1. Anti-infection Metabolic Enzyme/Protease Apoptosis
  2. HIV HIV Protease SARS-CoV Apoptosis MMP
  3. Indinavir sulfate

Indinavir sulfate  (Synonyms: MK-639; L735524)

Cat. No.: HY-B0689A Purity: 99.96%
COA Handling Instructions

Indinavir sulfate (MK-639) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate is also a SARS-CoV 3CLpro inhibitor.

For research use only. We do not sell to patients.

Indinavir sulfate Chemical Structure

Indinavir sulfate Chemical Structure

CAS No. : 157810-81-6

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
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100 mg USD 96 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Indinavir sulfate:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Indinavir sulfate (MK-639) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate is also a SARS-CoV 3CLpro inhibitor[1][2][3][4].

IC50 & Target

MMP-2

 

HIV-1

 

In Vitro

Indinavir sulfate (0-50 μM; 18 h) blocks lymphocyte cell cycle in G0/G1 phase in PBMCs cells and impairs lymphoproliferative responses[1].
Indinavir sulfate (40 μM-40 nM; 5 days) inhibits cell invasion and (40 μM-40 nM; 48 h) MMPs-2 activation of the Huh7 and SK-HEP-1 hepatocarcinoma cells in vitro[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: PBMCs (from healthy and HIV-infected volunteers)
Concentration: 0-50 µM
Incubation Time: 18 h (pretreatment; stimulation with anti-CD3 for an additional 48 hours)
Result: Blocked anti-CD3-induced cell-cycle progression in a dose-dependent manner.
Resulted in dose-dependent reduction of lymphoproliferative responses.

Cell Invasion Assay[2]

Cell Line: Huh7 and SK-HEP-1 cells
Concentration: 40 µM-40 nM
Incubation Time: 5 days
Result: Reduced ability to invade an in vitro constituted extracellular matrix for both cell lines treated compared with the untreated cells.

Western Blot Analysis[2]

Cell Line: Huh7 and SK-HEP-1 cells
Concentration: 40 µM-40 nM
Incubation Time: 48 h
Result: Blocked the conversion of latent MMP-2 to its 62/64-kDa active form.
In Vivo

Indinavir sulfate (70 mg/kg; i.g.; once a day for 3 weeks) inhibits the growth of hepatocarcinoma cells in vivo[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice(s.c. into Huh7 and SK-HEP-1 cells)[2].
Dosage: 70 mg/kg
Administration: Oral gavage; once a day for 3 weeks.
Result: Delaied the growth of s.c. implanted hepatocarcinoma xenografts in nude mice compared with placebo.
Clinical Trial
Molecular Weight

711.87

Formula

C36H49N5O8S

CAS No.
Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (140.48 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 50 mg/mL (70.24 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4048 mL 7.0238 mL 14.0475 mL
5 mM 0.2810 mL 1.4048 mL 2.8095 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.51 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (3.51 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (140.48 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.96%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.4048 mL 7.0238 mL 14.0475 mL 35.1188 mL
5 mM 0.2810 mL 1.4048 mL 2.8095 mL 7.0238 mL
10 mM 0.1405 mL 0.7024 mL 1.4048 mL 3.5119 mL
15 mM 0.0937 mL 0.4683 mL 0.9365 mL 2.3413 mL
20 mM 0.0702 mL 0.3512 mL 0.7024 mL 1.7559 mL
25 mM 0.0562 mL 0.2810 mL 0.5619 mL 1.4048 mL
30 mM 0.0468 mL 0.2341 mL 0.4683 mL 1.1706 mL
40 mM 0.0351 mL 0.1756 mL 0.3512 mL 0.8780 mL
50 mM 0.0281 mL 0.1405 mL 0.2810 mL 0.7024 mL
60 mM 0.0234 mL 0.1171 mL 0.2341 mL 0.5853 mL
DMSO 80 mM 0.0176 mL 0.0878 mL 0.1756 mL 0.4390 mL
100 mM 0.0140 mL 0.0702 mL 0.1405 mL 0.3512 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Indinavir sulfate
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