网站主页 >> 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
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- 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
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N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE化学性质
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沸点:
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660.7±65.0 °C(Predicted)
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密度:
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1.280±0.06 g/cm3(Predicted)
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储存条件:
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-20°C
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溶解度:
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Soluble to 100 mM in DMSO and to 100 mM in ethanol
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形态:
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Powder
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酸度系数(pKa):
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4.77±0.10(Predicted)
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颜色:
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white to light brown
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N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE性质、用途与生产工艺
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。
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.
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:
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Male NMRI mice (20-30 g)
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Dosage:
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1, 3, 10, 30, 100, 300 mg/kg
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Administration:
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Injected i.p. at a volume of 10 mL/kg
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Result:
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Dose-dependently reversed this [Ala
11
,D-Leu
15
]orexin-B-induced hyperlocomotion without itself significantly affecting LMA.
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Animal Model:
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France and Male Wistar rats (196-237 g)
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Dosage:
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3, 10, 30 mg/kg
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Administration:
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Injected i.p. at a volume of 5 mL/kg
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Result:
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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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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
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