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Cat. No.: HY-111509

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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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CAS No.: 1854901-94-2
Formule: C₂₈H₃₂FN₃O₅
Masse moléculaire:509.57

Stockage:

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

Data Sheet (273 KB)

TAK-828F Chemical Structure

CAS No.: 1854901-94-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

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

Voir tous les produits spécifiques à Isoform ROR :

Cellular Effect

Cell Line	Type	Value	Description	References
PBMC	IC₅₀	102 nM Compound: 37; TAK-828	Inhibition of IL-17 production in human PBMC Inhibition of IL-17 production in human PBMC	[PMID: 30010338]
PBMC	IC₅₀	9.5 nM Compound: 37; TAK-828	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	[PMID: 30010338]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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).

Chemical Information

CAS No. 1854901-94-2
Masse moléculaire 509.57
Formule C₂₈H₃₂FN₃O₅
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Kono M, et al. Discovery of [ cis-3-({(5 R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1 H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5 H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Reti [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Pureté et documentation
Références

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TAK-828F

Voir tous les produits spécifiques à Isoform ROR

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

TAK-828F Related Classifications

HY-111509 Related Classifications