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2',3'-Dideoxyinosine

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Chemical Structure| 69655-05-6 同义名 : 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
CAS号 : 69655-05-6
货号 : A259943
分子式 : C10H12N4O3
纯度 : 98%
分子量 : 236.227
MDL号 : MFCD00077728
存储条件:

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

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:
生物活性
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].
临床研究
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 <<
实验方案
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

参考文献

[1]Perry CM, Noble S. Didanosine: an updated review of its use in HIV infection. Drugs. 1999 Dec;58(6):1099-135.

[2]Benbrik E, Chariot P, et al. Cellular and mitochondrial toxicity of zidovudine (AZT), didanosine (ddI) and zalcitabine (ddC) on cultured human muscle cells. J Neurol Sci. 1997 Jul;149(1):19-25.

[3]Knupp CA, Shyu WC, Dolin R, Valentine FT, McLaren C, Martin RR, Pittman KA, Barbhaiya RH. Pharmacokinetics of didanosine in patients with acquired immunodeficiency syndrome or acquired immunodeficiency syndrome-related complex. Clin Pharmacol Ther. 1991 May;49(5):523-35

[4]Perry CM, Noble S. Didanosine: an updated review of its use in HIV infection. Drugs. 1999 Dec;58(6):1099-135

[5]Venhoff AC, Lebrecht D, Reuss FU, Heckl-Ostreicher B, Wehr R, Walker UA, Venhoff N. Mitochondrial DNA depletion in rat liver induced by fosalvudine tidoxil, a novel nucleoside reverse transcriptase inhibitor prodrug. Antimicrob Agents Chemother. 2009 Jul;53(7):2748-51