爱维莫潘
| 中文名称 | 爱维莫潘 |
|---|---|
| 中文同义词 | 爱维莫潘二水合物;2-((S)-2-苄基-3-((3R,4R)-4-(3-羟基苯基)-3,4-二甲基哌啶-1-基)丙酰胺基)乙酸二水合物;阿维莫泮二水合物;化合物 T22238;艾维莫潘二水合物 |
| 英文名称 | 2-[[(2S)-2-benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperi dyl]propanoyl]amino]acetic acid dihydrate |
| 英文同义词 | 2-[[(2S)-2-benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperi dyl]propanoyl]amino]acetic acid dihydrate;[[(2S)-2-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]methyl]-3-phenylpropanoyl]amino]acetic acid dehydrate;(((2S)-2-(((3R,4R)-4-(3-Hydroxyphenyl)-3,4-dimethylpiperidin-1-yl)methyl)-3-phenylpropanoyl)amino)acetic acid dihydrate;156053-89-3 (Anhydrous);Alvimopan hydrate;Entereg;Glycine, N-((2S)-2-(((3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl)methyl)-1-oxo-3-phenylpropyl)-, dihydrate;Glycine, N-(2-((4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl)methyl)-1-oxo-3-phenylpropyl)-,dihydrate, (3R-(1(S*),3-alpha,4-alpha))- |
| CAS号 | 170098-38-1 |
| 分子式 | C25H36N2O6 |
| 分子量 | 460.57 |
| EINECS号 | |
| 相关类别 | 原料药;化工中间体;API |
| Mol文件 | 170098-38-1.mol |
| 结构式 |  |
爱维莫潘 性质
| 熔点 | 210-213° |
|---|---|
| 比旋光度 | D25 +51.8° (c = 1.0 in DMSO) |
| 储存条件 | 2-8°C |
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 粉末 |
Alvimopan (LY-246736)是一种有效的、相对非选择性的opioid拮抗剂，对μ, δ 和 κ opioid receptors的Ki值分别为0.77、4.4和40 nM，选择性比对其他胺类G蛋白偶联受体高100倍以上
| Target | Value |
|
μ-opioid receptor
(Cell-free assay) | 0.77 nM(Ki) |
|
δ-opioid receptor
(Cell-free assay) | 4.4 nM(Ki) |
|
κ-opioid receptor
(Cell-free assay) | 40 nM(Ki) |
Alvimopan inhibits the loperamide-stimulated [ 35 S]GTPγS binding to membranes containing the cloned human μ-opioid receptor, with an IC 50 of 1.7 nM.
Alvimopan (0.1-1.0 mg/kg; p.o.) partially antagonizes the slowing of small intestinal transit of
113
Sn-labelled microspheres produced by morphine in rats.
Alvimopan (3 mg/kg; p.o.) has no effect on the visceromotor behavioural responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-76657A | Alvimopan dihydrate | 1 mg | 431元 | |
| 2024/01/25 | HY-76657A | 爱维莫潘二水合物 Alvimopan dihydrate | 170098-38-1 | 5mg | 950元 |