| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| Targets |
RORγt 51 nM (IC50)
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| ln Vitro |
The liver microsome stability of RORγt Inverse Antagonist 10 is good (human CLint=0.010 mL/min/mg, mouse CLint=0.030 mL/min/mg)[1]. In a test using human whole blood, RORγt Inverse Antagonist 10 inhibits the synthesis of IL-17A in a dose-dependent manner, with an IC50 of 130 nM[1].
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| ln Vivo |
In the mouse IL-18/23-induced cytokine expression paradigm, RORγt Inverse Antagonist 10 (3-100 mg/kg; po) exhibits a strong and dose-dependent inhibitory effect on the production of IL-17A[1]. The inverse agonist RORγt 10 (1.145 mg/kg; po) has a 3.6-hour t1/2 and a high AUC of 15000 nM*h[1].
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| Animal Protocol |
Animal/Disease Models: C57/BL6 male mice, mouse IL-18/23-induced cytokine expression model[1]
Doses: 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg Route of Administration: Oral administration Experimental Results: Dramatically inhibited the IL-17A production in a dose-dependent manner. Animal/Disease Models: Mice[1] Doses: 1.145 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: Oral administration Experimental Results: AUC=15000 nM*h, t1/2=3.6 hrs (hours). |
| References |
[1]. Ryota Nakajima, et al. Discovery of [1,2,4]Triazolo[1,5- a]pyridine Derivatives as Potent and Orally Bioavailable RORγt Inverse Agonists. ACS Med Chem Lett. 2020 Feb 27;11(4):528-534.
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| Molecular Formula |
C25H26F6N6O3
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|---|---|
| Molecular Weight |
572.50
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| CAS # |
2413986-35-1
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| SMILES |
C(F)(F)(C(CC(N1[C@@H](C)C[C@@H](OC2C3=NC=NN3C=C(NC(=O)C3C=CC(C)=NC=3)C=2C)CC1)=O)C(F)(F)F)F
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 100 mg/mL (174.67 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 10 mg/mL (17.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 100.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 10 mg/mL (17.47 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 100.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 10 mg/mL (17.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7467 mL | 8.7336 mL | 17.4672 mL | |
| 5 mM | 0.3493 mL | 1.7467 mL | 3.4934 mL | |
| 10 mM | 0.1747 mL | 0.8734 mL | 1.7467 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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