GDC-0310

• 常用名: GDC-0310
• 英文名: GDC-0310
• CAS号: 1788063-52-4
• 分子量: 480.3991232
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₅H₂₈Cl₂FNO₃
• 熔点: N/A
• 闪点: N/A

GDC-0310用途

GDC-0310是一种选择性酰基磺酰胺Nav1.7抑制剂,hNav1.7的IC50为0.6 nM[1]。

GDC-0310名称

• 英文名: (S) -methyl 5-cyclopropyl-4- ( (1- (1- (3, 5-dichlorophenyl) ethyl) piperidin-4-yl) methoxy) -2-fluorobenzoate

GDC-0310生物活性

• 描述: GDC-0310是一种选择性酰基磺酰胺Nav1.7抑制剂,hNav1.7的IC50为0.6 nM[1]。
• 相关类别:
  信号通路 >> 跨膜转运 >> 钠通道
  研究领域 >> 神经疾病
• 靶点实验:

  hNav1.4:3.4 nM (IC50)

  hNav1.2:38 nM (IC50)

  hNav1.6:198 nM (IC50)

  hNav1.1:202 nM (IC50)

  hNav1.5:551 nM (IC50)

• 体外研究: GDC-0310在体内的EC50为1.1μM,Nav1.7的Ki为1.8 nM[1]。
• 体内研究: GDC-0310显示出显著改善的Nav选择性和ADME性能[1]。GDC-0310在大鼠(5mg/kg,iv)、狗(1mg/kg,iv)和食蟹猴(2mg/kg,iv)中分别显示出5h、46h和4.4h的t1/2值[1]。
• 参考文献:

  [1]. Brian S Safina, et al. Discovery of Acyl-sulfonamide Na v 1.7 Inhibitors GDC-0276 and GDC-0310. J Med Chem. 2021 Mar 25;64(6):2953-2966.

  [2]. Lei Xu, et al. Voltage-gated sodium channels: structures, functions, and molecular modeling. Drug Discov Today. 2019 Jul;24(7):1389-1397.

GDC-0310物理化学性质

• 分子式: C₂₅H₂₈Cl₂FNO₃
• 分子量: 480.3991232

GDC-0310靶点实验

查看更多实验

实验名称：Inhibition of human Nav1.5/beta1/2 transfected in HEK293-A cells assessed as inhibiti... 来源：ChEMBL 靶标：Sodium channel protein type 5 subunit alpha External Id：CHEMBL5252388

实验名称：Metabolic stability in human liver microsomes assessed as intrinsic clearance at 1 uM... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5055694

实验名称：Inhibition of human Nav1.1/beta1/2 transfected in HEK293-A cells assessed as inhibiti... 来源：ChEMBL 靶标：Sodium channel protein type 1 subunit alpha External Id：CHEMBL5252387

实验名称：Inhibition of human Nav1.7/beta1/2 transfected in HEK293-A cells assessed as inhibiti... 来源：ChEMBL 靶标：Sodium channel protein type 9 subunit alpha External Id：CHEMBL5252384

实验名称：Lipophilicity, logD of the compound at pH 7.4 by shake flask assay based LC-MS/MS ana... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5055696

实验名称：Metabolic stability in human hepatocytes assessed as intrinsic clearance at 1 uM meas... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5055695

实验名称：Selectivity index, ratio of IC50 for human Nav1.6 expressed in CHO cells to IC50 for ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5055731

实验名称：Selectivity index, ratio of IC50 for human Nav1.1 expressed in HEK cells to IC50 for ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5055726

实验名称：Selectivity index, ratio of IC50 for human Nav1.2 expressed in HEK cells to IC50 for ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5055725

实验名称：Oral bioavailability in cynomolgus monkey at 2 mg/kg measured upto 24 hrs by LC-MS/MS... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5055724

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