RORγt Inverse agonist 10

COA

级别和纯度:

≥99%

CAS编号: 2413986-35-1
分子式: C₂₅H₂₆F₆N₆O₃
分子量: 572.50

有货

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货号 (SKU)	包装规格	是否现货
R648118-1mg	1mg	期货
R648118-5mg	5mg	期货
R648118-10mg	10mg	期货

查看相关系列

Metabolic Enzyme/Protease (4889) ROR (47) Vitamin D Related/Nuclear Receptor (908) 脂质代谢 (4331)

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基本描述

别名	RORγt 反向激动剂 10
规格或纯度	≥99%
英文名称	RORγt Inverse agonist 10
生化机理	RORγt 反激动剂 10 是一种强效的口服生物活性 RORγt（视黄酸受体相关孤儿核受体γt）反激动剂，IC 50 为 51 nM。RORγt 是牛皮癣发病相关基因的主要转录因子。
储存温度	2-8°C储存,避光,干燥
运输条件	冰袋运输
产品介绍	RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC 50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A , IL-22 , and IL-23R In Vitro RORγt Inverse agonist 10 has a good liver microsome stability (human CL int =0.010 mL/min/mg, mouse CL int =0.030 mL/min/mg). RORγt Inverse agonist 10 suppresses the IL-17A production in a dose-dependent manner with an IC 50 of 130 nM in a human whole-blood assay. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo RORγt Inverse agonist 10 (3-100 mg/kg; p.o.) shows robust and dose-dependent inhibitory effect on the IL-17A production in mouse IL-18/23-induced cytokine expression model . RORγt Inverse agonist 10 (1.145 mg/kg; p.o.) shows a high AUC of 15000 nMh and t 1/2 of 3.6 hours . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57/BL6 male mice, mouse IL-18/23-induced cytokine expression model Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg Administration: Oral administration Result: Significantly inhibited the IL-17A production in a dose-dependent manner. Animal Model: Mice Dosage: 1.145 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration Result: AUC=15000 nMh, t 1/2 =3.6 hours. Form:Solid IC50& Target:RORγt 51 nM (IC 50 )
纯度	≥99%

名称和识别符

Smiles	C[C@H](N(C(CC(C(F)(F)F)C(F)(F)F)=O)CC1)C[C@H]1OC2=C(C)C(NC(C3=CN=C(C)C=C3)=O)=CN4C2=NC=N4
分子量	572.50

化学和物理性质

溶解性	DMSO : ≥ 100 mg/mL (174.67 mM)

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