OLORINAB
| 中文名称 | OLORINAB |
|---|---|
| 中文同义词 | 化合物 T14302;化合物OLORINAB;(4AS,5AS)-4,4A,5,5A-四氢-N-[(1S)-1-(羟甲基)-2,2-二甲基丙基]-1-(4-氧代-2-吡嗪基)-1H-环丙烷并[4,5]环戊二烯并[1,2-C]吡唑-3-甲酰胺;3-[(4AS,5AS)-3-[[(S)-1-羟基-3,3-二甲基-2-丁基]氨基甲酰基]-4,4A,5,5A-四氢-1H-环丙并[4,5]环戊并[1,2-C]吡唑-1-基]吡嗪-1-氧化物 |
| 英文名称 | Olorinab |
| 英文同义词 | Olorinab;1H-Cyclopropa[4,5]cyclopenta[1,2-c]pyrazole-3-carboxamide, 4,4a,5,5a-tetrahydro-N-[(1S)-1-(hydroxymethyl)-2,2-dimethylpropyl]-1-(4-oxido-2-pyrazinyl)-, (4aS,5aS)-;APD 371 - Bio-X;(2S,4S)-N-[(1S)-1-(hydroxymethyl)-2,2-dimethyl-propyl]-9-(4-oxidopyrazin-4-ium-2-yl)-8,9-diazatricyclo[4.3.0.02?]nona-1(6),7-diene-7-carboxamide;3-[(4aS,5aS)-3-[[(S)-1-Hydroxy-3,3-dimethyl-2-butyl]carbamoyl]-4,4a,5,5a-tetrahydro-1H-cyclopropa[4,5]cyclopenta[1,2-c]pyrazol-1-yl]pyrazine 1-Oxide |
| CAS号 | 1268881-20-4 |
| 分子式 | C18H23N5O3 |
| 分子量 | 357.41 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1268881-20-4.mol |
| 结构式 |  |
OLORINAB 性质
| 沸点 | 636.6±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.49±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 可溶于氯仿（少许）、甲醇（少许） |
| 酸度系数(pKa) | 13.39±0.20(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至类白色 |
EC50: 6.2 nM (hCB 2 ).
A comprehensive in vitro profile of Olorinab (APD 371) (6) shows that single digit nanomolar potency and full intrinsic efficacy are maintained in all species assessed, and that Olorinab (APD 371) is highly selective for CB 2 over CB 1 in both binding and functional assays. Furthermore, Olorinab (APD 371) induces efficient receptor internalization (~106% relative to the CB1/2 agonist CP55,940) in CHO cells expressing HA-tagged rat CB 2 suggesting that, according to the hypothesis, Olorinab (APD 371) would be able to drive agonist-induced receptor recycling.
Olorinab (APD 371) significantly increases paw withdrawal thresholds at doses ≥3 mg/kg PO (ED 50 =2.3 mg/kg). In a separate experiment, a single dose of Olorinab (APD 371) (10 mg/kg, PO) inhibits paw withdrawal threshold for up to 4 hours after administration. Seperately, the analgesic effects of Olorinab (APD 371) are shown to be highly likely mediated via activity at CB 2 receptors.
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-111110 | Olorinab | 1 mg | 681元 | |
| 2024/01/25 | HY-111110 | OLORINAB Olorinab | 1268881-20-4 | 5mg | 1500元 |