TAK-828F
TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC50=1.9 nM, reporter gene IC50=6.1 nM). TAK-828F shows excellent RORγt isoforms selectivity (>5000-fold selectivity against human RORα and RORβ).
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- No. CAS: 1854901-94-2
- Fòrmula: C28H32FN3O5
- Peso molecular:509.57
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
IC50: 1.9 nM (RORγt, binding IC50), 6.1 nM (RORγt, reporter gene IC50)[1]
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Cell Line
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Type | Value | Description | References |
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| PBMC | IC50 |
102 nM
Compound: 37; TAK-828
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Inhibition of IL-17 production in human PBMC
Inhibition of IL-17 production in human PBMC
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[PMID: 30010338] |
| PBMC | IC50 |
9.5 nM
Compound: 37; TAK-828
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Decrease in Tc17 cell differentiation in CD8+ T cells from human PBMC cells cultured under the Tc17-skewing conditions measured after 6 days
Decrease in Tc17 cell differentiation in CD8+ T cells from human PBMC cells cultured under the Tc17-skewing conditions measured after 6 days
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[PMID: 30010338] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice with IL-23-induced cytokine expression model[1]
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Dosage:0.3, 1, and 3 mg/kg
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Administration:Orally administered; b.i.d.; 28 days
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Result:Showed robust and dose-dependent inhibition of IL-17A expression (ED80=0.5 mg/kg).
Chemical Information
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No. CAS 1854901-94-2
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Peso molecular 509.57
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Fòrmula C28H32FN3O5
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SMILES
CC1(C)C2=C(F)C=C(NC([C@@H]3N(C([C@@H]4C[C@H](CC(O)=O)C4)=O)CCC5=C3C=CC(OC)=N5)=O)C=C2CC1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TAK-828F Related Classifications
HY-111509 Related Classifications
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