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](https://www.chemicalbook.com/CAS/GIF/680590-49-2.gif)
- 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
- 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
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。
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靶点
OX 2 Receptor
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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.
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- 联系电话：--
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- 国家：英国
- 产品数：5726
- 优势度：77
