多佐胺
| 中文名称 | 多佐胺 |
|---|---|
| 中文同义词 | 多佐胺杂质;多佐胺/杜塞酰胺;(2R,4R)-2-乙基氨基-4-甲基-5,5-二氧代-5,7-二硫杂双环[4.3.0]壬-8,10-二烯-8-磺酰胺;多佐胺-2-6;杜塞酰胺;多佐胺;多佐胺盐酸盐;蒲勒酮 |
| 英文名称 | Dorzolamide |
| 英文同义词 | DORZOLAMIDE;DORZOLAMIDE(SUBJECTTOPATENTFREE);4H-Thieno[2,3-b]thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, (4S,6S)-;4H-Thieno[2,3-b]thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, (4S-trans)-;4S,6S-Dorzolamide;(4S,6S)-4H-Thieno[2,3-b]thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide;(4S,6S)-4-(ethylamino)-5,6-dihydro-6-methyl-7,;Dorzalamide hydrochloride |
| CAS号 | 120279-96-1 |
| 分子式 | C10H16N2O4S3 |
| 分子量 | 324.44 |
| EINECS号 | 1533716-785-6 |
| 相关类别 | |
| Mol文件 | 120279-96-1.mol |
| 结构式 |  |
多佐胺 性质
| 沸点 | 575.8±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.53±0.1 g/cm3(Predicted) |
| 储存条件 | room temp |
| 溶解度 | DMSO：可溶5mg/mL（透明溶液，加热） |
| 酸度系数(pKa) | pKa 6.35 (Uncertain);8.50 (Uncertain) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| 旋光性 (optical activity) | [α]/D -25 to -35°, c = 1 in methanol |
| CAS 数据库 | 120279-96-1(CAS DataBase Reference) |
Dorzolamide (L671152) 是有效的碳酸酐酶 carbonic anhydrase II 的抑制剂，其对红细胞 CA-II 和 CA-I 的 IC50 值分别为 0.18 nM 和 600 nM。
Component A, caused by an inward flux of CO2 and its subsequent hydration by CA-II, is blocked by Dorzolamide in a dose-dependent manner with an 50% inhibitory concentration IC
50
of 2.4 μM (95% confidence interval: 0.5-10.85 μM).
Dorzolamide (3, 10, or 30 mg/kg/day, ip) synergized mitomycin C exhibits anti-tumor activity in EAC solid tumor models. Dorzolamide produces a dose-dependent decrease in the calculated ratio (relative value of 57.3±1, 25.5±1.8, and 24.3± 0.7 %, respectively).
| Animal Model: | Female Swiss albino mice (EAC solid tumor). |
| Dosage: | 3, 10, or 30 mg/kg/day (synergized mitomycin C). |
| Administration: | IP, daily for 3 weeks. |
| Result: |
Upregulated TXNIP and p53 while downregulated bcl-2.
Effective in retarding the growth of EAC in mice. |
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