盐酸阿扎司琼
| 中文名称 | 盐酸阿扎司琼 |
|---|---|
| 中文同义词 | N-(1-氮杂双环[2.2.2]辛-8-基)-6-氯-4-甲基-3-氧代-3,4-二氢-2H-1,4-苯并恶嗪-8-甲酰胺盐酸盐;盐酸阿扎司琼;半合成脂肪酸甘油酯 (又名混合脂肪酸甘油酯);半混甘脂;盐酸阿扎西隆;6-氯-4-甲基-3-氧代-N-(奎宁环-3-基)-3,4-二氢-2H-苯并[B][1,4]恶嗪-8-甲酰胺盐酸盐 |
| 英文名称 | Azasetron hydrochloride |
| 英文同义词 | N-(1-Azabicyclo[2.2.2]octane-3-yl)-6-chloro-4-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide·hydrochloride;6-chloro-3-keto-4-methyl-N-quinuclidin-3-yl-1,4-benzoxazine-8-carboxamide hydrochloride;N-{1-azabicyclo[2.2.2]octan-3-yl}-6-chloro-4-Methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-8-carboxaMide;Azastron hydrochloride injection;N-(1-Azabicyclo[2.2.2]oct-3-yl)-6-chloro-4-Methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-8-carboxaMide hydrochloride (1:1);N-1-AZABICYCLO[2.2.2]-OCT-3-YL-6-CHLORO-3,4-DIHYDRO-4-METHYL-3-OXO-2H-1,4-BENZOXAZINE-8-CARBOXAMIDE, HYDROCHLORIDE;N-(1-AZABICYCLO[2.2.2]OCT-3-YL)-6-CHLORO-4-METHYL-3-OXO-3,4-DIHYDRO-2H-1,4-BENZOXAZINE-8-CARBOXAMIDE HCL;N-(1-AZABICYCLO[2.2.2]OCT-3-YL)-6-CHLORO-4-METHYL-3-OXO-3,4-DIHYDRO-2H-1,4-BENZOXAZINE-8-CARBOXAMIDE HYDROCHLORIDE |
| CAS号 | 123040-16-4 |
| 分子式 | C17H21Cl2N3O3 |
| 分子量 | 386.27 |
| EINECS号 | 692-159-3 |
| 相关类别 | 小分子抑制剂;有机原料;止吐药物;神经信号;标准品;中药对照品;医药原料和中间体;医药、农药及染料中间体;anti-emetic;Serotonin receptor;化工原料 |
| Mol文件 | 123040-16-4.mol |
| 结构式 |  |
盐酸阿扎司琼 性质
| 熔点 | 281° (dec); mp 305° (dec) (Kawakita) |
|---|---|
| 储存条件 | Sealed in dry,Room Temperature |
| 溶解度 | 甲醇（微溶）、水（微溶） |
| 形态 | 白色固体。 |
| 颜色 | 白色 |
| CAS 数据库 | 123040-16-4(CAS DataBase Reference) |
Azasetron HCl (Y-25130) 是一种选择性5-HT3受体拮抗剂，IC50为0.33 nM，用于癌症化疗引起的恶心和呕吐。
| Target | Value |
| 5-HT3 | 0.33 nM |
Azasetron could effectively penetrate through the skin and pass into the systemic circulation.
| Animal Model: | Four male Bama miniature pigs weighing 9-11 kg (15-16 weeks old). |
| Dosage: | 0.5 mg/kg. |
| Administration: | I.V. administration via the abdominal vein. |
| Result: | The mean plasma concentration dropped to minimum at 36 h. C max = 44.88 ± 7.16 ng/mL) was achieved at the time point of 66.00 ± 22.98 h (T max ). |
用途
预防化疗引起的恶心呕吐（5-HT3受体拮抗剂）安全信息
| 毒性 | LD50 in male, female rats (mg/kg): 135, 132 i.v. (Takagi) |
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| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-B0068 | Azasetron hydrochloride | 5 mg | 375元 | |
| 2024/01/25 | HY-B0068 | 盐酸阿扎司琼 Azasetron hydrochloride | 123040-16-4 | 10mg | 600元 |