Mavatrep
Based on 1 Customer Validation
Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.67%
- CAS 番号: 956274-94-5
- 分子式: C25H21F3N2O
- 分子量:422.44
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Mavatrep (Standard)TRPV1 Antagonist
生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
21 nM
Compound: 4, Mavatrep
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Antagonist activity at recombinant rat TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx preincubated for 5 mins followed by capsaicin challenge
Antagonist activity at recombinant rat TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx preincubated for 5 mins followed by capsaicin challenge
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[PMID: 25850459] |
| HEK293 | IC50 |
23 nM
Compound: 4, Mavatrep
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Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced current measured for 150 secs by patch clamp assay
Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced current measured for 150 secs by patch clamp assay
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[PMID: 25850459] |
| HEK293 | IC50 |
4.6 nM
Compound: 4, Mavatrep
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Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx preincubated for 5 mins followed by capsaicin challenge
Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx preincubated for 5 mins followed by capsaicin challenge
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[PMID: 25850459] |
| HEK293 | IC50 |
6.8 nM
Compound: 4, Mavatrep
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Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of pH 5-induced current measured for 150 secs by patch clamp assay
Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of pH 5-induced current measured for 150 secs by patch clamp assay
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[PMID: 25850459] |
体外実験
Mavatrep (series of decreasing concentrations from 1 μM; 25 min) inhibits capsaicin-induced Ca2+ influx in HEK293 cells expressing TRPV1 channels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells (stably expressing TRPV1 channels)
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Concentration:Series of decreasing concentrations from 1 μM
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Incubation Time:25 min
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Result:Inhibited capsaicin-induced Ca2+ influx with an IC50 value of 4.6 nM.
体内実験
Mavatrep (10 mg/kg; p.o.; single) exhibits substantial bioavailability in the rat (51%)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (195-350 g; CFA model of inflammatory of pain)[1].
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Dosage:10 mg/kg
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Administration:Oral administration, single.
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Result:Significantly reversed CFA-induced thermal hypersensitivity, beginning 30 min after administration and lasting for at least 3 h.
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Animal Model:Male Sprague-Dawley rats (195-350 g; CFA model of inflammatory of pain)[1].
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Dosage:1, 3, 10, 30 mg/kg
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Administration:Oral administration, single.
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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.
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Animal Model:Male Sprague-Dawley rats (195-350 g; carrageenan model of inflammatory pain)[1].
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Dosage:0.1, 0.3, 1, 3, 10 mg/kg
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Administration:Oral administration, single.
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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.
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Animal Model:Male Sprague-Dawley rats (195-350 g)[1].
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Dosage:2 mg/kg (for i.v.); 10 mg/kg (for p.o.). (Dissolved in 20% HPβCD)
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Administration:Oral administration, single.
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Result:
1.19 Pharmacokinetic 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 (ng•h/mL) T1/2 (h) F (%) 33 10 3.4 421 4203 3.8 51
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
化学情報
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CAS 番号 956274-94-5
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性状 Solid
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分子量 422.44
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分子式 C25H21F3N2O
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Color White to off-white
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SMILES
OC(C)(C)C1=CC=CC=C1C2=CC=C3N=C(/C=C/C4=CC=C(C(F)(F)F)C=C4)NC3=C2
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別名
JNJ-39439335
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
溶剤 & 溶解度
体外:
DMSO : 16.67 mg/mL (39.46 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.92 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.92 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (276 KB)
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SDS (252 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3672 mL | 11.8360 mL | 23.6720 mL | 59.1800 mL |
| 5 mM | 0.4734 mL | 2.3672 mL | 4.7344 mL | 11.8360 mL | |
| 10 mM | 0.2367 mL | 1.1836 mL | 2.3672 mL | 5.9180 mL | |
| 15 mM | 0.1578 mL | 0.7891 mL | 1.5781 mL | 3.9453 mL | |
| 20 mM | 0.1184 mL | 0.5918 mL | 1.1836 mL | 2.9590 mL | |
| 25 mM | 0.0947 mL | 0.4734 mL | 0.9469 mL | 2.3672 mL | |
| 30 mM | 0.0789 mL | 0.3945 mL | 0.7891 mL | 1.9727 mL |
Mavatrep 関連分類
HY-16935 関連分類
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