他非诺喹

• 常用名: 他非诺喹
• 英文名: Tafenoquine
• CAS号: 106635-80-7
• 分子量: 463.49300
• 密度: 1.237g/cm3
• 沸点: 565.6ºC at 760mmHg
• 分子式: C₂₄H₂₈F₃N₃O₃
• 熔点: N/A
• 闪点: 295.9ºC

他非诺喹用途

Tafenoquine (WR 238605) 是一种 8-氨基喹啉。Tafenoquine 作为抗疟疾预防剂[1]。

他非诺喹名称

• 中文名: 他非诺喹
• 英文名: 4-N-[2,6-dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]quinolin-8-yl]pentane-1,4-diamine

他非诺喹生物活性

• 描述: Tafenoquine (WR 238605) 是一种 8-氨基喹啉。Tafenoquine 作为抗疟疾预防剂[1]。
• 相关类别:
  信号通路 >> 抗感染 >> 寄生物
  研究领域 >> 感染
• 靶点实验:

  Anti-malarial[1]

• 体内研究: 当以在WT小鼠中建立的ED100值(3mg/kg)给药时,Tafenoquine在CYP 2D敲除小鼠中没有表现出抗疟疾活性。当人源化/ CYP 2D6敲入小鼠的ED100(6mg/kg)的两倍测试时,Tafenoquine抗疟疾活性部分恢复[1]。
• 参考文献:

  [1]. Marcsisin SR, et al. Tafenoquine and NPC-1161B require CYP 2D metabolism for anti-malarial activity: implications for the 8-aminoquinoline class of anti-malarial compounds. Malar J. 2014 Jan 3;13:2.

他非诺喹物理化学性质

• 密度: 1.237g/cm3
• 沸点: 565.6ºC at 760mmHg
• 分子式: C₂₄H₂₈F₃N₃O₃
• 分子量: 463.49300
• 闪点: 295.9ºC
• 精确质量: 463.20800
• PSA: 78.63000
• LogP: 6.68410
• InChIKey: LBHLFPGPEGDCJG-UHFFFAOYSA-N
• SMILES: COc1cc(C)c2c(Oc3cccc(C(F)(F)F)c3)c(OC)cc(NC(C)CCCN)c2n1
• 蒸汽压: 8.17E-13mmHg at 25°C
• 折射率: 1.572
• 储存条件: 2-8℃

他非诺喹靶点实验

查看更多实验

实验名称：Binding affinity towards rat Gabra1 in an in vitro assay with cellular components mea... 来源：ChEMBL 靶标：Gamma-aminobutyric acid receptor subunit alpha-1 External Id：CHEMBL5291800

实验名称：Effect on ATP synthesis in tafenoquine-resistant promastigotes of Leishmania major R4... 来源：ChEMBL 靶标：Leishmania major External Id：CHEMBL1693164

实验名称：Induction of acidification in tafenoquine-resistant promastigotes of Leishmania major... 来源：ChEMBL 靶标：Leishmania major External Id：CHEMBL1693165

实验名称：Induction of acidification in wild type promastigotes of Leishmania major MHOM/JL/80/... 来源：ChEMBL 靶标：Leishmania major External Id：CHEMBL1693166

实验名称：Induction of acidification in tafenoquine-resistant promastigotes of Leishmania major... 来源：ChEMBL 靶标：Leishmania major External Id：CHEMBL1693167

实验名称：Induction of acidification in tafenoquine-resistant promastigotes of Leishmania major... 来源：ChEMBL 靶标：Leishmania major External Id：CHEMBL1693168

实验名称：Binding affinity towards human ESR1 in an in vitro cell free assay (CRO assay) measur... 来源：ChEMBL 靶标：Estrogen receptor External Id：CHEMBL5291792

实验名称：Antimalarial activity against asexual stage of Plasmodium falciparum 3D7 after 72 hrs... 来源：ChEMBL 靶标：Plasmodium falciparum External Id：CHEMBL2439161

实验名称：Compound was evaluated for inhibition of human F2 in an in vitro cell free assay meas... 来源：ChEMBL 靶标：Prothrombin External Id：CHEMBL5291794

实验名称：Antimalarial activity against early (1 to 3) gametocytic stage of Plasmodium falcipar... 来源：ChEMBL 靶标：Plasmodium falciparum External Id：CHEMBL2439659

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他非诺喹英文别名

• 8-<(4-amino-1-methylbutyl)amino>-2,6-dimethoxy-4-methyl-5-<3-(trifluoromethyl)phenoxy>quinoline
• Tafenoquine
• N(4)-(2,6-Dimethoxy-4-methyl-5-((3-trifluoromethyl)phenoxy)-8-quinolinyl)-1,4-pentanediamine
• (R)-N3-(2,6-Dimethoxy-4-methyl-5-(3-trifluoromethyl)phenoxy)quinolin-8-yl)pentane-1,4-diamine
• 1,4-Pentanediamine,N4-(2,6-dimethoxy-4-methyl-5-(3-(trifluoromethyl)phenoxy)-8-quinolinyl)
• Tafenoquine (USAN)
• (RS)-N(sup 3)-(2,6-Dimethoxy-4-methyl-5-(3-trifluoro-methylphenoxy)quinolin-8-yl)pentane-1,4-diamine