Indinavir sulfate
(Synonyms: 硫酸茚地那韦; MK-639; L735524) 目录号 : GC36310
An HIV-
Cas No.:157810-81-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Indinavir is an HIV-1 protease inhibitor (Ki = 0.358 nM).1 It is selective for HIV-1 protease over HIV-2 protease (Ki = 3.316 nM), as well as human cathepsin D, porcine pepsin, bovine chymosin, human plasma renin, Factor Xa, and elastase at 10 μM. It is also selective for wild-type HIV-1 protease over the protease inhibitor-resistant mutants A-44, K-60, and V-18 (Kis = 0.24, 15, 50, and 40 nM, respectively).2 Indinavir is active against multiple HIV-1 variants in cell-based assays (IC95s = 12-100 nM).1 Formulations containing indinavir have been used in combination with antiretroviral agents in the treatment of HIV infection.
1.Vacca, J.P., Dorsey, B.D., Schleif, W.A., et al.L-735,524: An orally bioavailable human immunodeficiency virus type 1 protease inhibitorProc. Natl. Acad. Sci. USA91(9)4096-4100(1994) 2.Dorsey, B.D., McDonough, C., McDaniel, S.L., et al.Identification of MK-944a: A second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitorsJ. Med. Chem.43(18)3386-3399(2000)
| Cas No. | 157810-81-6 | SDF | |
| 别名 | 硫酸茚地那韦; MK-639; L735524 | ||
| 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.O=S(O)(O)=O | ||
| 分子式 | C36H49N5O8S | 分子量 | 711.87 |
| 溶解度 | DMSO: ≥ 100 mg/mL (140.48 mM); Water: 50 mg/mL (70.24 mM) | 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 | 1.4048 mL | 7.0238 mL | 14.0475 mL |
| 5 mM | 0.281 mL | 1.4048 mL | 2.8095 mL |
| 10 mM | 0.1405 mL | 0.7024 mL | 1.4048 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.
Desolvation behavior of Indinavir sulfate ethanol and follow-up by terahertz spectroscopy
Int J Pharm 2019 Aug 15;567:118446.PMID:31220565DOI:10.1016/j.ijpharm.2019.06.037.
Active pharmaceutical ingredients are composed of single-component or multicomponent crystals. Multicomponent crystals include salts, co-crystals, and solvates. Indinavir sulfate is the ethanol solvate form of indinavir that is known to deliquesce through moisture absorption. However, the detailed behavior of solvent molecules in the crystal has not been investigated. In this study, we studied the desolvation mechanism of Indinavir sulfate ethanol and investigated the behavior of solvent molecules in the solid from. Indinavir sulfate ethanol contained 1.7 molecules of ethanol, 0.7 of which desolvated at room temperature. They were originally two ethanol solvent molecules; one molecule of ethanol desolvated at room temperature, and the conformation of the remaining ethanol and t-butyl groups changed in conjunction with the removal of one ethanol molecule. Desolvation could hardly be detected by powder X-ray diffraction; however, it was detected using terahertz spectroscopy. Terahertz measurement of desolvation showed a high correlation with thermogravimetry data, suggesting that desolvation could be observed non-destructively using terahertz spectroscopy. We concluded that Indinavir sulfate 1 ethanol deliquesced at 60% relative humidity, and it turned into an amorphous solid after drying.
Indinavir sulfate renal toxicity in a pediatric hemophiliac with HIV infection
Ann Pharmacother 1997 Oct;31(10):1146-9.PMID:9337438DOI:10.1177/106002809703101005.
Objective: To report a case of renal toxicity associated with administration of Indinavir sulfate in a pediatric hemophiliac with HIV infection. Case summary: A 16-year-old white hemophiliac boy with HIV infection secondary to tainted coagulation factor VIII was treated with Indinavir sulfate. The patient developed gross hematuria, proteinuria, pyuria, abdominal pain, increased bilirubin, an elevated serum creatinine (SCr) of 1.2 mg/dL (baseline 0.9-1.0), and symptoms of renal colic within 1 month of starting Indinavir sulfate therapy. Approximately 2 months later the patient developed a low-grade fever with a further increase in SCr. He was prescribed a 10-day course of cefpodoxime proxetil for a possible urinary tract infection. One week later, the patient developed fever, chills, nausea, vomiting, decreased appetite, sterile pyuria, nasal congestion, and an elevated SCr of 1.3-1.7 mg/dL. Indinavir sulfate and cefpodoxime proxetil were discontinued and the patient was suspected of having tubulointerstitial nephritis secondary to Indinavir sulfate. The patient's nephritis resolved and the SCr decreased to 1.1 mg/dL within 1 month of discontinuing Indinavir sulfate. Conclusions: This case demonstrates the potential for renal toxicity with the use of Indinavir sulfate in HIV-infected hemophiliacs.
Solid-State Insight Into the Action of a Pharmaceutical Solvate: Structural, Thermal, and Dissolution Analysis of Indinavir sulfate Ethanolate
J Pharm Sci 2018 Oct;107(10):2731-2734.PMID:29960024DOI:10.1016/j.xphs.2018.06.020.
The crystal structure of Indinavir sulfate, a pharmaceutical administered as an ethanol solvate, is presented, revealing a unique channel/ionic solvate structure to be characteristic of the compound. The properties of the material with regard to thermal treatment and water adsorption follow closely from the structure. The in situ amorphization of the pharmaceutical upon contacting liquid water is observed and highlights the unique dissolution enhancement of marketing the crystalline solvate dosage. Through survey of published crystal structures, an ambiguous sulfate/bisulfate ionization state is also observed in the crystal, which challenges the general understanding of the pharmaceutical. This study provides a solid-state insight into the function of a special multicomponent crystalline pharmaceutical form.
Treatment of Indinavir sulfate induced urolithiasis in HIV-positive patients
Int Urol Nephrol 2002;34(1):13-5.PMID:12549631DOI:10.1023/a:1021340915465.
Indinavir sulfate is a protease inhibitor used of the treatment of primary HIV infection either as monotherapy or as part of antiretroviral treatment schemes. Approximately 10% of all patients develop urolithiasis with radiolucent stones consisting of indinavir. We present our results of the treatment in 11 HIV positive patients (9 men, 2 women), who developed Indinavir lithiasis after 5-8 months of antiretroviral therapy. Following the initial procedures (spasmoanalgetic drugs, ureteroscopy, double J-stent or nephrostomy), the patients were further treated by increasing diuresis and urinary acidification. All the patients responded well to the treatment, the obstruction was releieved and their renal function was restored to normal.