JNJ-17203212
Based on 1 publication(s) in Google Scholar
JNJ-17203212 is a selective, potent and competitive TRPV1 antagonist. JNJ-17203212 is developed for researching pain management, such as migraine.
For research use only. We do not sell to patients.
- Purity: 99.44%
- CAS No.: 821768-06-3
- Formula: C17H15F6N5O
- Molecular Weight:419.32
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) JNJ-17203212
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Biological Activity
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TRPV1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
102 nM
Compound: 10
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Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay
Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay
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[PMID: 17489570] |
| HEK293 | IC50 |
16 nM
Compound: 10
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Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay
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[PMID: 17489570] |
| HEK293 | IC50 |
16 nM
Compound: 10
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Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay
Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay
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[PMID: 17489570] |
| HEK293 | IC50 |
65 nM
Compound: 10
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Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay
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[PMID: 17489570] |
JNJ-17203212 completely blocks capsaicin-induced CGRP (the neurotransmitter calcitonin gene-related peptide) release in a dose-dependent manner[2].
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 (260-300 g)[2]
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Dosage:0.3 mg/kg
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Administration:Intravenous injection
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Result:Had a dose-dependent effect on the elevated c-fos expression that occurred after intracisternal injection of IS.
Chemical Information
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CAS No. 821768-06-3
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Appearance Solid
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Molecular Weight 419.32
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Formula C17H15F6N5O
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Color Off-white to light yellow
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SMILES
O=C(N1CCN(C2=NC=CC=C2C(F)(F)F)CC1)NC3=NC=C(C(F)(F)F)C=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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EBioMedicine
Single cell RNA-seq analysis identifies ferroptotic chondrocyte cluster and reveals TRPV1 as an anti-ferroptotic target in osteoarthritis. [Abstract]2022 Oct;84:104258. PMID: 36137413
Solvent & Solubility
DMSO : ≥ 100 mg/mL (238.48 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.75 mg/mL (6.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
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.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[1]. Xingjuan Chen, et al. Furanocoumarins are a novel class of modulators for the transient receptor potential vanilloid type 1 (TRPV1) channel.J Biol Chem. 2014 Apr 4; 289(14): 9600-9610. [Content Brief]
[2]. Jannis E Meents, et al. Two TRPV1 receptor antagonists are effective in two different experimental models of migraine. J Headache Pain. 2015; 16: 57. [Content Brief]
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 | 2.3848 mL | 11.9241 mL | 23.8481 mL | 59.6203 mL |
| 5 mM | 0.4770 mL | 2.3848 mL | 4.7696 mL | 11.9241 mL | |
| 10 mM | 0.2385 mL | 1.1924 mL | 2.3848 mL | 5.9620 mL | |
| 15 mM | 0.1590 mL | 0.7949 mL | 1.5899 mL | 3.9747 mL | |
| 20 mM | 0.1192 mL | 0.5962 mL | 1.1924 mL | 2.9810 mL | |
| 25 mM | 0.0954 mL | 0.4770 mL | 0.9539 mL | 2.3848 mL | |
| 30 mM | 0.0795 mL | 0.3975 mL | 0.7949 mL | 1.9873 mL | |
| 40 mM | 0.0596 mL | 0.2981 mL | 0.5962 mL | 1.4905 mL | |
| 50 mM | 0.0477 mL | 0.2385 mL | 0.4770 mL | 1.1924 mL | |
| 60 mM | 0.0397 mL | 0.1987 mL | 0.3975 mL | 0.9937 mL | |
| 80 mM | 0.0298 mL | 0.1491 mL | 0.2981 mL | 0.7453 mL | |
| 100 mM | 0.0238 mL | 0.1192 mL | 0.2385 mL | 0.5962 mL |
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