N-[3-[4-[[4-(3,4-二氢-2-氧代-1(2H)-喹啉基)-1-哌啶基]羰基]苯氧基]丙基]乙酰胺
中文名称 | N-[3-[4-[[4-(3,4-二氢-2-氧代-1(2H)-喹啉基)-1-哌啶基]羰基]苯氧基]丙基]乙酰胺 |
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中文同义词 | N-[3-[4-[[4-(3,4-二氢-2-氧代-1(2H)-喹啉基)-1-哌啶基]羰基]苯氧基]丙基]乙酰胺;化合物OPC 21268;OPC 21268,加压素V1拮抗剂 |
英文名称 | OPC 21268 |
英文同义词 | 1-[1-[4-(3-Acetylaminopropoxy)benzoyl]-4-piperidyl]-3,4-dihydroquinolin-2(1H)-one;1-{1-[4(3-acetylaminopropoxy)benzoyl]-4-piperidyl}-3,4-dihydro-2(1H)-quinolinone hydrate;N-[3-[4-[[4-(3,4-dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-acetamide hydrate;OPC-21268 hydrate;N-[3-[4-[[4-(3,4-Dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]acetamide;OPC 21268;N-[3-[4-[4-(2-oxo-3,4-dihydroquinolin-1-yl)piperidine-1-carbonyl]phenoxy]propyl]acetamide;OPC 21268;OPC-21268;OPC21268 |
CAS号 | 131631-89-5 |
分子式 | C26H31N3O4 |
分子量 | 449.54 |
EINECS号 | |
相关类别 | |
Mol文件 | 131631-89-5.mol |
结构式 |
N-[3-[4-[[4-(3,4-二氢-2-氧代-1(2H)-喹啉基)-1-哌啶基]羰基]苯氧基]丙基]乙酰胺 性质
沸点 | 772.5±60.0 °C(Predicted) |
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密度 | 1?+-.0.06 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | 二甲基亚砜:≥20mg/mL |
酸度系数(pKa) | 16.17±0.46(Predicted) |
形态 | 粉末 |
颜色 | 白色至类白色 |
IC50: 0.4 μM (vasopressin V1)
Ki: 0.14 μM (vasopressin V1)
The concentration of Fuscoside (OPC-21268) that displaces 50% of specific AVP binding (IC 50 ) is 0.4 μM for VI receptors and 100 μM for V2 receptors. The inhibition constant (K i ) of Fuscoside (OPC-21268) for V1 receptors (0.14 μM).
Fuscoside (OPC-21268) competitively and specifically antagonizes pressor responses to AVP in vivo . Oral administration of Fuscoside (OPC-21268) (10 mg/kg) inhibits the vasoconstriction induced by exogenous AVP in a dose- and time-dependent manner and the effect lasts for more than 8 hours at 30 mg/kg. Fuscoside (OPC-21268) predominantly exerts a protective effect in areas where the maximum amount of blood-brain barrier breakdown occurs, and it is effective in the treatment of cold-induced vasogenic brain edema. Fuscoside (OPC-21268) treatment at the dosages of 200 and 300 mg/kg significantly reduces brain water content in both hemispheres. Swelling of the traumatized hemispheres is also significantly reduced at 200 and 300 mg/kg dosages.
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-15009 | Fuscoside | 1 mg | 377元 | |
2024/08/19 | HY-15009 | N-[3-[4-[[4-(3,4-二氢-2-氧代-1(2H)-喹啉基)-1-哌啶基]羰基]苯氧基]丙基]乙酰胺 Fuscoside | 131631-89-5 | 5mg | 900元 |