货号:A259943 同义名: 地达诺辛;去羟肌苷 / Didanosine;ddI
Didanosine is an inhibitor of reverse transcriptase with IC50 of 0.49 μM.
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描述 | Didanosine is a reverse transcriptase inhibitor with an IC50 of 0.49 μM. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Didanosine demonstrated linear pharmacokinetic behavior over the dose ranges of 0.4 to 16.5 mg/kg intravenously and 0.8 to 10.2 mg/kg orally. Bioavailability of didanosine when administered as a solution with an antacid was approximately 43% for doses from 0.8 to 10.2 mg/kg in patients with AIDS and advanced AIDS-related complex[3]. In the target cell for HIV, didanosine is converted to its active moiety, dideoxyadenosine-5'-triphosphate (ddATP), which inhibits HIV reverse transcriptase and terminates viral DNA growth. Didanosine is an effective and generally well tolerated drug in previously untreated and antiretroviral therapy-experienced patients with HIV infection[4]. Didanosine (100 mg/kg/day) induced a loss of mtDNA (to 48% of the control level) similar to that induced by fosalvudine tidoxil[5]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00000924 | HIV Infections | Phase 2 | Completed | - | - |
NCT00618176 | HIV Infections | Phase 4 | Completed | - | China ... 展开 >> Peking Union Medical College Hospital Beijing, China, 100730 收起 << |
NCT00214435 | HIV Infection ... 展开 >> AIDS 收起 << | Phase 4 | Unknown | - | Australia, New South Wales ... 展开 >> 407 Doctors Recruiting Sydney, New South Wales, Australia, 2010 Contact: David A Baker, MB ChB 02 9332 2531 db@407.com.au Principal Investigator: David A Baker, MB ChB 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.23mL 0.85mL 0.42mL |
21.17mL 4.23mL 2.12mL |
42.33mL 8.47mL 4.23mL |
CAS号 | 69655-05-6 |
分子式 | C10H12N4O3 |
分子量 | 236.227 |
别名 | 地达诺辛;去羟肌苷;2',3'-二脱氧肌苷 ;Didanosine;ddI;Videx EC;Videx;DIDEOXYINOSINE;69655-05-6;NSC 612049;2′,3′-Dideoxyinosine;ddl |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
DMSO: 60 mg/mL(253.99 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |