（JNJ-39439335）是一种口服活性、选择性和强效的 TRPV1 拮抗剂，对 hTRPV1 通道具有高亲和力（K i =6.5 nM）。Mavatrep 可拮抗辣椒素诱导的 Ca 2+ 流入，IC 50 值为 4.6 nM。在某些研究中，Mavatrep 可用于拮抗辣椒素诱导的 Ca 2+ 流入。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
拮抗剂
作用机制
类香草素受体拮抗剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC(C)(C1=CC=CC=C1C2=CC3=C(C=C2)N=C(N3)/C=C/C4=CC=C(C=C4)C(F)(F)F)O
关联CAS
PubChem CID
MeSH Entry Terms
2-(2-(2-(2-(4-trifluoromethylphenyl)vinyl)-1H-benzimidazol-5-yl)phenyl)propan-2-ol;mavatrep
分子量
422.44
技术文档
高级数据
产品属性
| ALogP | 6 |
|---|
关联靶点（人）
TRPV1
Tclin
瞬时受体电位阳离子通道亚家族V成员1(Transient receptor potential cation channel subfamily V member 1)
(4 活性数据)
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 956274-94-5，分子式为 C25H21F3N2O，分子量为 422.44 g/mol。
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