PCO371

• 常用名: PCO371
• 英文名: PCO371
• CAS号: 1613373-33-3
• 分子量: 635.654
• 密度: 1.5±0.1 g/cm3
• 沸点: N/A
• 分子式: C₂₉H₃₂F₃N₅O₆S
• 熔点: N/A
• 闪点: N/A

PCO371用途

PCO371 是一种可口服的甲状旁腺激素受体 1 (PTHR1) 的完全抑制剂，对 PTHR2 无作用。

PCO371名称

• 中文名: PCO371
• 英文名: PCO371

PCO371生物活性

• 描述: PCO371 是一种可口服的甲状旁腺激素受体 1 (PTHR1) 的完全抑制剂,对 PTHR2 无作用。
• 相关类别:
  信号通路 >> 其他 >> 甲状腺激素受体
  研究领域 >> 内分泌
• 靶点实验:

  PTHR1[1]

• 体外研究: PCO371是甲状旁腺激素受体1(PTHR1)的口服活性完全激动剂,对PTH 2型受体没有影响。 PCO371在表达hPTHR1的COS-7细胞中诱导cAMP产生,EC50为2.4μM,在用hPTHR1-delNT转染的COS-7细胞中诱导2.5μM,并且还增强磷脂酶C活性(EC50,17μM)[1]。
• 参考文献:

  [1]. Tamura T, et al. Identification of an orally active small-molecule PTHR1 agonist for the treatment of hypoparathyroidism. Nat Commun. 2016 Nov 18;7:13384.

PCO371物理化学性质

• 密度: 1.5±0.1 g/cm3
• 分子式: C₂₉H₃₂F₃N₅O₆S
• 分子量: 635.654
• 精确质量: 635.202515
• LogP: 4.56
• InChIKey: LDZJFVOUPUFOHX-UHFFFAOYSA-N
• SMILES: Cc1cc(N2C(=O)NC(=O)C2(C)C)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O
• 折射率: 1.636
• 储存条件: 2-8°C

PCO371靶点实验

查看更多实验

实验名称：Anti-hypoparathyroidism activity in po dosed TPTX Crl:CD(SD) rat assessed as time req... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4344453

实验名称：Anti-hypoparathyroidism activity in po dosed TPTX Crl:CD(SD) rat assessed as time req... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4344452

实验名称：Anti-hypoparathyroidism activity in po dosed TPTX Crl:CD(SD) rat assessed as increase... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4344450

实验名称：Anti-hypoparathyroidism activity in po dosed TPTX Crl:CD(SD) rat assessed as decrease... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4344449

实验名称：Anti-hypoparathyroidism activity in po dosed TPTX Crl:CD(SD) rat assessed as increase... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4344448

实验名称：cAMP Assay from US Patent US9428505: "Hydantoin derivative" 来源：BindingDB 靶标：N/A External Id：BindingDB_8383_1

实验名称：Oral bioavailability in rat at 2 mg/kg by LC-MS/MS analysis 来源：ChEMBL 靶标：N/A External Id：CHEMBL4344447

实验名称：Half life in rat at 2 mg/kg, po by LC-MS/MS analysis 来源：ChEMBL 靶标：N/A External Id：CHEMBL4344446

实验名称：Glutathione reactivity in human liver microsomes assessed as GSH-adduct formation at ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4344437

实验名称：Clearance in human liver microsomes at 1 uM measured after 30 mins in presence of NAD... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4344436

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PCO371英文别名

• 1-{3,5-Dimethyl-4-[2-({4-oxo-2-[4-(trifluoromethoxy)phenyl]-1,3,8-triazaspiro[4.5]dec-1-en-8-yl}sulfonyl)ethyl]phenyl}-5,5-dimethyl-2,4-imidazolidinedione