产品说明书

Ritonavir

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Chemical Structure| 155213-67-5 同义名 : ABT 538;RTV;538, ABT;Norvir Sec;Norvir;NSC 693184;A-84538
CAS号 : 155213-67-5
货号 : A547820
分子式 : C37H48N6O5S2
纯度 : 98%
分子量 : 720.944
MDL号 : MFCD00927142
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(34.68 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
靶点

  • HIV Protease
描述 Ritonavir is n antiretroviral medication used along with other medications to treat HIV/AIDS. It is now rarely used for its own antiviral activity, but remains widely used as a booster of other protease inhibitors. More specifically, ritonavir is used to inhibit a particular liver enzyme that normally metabolizes protease inhibitors, cytochrome P450-3A4 (CYP3A4) [3]. The HIV-1 protease inhibitor ritonavir undergoes cytochrome P450-mediated biotransformation in human liver microsomes to three major metabolites, Ml, M2 and M11, with wide interindividual variation in the rates of metabolite formation. Ritonavir was found to be a potent inhibitor of CYP3A-mediated biotransformations. Ritonavir was also found to be an inhibitor of the reactions mediated by CYP2D6 (IC50 = 2.5 microM) and CYP2C9/10 (IC50 = 8.0 microM) [4].
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
NCT00775606 - Terminated(Study stopped 12/20... 展开 >>10 due to poor enrollment. Only 15 of 60 needed enrolled.) 收起 << - -
NCT01346982 HIV Phase 4 Completed - Spain ... 展开 >> Lluita contra la Sida Foundation, HIV Unit Badalona, Barcelona, Spain, 08916 收起 <<
NCT00744887 HIV AIDS Phase 1 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.39mL

0.28mL

0.14mL

6.94mL

1.39mL

0.69mL

13.87mL

2.77mL

1.39mL
参考文献

[1]Eagling VA, Back DJ, et al. Differential inhibition of cytochrome P450 isoforms by the protease inhibitors, ritonavir, saquinavir and indinavir. Br J Clin Pharmacol. 1997 Aug;44(2):190-4.

[2]Kumar GN, Rodrigues AD, et al. Cytochrome P450-mediated metabolism of the HIV-1 protease inhibitor ritonavir (ABT-538) in human liver microsomes. J Pharmacol Exp Ther. 1996 Apr;277(1):423-31.

[3]Zeldin RK, Petruschke RA. Pharmacological and therapeutic properties of ritonavir-boosted protease inhibitor therapy in HIV-infected patients. J Antimicrob Chemother. 2004 Jan;53(1):4-9. doi: 10.1093/jac/dkh029. Epub 2003 Dec 4. PMID: 14657084.

[4] Kumar GN, Rodrigues AD, Buko AM, Denissen JF. Cytochrome P450-mediated metabolism of the HIV-1 protease inhibitor ritonavir (ABT-538) in human liver microsomes. J Pharmacol Exp Ther. 1996 Apr;277(1):423-31. Erratum in: J Pharmacol Exp Ther 1997 Jun;281(3):1506. PMID: 8613951.