A-9758 |
| رقم الكتالوجGC35214 |
A-9758 عبارة عن يجند RORγ وناهض عكسي انتقائي RORγt (IC50 = 5 نانومتر) ، ويظهر فاعلية قوية ضد إطلاق IL-17A
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2055271-22-0
Sample solution is provided at 25 µL, 10mM.
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A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation[1]. IC50: 5 nM (RORγt), 73 nM (RORα), 1370 nM (RORβ)[1]
A-9758 inhibits human, mouse, dog and rat RORγ transactivation (IC50=38 nM, 20 nM, 25 nM and 64 nM, respectively)[1].A-9758 displays a cofactor profile in recruiting co-repressors (NCoR1: EC50=60 nM, NCoR2: EC50=43 nM) and derecruiting co-activators (NCoA1: IC50=110 nM, PGC1α: IC50=49 nM)[1].A-9758 inhibits TCR-mediated IL-17A secretion with an IC50 of 100 and 38 nM for human CD4+ T cells and in vitro differentiated mouse Th17 cells, respectively. A-9758 attenuates the differentiation of RORγt expressing Th17 cells and/or their effector function[1].
[1]. Gauld S, et al. Inhibition of IL-23 mediated inflammation with a novel small molecule inverse agonist of RORgt. J Pharmacol Exp Ther. 2019 Aug 2. pii: jpet.119.258046.
| Cas No. | 2055271-22-0 | SDF | |
| Canonical SMILES | O=C(C1CCN(C(C2=CC=C(Cl)C(CC(N3C)=CC4=C3C=C(C(F)(F)F)C=C4C)=C2Cl)=O)CC1)O | ||
| Formula | C25H23Cl2F3N2O3 | M.Wt | 527.36 |
| الذوبان | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8962 mL | 9.4812 mL | 18.9624 mL |
| 5 mM | 0.3792 mL | 1.8962 mL | 3.7925 mL |
| 10 mM | 0.1896 mL | 0.9481 mL | 1.8962 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)
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