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TAK-828F 

Cat. No.: HY-111509
Handling Instructions

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).

For research use only. We do not sell to patients.

TAK-828F Chemical Structure

TAK-828F Chemical Structure

CAS No. : 1854901-94-2

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Description

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)[1].

IC50 & Target

IC50: 1.9 nM (RORγt, binding IC50), 6.1 nM (RORγt, reporter gene IC50)[1]

In Vivo

TAK-828F (0.3, 1, and 3 mg/kg; orally administered; b.i.d.; 28 days; in mice with IL-23-induced cytokine expression model) shows robust and dose-dependent inhibition of IL-17A expression with an ED80 of 0.5 mg/kg[1].

Animal Model: Mice with IL-23-induced cytokine expression model[1]
Dosage: 0.3, 1, and 3 mg/kg
Administration: Orally administered; b.i.d.; 28 days
Result: Showed robust and dose-dependent inhibition of IL-17A expression (ED80=0.5 mg/kg).
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

509.57

Formula

C₂₈H₃₂FN₃O₅

CAS No.

1854901-94-2

SMILES

CC1(C)C2=C(F)C=C(NC([[email protected]@H]3N(C([[email protected]@H]4C[[email protected]](CC(O)=O)C4)=O)CCC5=C3C=CC(OC)=N5)=O)C=C2CC1

Shipping

Room temperature in continental US; may vary elsewhere

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TAK-828F
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HY-111509
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Cat. No.: HY-111509