TAK-828F

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TAK-828F

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1854901-94-2

TAK-828F 是一种口服有效的选择性视黄酸受体相关孤儿受体 γt (RORγt) 反向激动剂 (结合IC₅₀=1.9 nM，报告基因IC₅₀=6.1nM)。TAK-828F 具有优异的 ROR 亚型选择性 (对 RORγt 的选择性比对人 RORα 和 RORβ 高 5000 多倍)。

生物活性

TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (bindingIC₅₀=1.9 nM, reporter geneIC₅₀=6.1 nM). TAK-828F shows excellent RORγt isoforms selectivity (>5000-fold selectivity against humanRORαand RORβ)^[1].

IC₅₀& Target

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

体内研究
(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 ED₈₀of 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).

分子量

509.57

Formula

C₂₈H₃₂FN₃O₅

CAS 号

1854901-94-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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