PF-4840154
Based on 1 publication(s) in Google Scholar
PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel with EC50s of 97 and 23 nM, respectively. PF-4840154 elicits TrpA1-mediated nocifensive behaviour in mouse.
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- Pureté: 98.15%
- CAS No.: 1332708-14-1
- Formule: C26H38N6O2
- Masse moléculaire:466.62
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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
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) PF-4840154
More
Activité biologique
IC50: 97 nM (rTrpA1), 23 nM (hTrpA1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
23 nM
Compound: 16a, PF-4840154
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Agonist activity at human TRPA1 channel expressed in HEK293 cells assessed as calcium influx measured at every 1 second for 60 seconds by fluorescence analysis
Agonist activity at human TRPA1 channel expressed in HEK293 cells assessed as calcium influx measured at every 1 second for 60 seconds by fluorescence analysis
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[PMID: 21741838] |
| HEK293 | EC50 |
97 nM
Compound: 16a, PF-4840154
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Agonist activity at rat TRPA1 channel expressed in HEK293 cells assessed as calcium influx measured at every 1 second for 60 seconds by fluorescence analysis
Agonist activity at rat TRPA1 channel expressed in HEK293 cells assessed as calcium influx measured at every 1 second for 60 seconds by fluorescence analysis
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[PMID: 21741838] |
| HEK293 | IC50 |
580 nM
Compound: 16a, PF-4840154
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Inhibition of human ERG expressed in human HEK293 cells by patch-clamp electrophysiology
Inhibition of human ERG expressed in human HEK293 cells by patch-clamp electrophysiology
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[PMID: 21741838] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female CD1 mice (25-30g) (In TrpA1+/+ mice)[1]
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Dosage:30 nmol
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Administration:Intraplantar (i.pl) injection
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Result:Elicited robust licking behavior.
Chemical Information
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CAS No. 1332708-14-1
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Appearance Solid
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Masse moléculaire 466.62
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Formule C26H38N6O2
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Color White to off-white
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SMILES
O=C(C1=CN=C(N2CCN(CC3COCCC3)CC2)N=C1NCC(C)C)NCC4=CC=CC=C4
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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 (1)
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Journal Impact Factor
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Most Recent
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Acta Physiol
2021 Aug;232(4):e13659. PMID: 33819369
Solvant et solubilité
DMSO : 50 mg/mL (107.15 mM; Need ultrasonic; 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.
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 (5.36 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 (5.36 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 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.
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.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 | 2.1431 mL | 10.7154 mL | 21.4307 mL | 53.5768 mL |
| 5 mM | 0.4286 mL | 2.1431 mL | 4.2861 mL | 10.7154 mL | |
| 10 mM | 0.2143 mL | 1.0715 mL | 2.1431 mL | 5.3577 mL | |
| 15 mM | 0.1429 mL | 0.7144 mL | 1.4287 mL | 3.5718 mL | |
| 20 mM | 0.1072 mL | 0.5358 mL | 1.0715 mL | 2.6788 mL | |
| 25 mM | 0.0857 mL | 0.4286 mL | 0.8572 mL | 2.1431 mL | |
| 30 mM | 0.0714 mL | 0.3572 mL | 0.7144 mL | 1.7859 mL | |
| 40 mM | 0.0536 mL | 0.2679 mL | 0.5358 mL | 1.3394 mL | |
| 50 mM | 0.0429 mL | 0.2143 mL | 0.4286 mL | 1.0715 mL | |
| 60 mM | 0.0357 mL | 0.1786 mL | 0.3572 mL | 0.8929 mL | |
| 80 mM | 0.0268 mL | 0.1339 mL | 0.2679 mL | 0.6697 mL | |
| 100 mM | 0.0214 mL | 0.1072 mL | 0.2143 mL | 0.5358 mL |
PF-4840154 Related Classifications
HY-18779 Related Classifications
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