A-1165442
Based on 2 publication(s) in Google Scholar
A-1165442 is a potent, competitive and orally available TRPV1 antagonist with an IC50 of 9 nM for human TRPV1.
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- Pureté: 99.94%
- CAS No.: 1221443-94-2
- Formule: C22H20ClF2N3O2
- Masse moléculaire:431.86
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) A-1165442
More
Activité biologique
IC50: 9 nM (human TRPV1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
9 nM
Compound: 52, A-1165442
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Antagonist activity against human TRPV1 expressed in HEK293 cells assessed as capsaicin-induced calcium flux by FLIPR assay
Antagonist activity against human TRPV1 expressed in HEK293 cells assessed as capsaicin-induced calcium flux by FLIPR assay
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[PMID: 25100568] |
A-1165442 displays potent, competitive antagonism at recombinant human TRPV1 activated by capsaicin (IC50=9 nM) and incomplete blockade of acid-evoked response (62% block at 30 μM). A-1165442 possesses excellent selectivity (>100-fold) versus other members of the TRP family (TRPA1, TRPM8, TRPV2, TRPV3) and other receptors expressed in peripheral sensory neurons including P2X2/3, Cav2.2, Nav channels, and KCNQ2/3. A-1165442 shows minimal cross-reactivity upon evaluation (10 μM) in a broad screening panel (n=74, CEREP) of cell-surface receptors, ion channels, and enzymes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1221443-94-2
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Appearance Solid
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Masse moléculaire 431.86
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Formule C22H20ClF2N3O2
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Color White to off-white
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SMILES
O=C(NC1=CC=CC2=C1C=C(C)N=C2)N[C@H]3C4=CC=C(Cl)C=C4OC(CF)(CF)C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
Solvant et solubilité
DMSO : ≥ 100 mg/mL (231.56 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: ≥ 2.5 mg/mL (5.79 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.
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.
Protocole
Dogs: Male beagle dogs are instrumented with telemetry transmitters capable of monitoring core body temperature and then allowed to recover. Dosing is initiated at time zero, with dogs receiving a single oral dose of vehicle, compound 1 at (30 μmol/kg), or A-1165442 (100 μmol/kg); n=4−6 per group. Measurements are recorded every 5 min for the duration of the study, then averaged to 15 min and 1 h intervals. Temperature signals are transmitted as radio signals by each implanted transmitter to a receiver placed on the cage and interfaced with a desktop personal computer[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.3156 mL | 11.5778 mL | 23.1557 mL | 57.8891 mL |
| 5 mM | 0.4631 mL | 2.3156 mL | 4.6311 mL | 11.5778 mL | |
| 10 mM | 0.2316 mL | 1.1578 mL | 2.3156 mL | 5.7889 mL | |
| 15 mM | 0.1544 mL | 0.7719 mL | 1.5437 mL | 3.8593 mL | |
| 20 mM | 0.1158 mL | 0.5789 mL | 1.1578 mL | 2.8945 mL | |
| 25 mM | 0.0926 mL | 0.4631 mL | 0.9262 mL | 2.3156 mL | |
| 30 mM | 0.0772 mL | 0.3859 mL | 0.7719 mL | 1.9296 mL | |
| 40 mM | 0.0579 mL | 0.2894 mL | 0.5789 mL | 1.4472 mL | |
| 50 mM | 0.0463 mL | 0.2316 mL | 0.4631 mL | 1.1578 mL | |
| 60 mM | 0.0386 mL | 0.1930 mL | 0.3859 mL | 0.9648 mL | |
| 80 mM | 0.0289 mL | 0.1447 mL | 0.2894 mL | 0.7236 mL | |
| 100 mM | 0.0232 mL | 0.1158 mL | 0.2316 mL | 0.5789 mL |
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