Foliglurax

• 常用名: Foliglurax
• 英文名: Foliglurax
• CAS号: 1883329-51-8
• 分子量: 421.51
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₃H₂₃N₃O₃S
• 熔点: N/A
• 闪点: N/A

Foliglurax用途

Foliglurax (PXT002331) 是一种可渗透脑的,有效的选择性 mGluR4 正变构调节剂 (PAM),EC50 为 79 nM。抗帕金森病。

Foliglurax名称

• 英文名: Foliglurax

Foliglurax生物活性

• 描述: Foliglurax (PXT002331) 是一种可渗透脑的,有效的选择性 mGluR4 正变构调节剂 (PAM),EC50 为 79 nM。抗帕金森病。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 谷氨酸受体
  研究领域 >> 神经疾病
• 靶点实验:

  mGlu4:79 nM (EC50)

• 体外研究: Foliglurax是一种高度选择性和有效的mglu4受体PAM,具有显著的脑外显率特征,可能会彻底改变mglu4受体药物靶向中枢神经系统疾病的领域[2]。
• 参考文献:

  [1]. Charvin D, et al. Discovery, Structure-Activity Relationship, and Antiparkinsonian Effect of a Potent and Brain-Penetrant Chemical Series of Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4. J Med Chem. 2017 Oct 26;60(20):8515-8537.

  [2]. Volpi C, et al. Opportunities and challenges in drug discovery targeting metabotropic glutamate receptor 4. Expert Opin Drug Discov. 2018 May;13(5):411-423.

Foliglurax物理化学性质

• 分子式: C₂₃H₂₃N₃O₃S
• 分子量: 421.51
• InChIKey: WVFFSBHGWAUQIN-DUOAXNJCSA-N
• SMILES: Cl.Cl.ON=c1cc(-c2cc3sccc3cn2)oc2ccc(CCCN3CCOCC3)cc12
• 储存条件: 2-8°C

Foliglurax靶点实验

查看更多实验

实验名称：Positive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK29... 来源：ChEMBL 靶标：Metabotropic glutamate receptor 4 External Id：CHEMBL4019911

实验名称：Selectivity ratio of compound effect for positive allosteric modulation of recombinan... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4019906

实验名称：Plasma clearance in Sprague-Dawley rat at 1 mg/kg, iv administered as single dose by ... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4019857

实验名称：AUC (0 to infinity) in Sprague-Dawley rat at 1 mg/kg, iv administered as single dose ... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4019855

实验名称：Drug uptake in Sprague-Dawley rat brain at 10 mg/kg, po after 90 mins post dose admin... 来源：ChEMBL 靶标：Brain External Id：CHEMBL4019916

实验名称：Half life in Sprague-Dawley rat at 1 mg/kg, iv administered as single dose by LC-MS/M... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4019853

实验名称：Drug uptake in Sprague-Dawley rat brain at 10 mg/kg, po after 60 mins post dose admin... 来源：ChEMBL 靶标：Brain External Id：CHEMBL4019917

实验名称：Activity at kainate glutamate receptor in rat cerebral cortex at 10 uM 来源：ChEMBL 靶标：N/A External Id：CHEMBL4019831

实验名称：Selectivity ratio of compound effect for positive allosteric modulation of recombinan... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4019892

实验名称：Activity at NMDA glutamate receptor in rat cerebral cortex at 10 uM 来源：ChEMBL 靶标：N/A External Id：CHEMBL4019828

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