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ChemicalBook  CAS数据库列表  N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE

N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE

生物活性 靶点 体外研究 体内研究
N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE,680590-49-2,结构式
N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE
  • CAS号:680590-49-2
  • 英文名:EMPA
  • 中文名:N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE
  • CBNumber:CB32695845
  • 分子式:C23H26N4O4S
  • 分子量:454.54
  • MOL File:680590-49-2.mol
N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE化学性质
  • 沸点 :660.7±65.0 °C(Predicted)
  • 密度 :1.280±0.06 g/cm3(Predicted)
  • 储存条件 :-20°C
  • 溶解度 :Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • 形态 :Powder
  • 酸度系数(pKa) :4.77±0.10(Predicted)
  • 颜色 :white to light brown
安全信息
  • 危险品标志 :Xn
  • 危险类别码 :22
  • WGK Germany :3

N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE性质、用途与生产工艺

  • 生物活性 EMPA 是一种高亲和力的，可逆的选择性 orexin OX2 受体拮抗剂。[3H] EMPA 与人和大鼠 OX2-HEK293 膜结合，KD 值分别为 1.1 和 1.4 nM。
  • 靶点

    OX 2 Receptor

  • 体外研究

    EMPA competitively antagonizes orexin-A-and orexin-B-evoked accumulation of [ 3 H]inositol phosphates (IP) at hOX 2 receptors with pA 2 values of 8.6 and 8.8 respectively.
    EMPA displaces the [ 3 H]EMPA binding from cell membranes containing human and rat OX 2 receptors, with K i values of 1.10±0.24 nM and 1.45±0.13 nM, respectively.
    EMPA shows an IC 50 =5.75 µM, K i =2.63 µM, and IC 50 =12.8 µM, K i =5.8 µM in the binding assay at human and mouse V 1a receptors, respectively.
    In CHO(dHFr - ) cells stably expressing hOX 2 receptors, EMPA inhibits orexin-A-or orexin-B-evoked [Ca 2+ ] i response with IC 50 s of 8.8±1.7 nM and 7.9±1.7 nM, respectively.

  • 体内研究

    EMPA (1-300 mg/kg; i.p.) dose-dependently reverses this [Ala 11 ,D-Leu 15 ]orexin-B-induced hyperlocomotion without itself significantly affecting locomotor activity (LMA) in male NMRI mice.
    EMPA (3-30 mg/kg; i.p.) induces a significant and dose-dependent reduction in the baseline LMA in france and male Wistar rats. EMPA (3-30 mg/kg; i.p.) demonstrates a clear dose-dependent inhibition of spontaneous activity as compared with vehicle-treated animals.

    Animal Model: Male NMRI mice (20-30 g)
    Dosage: 1, 3, 10, 30, 100, 300 mg/kg
    Administration: Injected i.p. at a volume of 10 mL/kg
    Result: Dose-dependently reversed this [Ala 11 ,D-Leu 15 ]orexin-B-induced hyperlocomotion without itself significantly affecting LMA.
    Animal Model: France and Male Wistar rats (196-237 g)
    Dosage: 3, 10, 30 mg/kg
    Administration: Injected i.p. at a volume of 5 mL/kg
    Result: Induced a significant and dose-dependent reduction in the baseline LMA.
    Demonstrated a clear dose-dependent inhibition of spontaneous activity as compared with vehicle-treated animals.
N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE上下游产品信息
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N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE生产厂家
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