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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, 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
英文别名:
EMPA, CID 9981404;Hypocretin Receptor,EMPA,Orexin Receptor (OX Receptor),HCRT Receptor,inhibit,Inhibitor;N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE;N-Ethyl-2-[(6-methoxy-3-pyridinyl)[(2-methylphenyl)sulfonyl]amino]-N-(3-pyridinylmethyl)-acetamide;Acetamide, N-ethyl-2-[(6-methoxy-3-pyridinyl)[(2-methylphenyl)sulfonyl]amino]-N-(3-pyridinylmethyl)-
中文名:
N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE
中文别名:
化合物EMPA;EMPA,OX2拮抗剂;N-乙基-2-[(6-甲氧基-3-吡啶基)[(2-甲基苯基)磺酰基]氨基]-N-(3-吡啶基甲基)乙酰胺
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

上游原料

下游产品


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

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680590-49-2, N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE 相关搜索:

  • Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals, Sulfur & Selenium Compounds
  • N-乙基-2-[(6-甲氧基-3-吡啶基)[(2-甲基苯基)磺酰基]氨基]-N-(3-吡啶基甲基)乙酰胺
  • EMPA,OX2拮抗剂
  • 化合物EMPA
  • 680590-49-2
  • Hypocretin Receptor,EMPA,Orexin Receptor (OX Receptor),HCRT Receptor,inhibit,Inhibitor
  • Acetamide, N-ethyl-2-[(6-methoxy-3-pyridinyl)[(2-methylphenyl)sulfonyl]amino]-N-(3-pyridinylmethyl)-
  • EMPA, CID 9981404
  • N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE
  • N-Ethyl-2-[(6-methoxy-3-pyridinyl)[(2-methylphenyl)sulfonyl]amino]-N-(3-pyridinylmethyl)-acetamide
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