2,4,6-三氟-N-[6-[(1-甲基-4-哌啶基)羰基]-2-吡啶基]苯甲酰胺

• 常用名: 2,4,6-三氟-N-[6-[(1-甲基-4-哌啶基)羰基]-2-吡啶基]苯甲酰胺
• 英文名: Lasmiditan
• CAS号: 439239-90-4
• 分子量: 377.360
• 密度: 1.4±0.1 g/cm3
• 沸点: 433.3±45.0 °C at 760 mmHg
• 分子式: C₁₉H₁₈F₃N₃O₂
• 熔点: N/A
• 闪点: 215.9±28.7 °C

用途

Lasmiditan (COL-144; LY573144)是高亲和性5-HT1F选择性激动剂,Ki为2.1 nM,而对5-HT(1B)和5-HT(1D)受体的Ki则分别为1043 nM和1357 nM。

名称

• 中文名: 2,4,6-三氟-N-[6-[(1-甲基-4-哌啶基)羰基]-2-吡啶基]苯甲酰胺
• 英文名: 2,4,6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)pyridin-2-yl]benzamide

生物活性

• 描述: Lasmiditan (COL-144; LY573144)是高亲和性5-HT1F选择性激动剂,Ki为2.1 nM,而对5-HT(1B)和5-HT(1D)受体的Ki则分别为1043 nM和1357 nM。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体
  信号通路 >> 神经信号通路 >> 5-HT受体
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Nelson DL, et al. Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan. Cephalalgia. 2010 Oct;30(10):1159-69.

  [2]. Tfelt-Hansen PC, et al. The 5-HT1F receptor agonist lasmiditan as a potential treatment of migraine attacks: a review of two placebo-controlled phase II trials. J Headache Pain. 2012 Jun;13(4):271-5.

物理化学性质

• 密度: 1.4±0.1 g/cm3
• 沸点: 433.3±45.0 °C at 760 mmHg
• 分子式: C₁₉H₁₈F₃N₃O₂
• 分子量: 377.360
• 闪点: 215.9±28.7 °C
• 精确质量: 377.135101
• PSA: 62.30000
• LogP: 1.90
• InChIKey: XEDHVZKDSYZQBF-UHFFFAOYSA-N
• SMILES: CN1CCC(C(=O)c2cccc(NC(=O)c3c(F)cc(F)cc3F)n2)CC1
• 蒸汽压: 0.0±1.0 mmHg at 25°C
• 折射率: 1.585
• 储存条件: 2-8℃

安全信息

• 海关编码: 2933990090

海关

• 海关编码: 2933990090
• 中文概述: 2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
• 申报要素: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
• Summary: 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

靶点实验

查看更多实验

实验名称：Thermal Shift Assay. Domain: start/stop: M1-L298 来源：ChEMBL 靶标：Cyclin-dependent kinase 2 External Id：CHEMBL5063568

实验名称：Thermal Shift Assay. Domain: start/stop: M1-L298 来源：ChEMBL 靶标：Cyclin-dependent kinase 2 External Id：CHEMBL5062802

实验名称：Antimigraine activity against electrical stimulation of trigeminal ganglion migraine ... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4830590

实验名称：Antimigraine activity against electrical stimulation of trigeminal ganglion migraine ... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4830562

实验名称：Bioavailability in Sprague-Dawley rat at 5 mg/kg, ig measured for 24 hrs by LC-MS/MS ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4830561

实验名称：Clearance in Sprague-Dawley rat at 1 mg/kg, iv measured for 24 hrs by LC-MS/MS analys... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4830560

实验名称：Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv measured ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4830559

实验名称：Thermal Shift Assay. Domain: start/stop: M26-R383 来源：ChEMBL 靶标：Glycogen synthase kinase-3 beta External Id：CHEMBL5066355

实验名称：Thermal Shift Assay. Domain: start/stop: M26-R383 来源：ChEMBL 靶标：Glycogen synthase kinase-3 beta External Id：CHEMBL5065589

实验名称：Thermal Shift Assay. Domain: start/stop: S229-K512 来源：ChEMBL 靶标：Tyrosine-protein kinase ABL1 External Id：CHEMBL5060015

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英文别名

• COL-144
• 2,4,6-trifluoro-N-[6-(1-methyl-piperidin-4-ylcarbonyl)-pyridin-2-yl]-benzamide
• 2,4,6-Trifluoro-N-(6-(1-methylpiperidine-4-carbonyl)pyridin-2-yl)benzamide
• Lasmiditan [INN]
• 2,4,6-trifluoro-N-{6-[(1-methylpiperidin-4-yl)carbonyl]pyridin-2-yl}benzamide
• 2,4,6-trifluoro-N-[6-(1-methyl-piperidin-4-ylcarbonyl)-pyridine-2-yl]-benzamide
• 2,4,6-Trifluoro-N-{6-[(1-methyl-4-piperidinyl)carbonyl]-2-pyridinyl}benzamide
• 2,4,6-trifluoro-N-(6-(1-methylpiperidine-4-carbonyl)pyridine-2-yl)benzamide
• Lasmiditan (USAN/INN)
• lasmitidan
• Lasmiditan