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A-9758
Catalog No. T10210Cas No. 2055271-22-0
A-9758 is a RORγ ligand and selective RORγt inverse agonist (IC50: 5 nM) that effectively suppresses IL-17A release, Th17 differentiation, and Th17 effector function, significantly attenuating IL-23 driven psoriasiform dermatitis.
A-9758
Catalog No. T10210Cas No. 2055271-22-0
A-9758 is a RORγ ligand and selective RORγt inverse agonist (IC50: 5 nM) that effectively suppresses IL-17A release, Th17 differentiation, and Th17 effector function, significantly attenuating IL-23 driven psoriasiform dermatitis.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $2,570 | 10-14 weeks | |
| 50 mg | $3,380 | 10-14 weeks | |
| 100 mg | $4,600 | 10-14 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| Description | A-9758 is a RORγ ligand and selective RORγt inverse agonist (IC50: 5 nM) that effectively suppresses IL-17A release, Th17 differentiation, and Th17 effector function, significantly attenuating IL-23 driven psoriasiform dermatitis. |
| Targets&IC50 | RORβ:1370 nM , RORγt:5 nM , RORα:73 nM |
| In vitro | A-9758 inhibits RORγ transactivation in humans, mice, dogs, and rats (IC50s: 38 nM, 20 nM, 25 nM, and 64 nM, respectively). It exhibits a cofactor profile by recruiting co-repressors [NCoR1: EC50 = 60 nM, NCoR2: EC50 = 43 nM] and derecruiting co-activators [NCoA1: IC50 = 110 nM, PGC1α: IC50 = 49 nM]. A-9758 inhibits TCR-mediated IL-17A secretion with IC50s of 100 nM and 38 nM for human CD4+ T cells and in vitro differentiated mouse Th17 cells, respectively, and attenuates the differentiation and/or effector function of RORγt-expressing Th17 cells. |
| Molecular Weight | 527.36 |
| Formula | C25H23Cl2F3N2O3 |
| Cas No. | 2055271-22-0 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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