Indinavir
(Synonyms: 茚地那韦; MK-639 free base; L-735524 free base) 目录号 : GC36309
Indinavir sulfate (Crixivan, L-735524, MK-639) is a specific and potent inhibitor of HIV-1 protease and is widely used in the treatment of AIDS.
Cas No.:150378-17-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Indinavir sulfate (Crixivan, L-735524, MK-639) is a specific and potent inhibitor of HIV-1 protease and is widely used in the treatment of AIDS.
| Cas No. | 150378-17-9 | SDF | |
| 别名 | 茚地那韦; MK-639 free base; L-735524 free base | ||
| Canonical SMILES | O=C([C@@H](C[C@H](O)CN(CCN(CC1=CN=CC=C1)C2)[C@@H]2C(NC(C)(C)C)=O)CC3=CC=CC=C3)N[C@H]4C(C=CC=C5)=C5C[C@H]4O | ||
| 分子式 | C36H47N5O4 | 分子量 | 613.79 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6292 mL | 8.1461 mL | 16.2922 mL |
| 5 mM | 0.3258 mL | 1.6292 mL | 3.2584 mL |
| 10 mM | 0.1629 mL | 0.8146 mL | 1.6292 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Indinavir urolithiasis
Curr Opin Urol 2000 Nov;10(6):557-61.PMID:11148725DOI:10.1097/00042307-200011000-00004.
Indinavir sulfate is a protease inhibitor that has been found to be extremely effective in increasing CD4+ cell counts and in decreasing HIV-RNA titers in patients with HIV and AIDS. However, patients receiving Indinavir also have been noted to have a significant risk for developing urolithiasis. Published reports of Indinavir urolithiasis estimate its incidence at between 4 and 13%. Indinavir has a high urinary excretion with poor solubility in a physiologic pH solution. Consequently, patients develop urinary stones that are principally composed of Indinavir or of a mixture of Indinavir and other substances, such as calcium oxalate. Similar to other forms of urolithiasis, acute flank pain and hematuria are the typical symptoms of Indinavir urolithiasis. Indinavir urolithiasis is unique in that computed tomography, which was once thought to be efficacious in identifying all urinary calculi, is not useful in imaging stones that are composed of pure Indinavir. Indinavir urolithiasis generally responds to a conservative regimen of hydration, pain control, and the temporary discontinuation of the medication. Only a minority of patients need surgical intervention. Approximately 10% of patients ultimately need to discontinue Indinavir therapy altogether. Indinavir is an antiviral agent that has a significant role in the treatment of AIDS. Although urolithiasis is a significant side effect of Indinavir use, limiting its clinical application is not the answer. Rather, physicians need to know more about Indinavir urolithiasis to help their patients cope with its potential complications.
Indinavir: a review of its use in the management of HIV infection
Drugs 1999 Dec;58(6):1165-203.PMID:10651394DOI:10.2165/00003495-199958060-00011.
Indinavir is a protease inhibitor used in the treatment of patients with HIV infection. Combination antiretroviral therapy with Indinavir plus 2 nucleoside reverse transcriptase inhibitors (NRTIs) is associated with greater reductions in viral load, greater increases in CD4+ cell counts, and reduced morbidity and mortality when compared with 2 NRTIs alone. In the landmark clinical trial ACTG 320, the rate of progression to AIDS or death (primary end-point) among zidovudine-experienced patients treated with Indinavir, zidovudine and lamivudine was approximately half that of patients who received only zidovudine plus lamivudine (6 vs 11%; p < 0.001). The durability of an indinavir-containing regimen was demonstrated in Merck protocol 035, an ongoing trial in which a significant proportion of patients had sustained viral suppression for up to 3 years. Merck protocol 039, also an ongoing trial, showed a greater effect on surrogate markers of HIV disease progression with indinavir-based triple therapy than with zidovudine plus lamivudine or Indinavir monotherapy in patients with advanced disease (median baseline CD4+ count 15 cells/microL). Numerous additional clinical trials have established the beneficial antiviral and immunological effects of Indinavir in both antiretroviral-naive and -experienced patients with HIV infection. Indinavir is associated with various drug class-related adverse events, including gastrointestinal disturbances (e.g. nausea, diarrhoea), headache and asthenia/fatigue. A lipodystrophy syndrome has been commonly reported with Indinavir and other protease inhibitors combined with NRTIs, but it has also been reported in many protease inhibitor-naive patients, and a definitive causal link has not been established between the syndrome and protease inhibitors. Nephrolithiasis may develop in about 9% of patients receiving Indinavir but does not appear to be associated with other protease inhibitors; <0.5% of patients receiving Indinavir discontinue the drug because of nephrolithiasis, which may be the extreme end of a continuum of crystal-related renal syndromes. Additional renal problems (e.g. nephropathy) have been reported in small numbers of patients receiving Indinavir. In summary, Indinavir is a protease inhibitor with well documented efficacy when used as part of combined therapy in patients with HIV infection. Both US and UK treatment guidelines continue to recommend protease inhibitor-based regimens including Indinavir as a first-line option. Indinavir is being studied as a twice daily and once daily regimen with a low dosage of ritonavir as a way to alleviate tolerability, drug interaction and patient compliance/adherence issues. Indinavir-containing triple therapy has demonstrated positive effects not only on surrogate markers of disease progression, but also on clinical end-points of mortality and morbidity in patients with HIV disease. Protease inhibitors are a significant advance in the care of patients with HIV infection, and, in an era of evidence-based medicine, Indinavir represents an important component of antiretroviral treatment strategies.
Indinavir: the forgotten HIV-protease inhibitor. Does it still have a role?
Expert Opin Pharmacother 2007 May;8(7):957-64.PMID:17472541DOI:10.1517/14656566.8.7.957.
Indinavir is one of four first-generation HIV-protease inhibitors and was the most popular amongst them in the late 1990s. It was initially licensed for use alone, given three times daily, administered away from meals and together with at least 1.5 litres of fluid per day. In clinical practice, it became common for clinicians to prescribe it with a ritonavir pharmacokinetic 'boost' to remove the food restriction, reduce the pill burden and enable a more convenient twice-daily dosing schedule. However, at a ritonavir-boosted dosing schedule of Indinavir/ritonavir 800/100 mg b.i.d., the regimen proved toxic and poorly tolerable, and its use diminished as newer, better tolerated PIs became available. Recent research has suggested that ritonavir-boosted Indinavir administered at lower doses, particularly Indinavir/ritonavir 400/100 mg b.i.d., retains potency and is considerably less toxic. As a result, there is interest in its application in resource-constrained settings.
Indinavir/ritonavir remains an important component of HAART for the treatment of HIV/AIDS, particularly in resource-limited settings
Expert Opin Drug Metab Toxicol 2007 Jun;3(3):347-61.PMID:17539743DOI:10.1517/17425255.3.3.347.
For over a decade, Indinavir has been approved for the treatment of HIV/AIDS; however, following the introduction of new protease inhibitors (PIs) with improved safety and pharmacologic profiles, its use in developed countries has become almost obsolete. In contrast, in resource-limited settings where the majority of people living with HIV/AIDS reside, Indinavir is part of the most affordable PI-based highly active antiretroviral treatment regimen. A major drawback of Indinavir use is renal toxicity, but low-dose Indinavir plus ritonavir (400/100 mg) twice daily is both efficacious and tolerable. Similar low dosing levels in children have also proven successful, but data in pregnant women remains limited. Due to its low cost and proven efficacy Indinavir remains a key component of HIV/AIDS treatment in resource-limited settings.
Indinavir-induced nephropathy
Clin Nephrol 1999 Mar;51(3):181-3.PMID:10099891doi
We report the case of a 38-year-old male who developed renal insufficiency while on the protease inhibitor, Indinavir. This patient had an increase in serum creatinine over a period of approximately one year, along with persistently abnormal urinalysis. A renal biopsy was performed and showed marked tubular crystal deposition. The Indinavir was discontinued, and after two months the patient's serum creatinine and urinalysis returned to normal. To our knowledge this is the second case of Indinavir associated nephropathy.