RORγt Inverse agonist 10
Based on 1 Customer Validation
RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R
For research use only. We do not sell to patients.
- Purity: 99.13%
- CAS No.: 2413986-35-1
- Formula: C25H26F6N6O3
- Molecular Weight:572.50
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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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Biological Activity
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RORγt 51 nM (IC50) |
RORγt Inverse agonist 10 has a good liver microsome stability (human CLint=0.010 mL/min/mg, mouse CLint=0.030 mL/min/mg)[1].
RORγt Inverse agonist 10 suppresses the IL-17A production in a dose-dependent manner with an IC50 of 130 nM in a human whole-blood assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
RORγt Inverse agonist 10 (1.145 mg/kg; p.o.) shows a high AUC of 15000 nM*h and t1/2 of 3.6 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57/BL6 male mice, mouse IL-18/23-induced cytokine expression model[1]
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Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
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Administration:Oral administration
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Result:Significantly inhibited the IL-17A production in a dose-dependent manner.
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Animal Model:Mice[1]
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Dosage:1.145 mg/kg (Pharmacokinetic Analysis)
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Administration:Oral administration
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Result:AUC=15000 nM*h, t1/2=3.6 hours.
Chemical Information
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CAS No. 2413986-35-1
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Appearance Solid
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Molecular Weight 572.50
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Formula C25H26F6N6O3
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Color Off-white to light yellow
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SMILES
C[C@H](N(C(CC(C(F)(F)F)C(F)(F)F)=O)CC1)C[C@H]1OC2=C(C)C(NC(C3=CN=C(C)C=C3)=O)=CN4C2=NC=N4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : ≥ 100 mg/mL (174.67 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 10 mg/mL (17.47 mM); Clear solution
This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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: ≥ 10 mg/mL (17.47 mM); Clear solution
This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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 (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7467 mL | 8.7336 mL | 17.4672 mL | 43.6681 mL |
| 5 mM | 0.3493 mL | 1.7467 mL | 3.4934 mL | 8.7336 mL | |
| 10 mM | 0.1747 mL | 0.8734 mL | 1.7467 mL | 4.3668 mL | |
| 15 mM | 0.1164 mL | 0.5822 mL | 1.1645 mL | 2.9112 mL | |
| 20 mM | 0.0873 mL | 0.4367 mL | 0.8734 mL | 2.1834 mL | |
| 25 mM | 0.0699 mL | 0.3493 mL | 0.6987 mL | 1.7467 mL | |
| 30 mM | 0.0582 mL | 0.2911 mL | 0.5822 mL | 1.4556 mL | |
| 40 mM | 0.0437 mL | 0.2183 mL | 0.4367 mL | 1.0917 mL | |
| 50 mM | 0.0349 mL | 0.1747 mL | 0.3493 mL | 0.8734 mL | |
| 60 mM | 0.0291 mL | 0.1456 mL | 0.2911 mL | 0.7278 mL | |
| 80 mM | 0.0218 mL | 0.1092 mL | 0.2183 mL | 0.5459 mL | |
| 100 mM | 0.0175 mL | 0.0873 mL | 0.1747 mL | 0.4367 mL |
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