PF-06747711
Based on 1 Customer Validation
PF-06747711 is a potent, selective, and orally active retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) inverse agonist, with an IC50 of 4.1 nM. Anti-skin inflammatory activity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.83%
- CAS. Nr.: 1892576-58-7
- Formel: C26H26F3N5O2
- Molecular Weight:497.51
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Immunology/Inflammation Compound Library
HY-L007
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Metabolism/Protease Compound Library
HY-L012
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Small Molecule Immuno-Oncology Compound Library
HY-L031
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Orally Active Compound Library
HY-L061
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Transcription Factor-Targeted Library
HY-L090
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Nuclear Receptor Compound Library
HY-L126
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HY-L138
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Highly Selective Inhibitors Library
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Bioactive Compound Library Max
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MCE Bioactive Compound Library
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Protein Kinase Compound Library
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High-Throughput Bioactive Compound Library
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Biologische Aktivität
IC50: 4.1 nM (RORC2)[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:8−10 week old female Balb/c mice[1]
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Dosage:10, 30, and 100 mg/kg
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Administration:P.O. daily over 5 days
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Result:Inhibited ear swelling, and caused a maximum inhibition of 46% at 100 mg/kg.
Chemical Information
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CAS. Nr. 1892576-58-7
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Appearance Solid
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Molecular Weight 497.51
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Formel C26H26F3N5O2
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Color White to off-white
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SMILES
O=C(NC1=CN=C(N(C)C=C2C3CCN(C(C(C)C)=O)CC3)C2=C1C(F)(F)F)C4=CC=CC(C#N)=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
DMSO : 41.67 mg/mL (83.76 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.08 mg/mL (4.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Reinheit & Dokumentation
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Data Sheet (278 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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Handling Instructions (2659 KB)
Verweise
[1]. Schnute ME, et al. Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist. J Med Chem. 2018 Sep 9. [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 |
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| DMSO | 1 mM | 2.0100 mL | 10.0500 mL | 20.1001 mL | 50.2502 mL |
| 5 mM | 0.4020 mL | 2.0100 mL | 4.0200 mL | 10.0500 mL | |
| 10 mM | 0.2010 mL | 1.0050 mL | 2.0100 mL | 5.0250 mL | |
| 15 mM | 0.1340 mL | 0.6700 mL | 1.3400 mL | 3.3500 mL | |
| 20 mM | 0.1005 mL | 0.5025 mL | 1.0050 mL | 2.5125 mL | |
| 25 mM | 0.0804 mL | 0.4020 mL | 0.8040 mL | 2.0100 mL | |
| 30 mM | 0.0670 mL | 0.3350 mL | 0.6700 mL | 1.6750 mL | |
| 40 mM | 0.0503 mL | 0.2513 mL | 0.5025 mL | 1.2563 mL | |
| 50 mM | 0.0402 mL | 0.2010 mL | 0.4020 mL | 1.0050 mL | |
| 60 mM | 0.0335 mL | 0.1675 mL | 0.3350 mL | 0.8375 mL | |
| 80 mM | 0.0251 mL | 0.1256 mL | 0.2513 mL | 0.6281 mL |
PF-06747711 Related Classifications
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