RORγt inverse agonist 30

• 常用名: RORγt inverse agonist 30
• 英文名: RORγt inverse agonist 30
• CAS号: 1445901-41-6
• 分子量: 441.59
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₄H₃₁N₃O₃S
• 熔点: N/A
• 闪点: N/A

RORγt inverse agonist 30用途

RORγt反向激动剂30(化合物1)是一种有效的RORγt反向激动剂,IC50为46 nM。靶向核受体RORγt对自身免疫性疾病有效[1]。

RORγt inverse agonist 30名称

• 英文名: RORγt inverse agonist 30

RORγt inverse agonist 30生物活性

• 描述: RORγt反向激动剂30(化合物1)是一种有效的RORγt反向激动剂,IC50为46 nM。靶向核受体RORγt对自身免疫性疾病有效[1]。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> ROR
  研究领域 >> 炎症/免疫
• 靶点实验:

  RORγt:46 nM (IC50)

• 体外研究: RORγt反向激动剂30(化合物1)抑制小鼠Th17细胞分化,IC50为0.67μM[1]。
• 体内研究: RORγt反向激动剂30具有良好的药代动力学特征,T1/2为2.3分钟,CLint为612μL/min/mg,CLint(肝脏)为2423.5 mL/min/kg[1]。
• 参考文献:

  [1]. Nannan Sun, et al. Discovery of novel N-sulfonamide-tetrahydroquinolines as potent retinoic acid receptor-related orphan receptor γt inverse agonists for the treatment of autoimmune diseases. Eur J Med Chem. 2020 Feb 1;187:111984.

RORγt inverse agonist 30物理化学性质

• 分子式: C₂₄H₃₁N₃O₃S
• 分子量: 441.59
• InChIKey: KIHDXHLXSMPQSN-UHFFFAOYSA-N
• SMILES: CC(=O)N1CCN(c2ccc(CN(C3CCC3)S(=O)(=O)Cc3ccccc3)cc2)CC1

RORγt inverse agonist 30靶点实验

查看更多实验

实验名称：Selectivity ratio of EC50 for GAL4-fused human PXR expressed in HEK293T cells to EC50... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3367630

实验名称：Intrinsic clearance in CD-1 mouse liver at 1 uM measured up to 60 mins in presence of... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4707868

实验名称：Selectivity ratio of EC50 for GAL4-fused human LXRalpha expressed in HEK293T cells to... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3367628

实验名称：Selectivity ratio of EC50 for GAL4-fused human LXRbeta expressed in HEK293T cells to ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3367629

实验名称：Inverse agonist activity at APC-labeled RORgammat LBD (unknown origin) assessed as in... 来源：ChEMBL 靶标：Nuclear receptor ROR-gamma External Id：CHEMBL4707861

实验名称：Inverse agonist activity at APC-labeled RORgammat LBD (unknown origin) assessed as in... 来源：ChEMBL 靶标：Nuclear receptor ROR-gamma External Id：CHEMBL4707860

实验名称：Inverse agonist activity at RORgammat in mouse CD4+ T cells assessed as inhibition of... 来源：ChEMBL 靶标：Nuclear receptor ROR-gamma External Id：CHEMBL4707865

实验名称：Intrinsic clearance in CD-1 mouse liver microsomes assessed per mg protein at 1 uM me... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4707867

实验名称：Half life in CD-1 mouse liver microsomes at 1 uM measured up to 60 mins in presence o... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4707866

实验名称：Fraction unbound in human plasma after 4 hrs by LC-MS/MS analysis 来源：ChEMBL 靶标：Plasma External Id：CHEMBL3367614

共30条，当前第1页，共3页

1

2

3