1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
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  3. RORγt inverse agonist 14

RORγt inverse agonist 14 (8e) 是有效的、具有口服活性的、选择性的 RORγt 的反向激动剂 (EC50 of 2.5 nM),具有抗炎活性。RORγt inverse agonist 14 (8e) 用于风湿性关节炎和牛皮癣的研究。

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RORγt inverse agonist 14 Chemical Structure

RORγt inverse agonist 14 Chemical Structure

CAS No. : 2672496-70-5

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生物活性

RORγt inverse agonist 14 (8e) is a potent, orally active and selective RORγt inverse agonist (EC50 of 2.5 nM) with anti-inflammatory activity. RORγt inverse agonist 14 is used in the study for rheumatoid arthritis and psoriasis[1].

体内研究
(In Vivo)

RORγt inverse agonist 14 (8e) exhibits t1/2 of 11 h by iv injection of 1 mg/kg. RORγt inverse agonist 14 (8e) exhibits tmax of 2 h, %F of 101 by oral administration of 4 mg/kg in mouse[1].
RORγt inverse agonist 14 (8e, 5-20 mg/kg) provides essentially the same arthritic score reduction as a murine equivalent of the marketed TNF decoy receptor etanercept[1].

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

Animal Model: Mouse model of psoriasis: acanthosis induced by IL-23[1].
Dosage: 5, 10, 20 mg/kg.
Administration: Orally twice daily.
Result: A dose-dependent reduction in ear thickening was observed.
分子量

678.61

Formula

C26H26F8N2O6S2

CAS 号
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.

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参考文献

RORγt inverse agonist 14 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
RORγt inverse agonist 14
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HY-132195
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