2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. ROR
  4. RORγt inverse agonist 29

RORγt inverse agonist 29 是一种有效的、具有口服活性的 RORγt 选择性反向激动剂 (IC50: 21 nM)。RORγt inverse agonist 29 可用于皮肤炎症和银屑病等自身免疫性疾病的研究。

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RORγt inverse agonist 29 Chemical Structure

RORγt inverse agonist 29 Chemical Structure

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RORγt inverse agonist 29 相关抗体

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  • 生物活性

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  • 参考文献

生物活性

RORγt inverse agonist 29 is a potent, orally active and selective RORγt inverse agonist (IC50: 21 nM). RORγt inverse agonist 29 can be used in the research of skin inflammation and autoimmune diseases like psoriasis[1].

IC50 & Target[1]

RORγt

21 nM (IC50)

体外研究
(In Vitro)

RORγt inverse agonist 29 (compound b12) demonstrates high RORγt transcriptional inhibitory activity (IC50: 28 nM) in human Jurkat cells[1].
RORγt inverse agonist 29 (10 μM) shows good metabolic stabilities in in vitro human liver microsomes, with comparable half-life (T1/2: 4.46 h) and HLM (CLint(liver): 4.8 mL/min/kg)[1].

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

RORγt inverse agonist 29 相关抗体:
体内研究
(In Vivo)

RORγt inverse agonist 29 (p.o., 100 mg/kg) reduces the total Psoriasis Area and the development of clinical symptoms in mouse Imiquimod-induced skin inflammation model[1].
RORγt inverse agonist 29 (i.v., p.o., 0.3 or 1 mg/kg) displays an acceptable bioavailability and a half-life in rats[1].

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

Animal Model: Mouse Imiquimod-induced skin inflammation model[1]
Dosage: 15 mg/kg, 50 mg/kg, 100 mg/kg
Administration: Oral administration, twice a day for 13 days.
Result: Inhibited IL-6 and IL-17A protein in the serum, with inhibition rate of 58.06% (IL-6) and 84.07% (IL-17A) at 100 mg/kg.
Reduced the histopathological symptoms on the back skin at dose of 100 mg/kg.
Alleviated symptoms including mononuclear and inflammatory cell infiltration, skin layer thickening, and dermal telangiectasia.
Animal Model: Rats (pharmacokinetic assay)[1]
Dosage: 0.3 mg/kg (i.v.), 1 mg/kg (p.o.)
Administration: Intravenous injection, oral administration
Result: Pharmacokinetic profile of RORγt inverse agonist 29 (compound b12).
administration route T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng•h/mL) AUC0-∞ (ng•h/mL) F (%)
i.v. (0.3 mg/kg) 5.8 2.4 88 156 162
p.o. (1 mg/kg) 6.5 3.1 105 340 352 65
分子量

464.53

Formula

C25H24N2O5S
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.
纯度 & 产品资料
参考文献

RORγt inverse agonist 29 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.

Keywords:

RORγt inverse agonist 29RORγt inverse agonist29RORγt inverse agonist-29RORRAR-related orphan receptorInverse agonistautoimmuneinflammationTh17 cellpsoriasisskin inflammationInhibitorinhibitorinhibit

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