计算溶液所需的质量、体积或浓度。
概述
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 nM*h 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 nM*h, t 1/2 =3.6 hours.
Form:Solid
IC50& Target:RORγt 51 nM (IC 50 )
规格
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。
储存条件
2-8°C储存,避光,干燥
运输条件
低温运输
纯度
≥99%
名称和识别符
分子类型
小分子
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
高级数据
化学和物理性质
溶解性
DMSO : ≥ 100 mg/mL (174.67 mM)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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