Mavatrep
(Synonyms: JNJ-39439335) 目录号 : GC14761
Mavatrep (JNJ-39439335) 是一种具有口服活性、选择性和有效的 TRPV1 拮抗剂，对 hTRPV1 通道具有高亲和力 (Ki=6.5 nM)。
Cas No.:956274-94-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Mavatrep is a potent and orally bioavailable antagonist of TRPV1 with IC50 value of 4.6 nM [1][2].
Transient receptor potential vanilloid-1 (TRPV1) is a thermosensitive and nonselective cation channel, and is a member of the TRP channel superfamily. The channel is activated by acidic pH (<6.8), thermal stimuli (>43℃), and endogenous lipidic mediators (anandamide and oxidative metabolites of linoleic acid) [1].
Mavatrep is a potent and orally bioavailable TRPV1 antagonist. In HEK293 cells that stably express human or rat TRPV1 (rTRPV1) channels, mavatrep (1 μM) inhibited capsaicin-induced Ca2+ influx with IC50 values of 4.6 nM and 21 nM. In whole-cell patch clamp electrophysiology assay, mavatrep concentration-dependently inhibited the activation of hTRPV1 channels by pH (5.0) and capsaicin (1 μM) with IC50 values of 6.8 and 23 nM, respectively. Mavatrep (0.1 μM) also inhibited 74 ± 8.1% heat-evoked currents mediated by hTRPV1 [1].
In the CFA model of inflammatory of pain, mavatrep (10 mg/kg po) significantly reversed CFA-induced thermal hypersensitivity with ED50 and ED80 values of 1.8 and 7.8 mg/kg, respectively [1].
Reference:
[1]. Parsons WH, Calvo RR, Cheung W, et al. Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep). J Med Chem, 2015, 58(9): 3859-3874.
| Cas No. | 956274-94-5 | SDF | |
| 别名 | JNJ-39439335 | ||
| 化学名 | (E)-2-(2-(2-(4-(trifluoromethyl)styryl)-1H-benzo[d]imidazol-6-yl)phenyl)propan-2-ol | ||
| Canonical SMILES | CC(C1=CC=CC=C1C2=CC(N3)=C(N=C3/C([H])=C([H])/C4=CC=C(C(F)(F)F)C=C4)C=C2)(O)C | ||
| 分子式 | C25H21F3N2O | 分子量 | 422.44 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3672 mL | 11.836 mL | 23.672 mL |
| 5 mM | 0.4734 mL | 2.3672 mL | 4.7344 mL |
| 10 mM | 0.2367 mL | 1.1836 mL | 2.3672 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。