Cat. No.: HY-B0689A

Indinavir sulfate

(Synonyms: MK-639; L735524)

8 Cited Publications

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Based on 8 publication(s) in Google Scholar

Indinavir sulfate (MK-639) is an orally active and selective HIV-1 protease inhibitor with a K_i 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 3CL^pro inhibitor.

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Pureté: 99.97%
CAS No.: 157810-81-6
Formule: C₃₆H₄₉N₅O₈S
Masse moléculaire:711.87

Stockage:

-20°C, sealed storage, away from moisture

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

Indinavir sulfate Chemical Structure

CAS No.: 157810-81-6

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (8)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

MMP-2

HIV-1

Voir tous les produits spécifiques à Isoform HIV :

Voir tous les produits spécifiques à Isoform MMP :

Cellular Effect

Cell Line	Type	Value	Description	References
C8166	EC₅₀	8.18 nM Compound: indinavir sulfate	Inhibition of HIV1 LAI replication in C8166 cells after 4 days by ELISA Inhibition of HIV1 LAI replication in C8166 cells after 4 days by ELISA	[PMID: 18303847]
C8166	EC₅₀	5.5 nM Compound: indinavir sulfate	Antiviral activity against HIV1 LAI infected in human C8166 cells assessed as inhibition of viral replication by ELISA Antiviral activity against HIV1 LAI infected in human C8166 cells assessed as inhibition of viral replication by ELISA	[PMID: 18855443]
C8166	EC₅₀	8.81 nM Compound: indinavir sulfate	Antiviral activity against HIV1 replication in human C8166 cells by ELISA Antiviral activity against HIV1 replication in human C8166 cells by ELISA	[PMID: 19101157]
C8166	EC₅₀	8.71 nM Compound: indinavir sulfate	Antiviral activity against HIV-1 M:B_Lai replication in human C8166 cells assessed as inhibition of p24 antigen expression level after 4 days by ELISA Antiviral activity against HIV-1 M:B_Lai replication in human C8166 cells assessed as inhibition of p24 antigen expression level after 4 days by ELISA	[PMID: 19326880]
C8166	EC₅₀	0.0082 μM Compound: indinavir sulfate	Antiviral activity against HIV1 infected human C8166 cells assessed as inhibition of viral replication after 4 days by p24 antigen capture ELISA Antiviral activity against HIV1 infected human C8166 cells assessed as inhibition of viral replication after 4 days by p24 antigen capture ELISA	[PMID: 19618920]
CEM-SS	CC₅₀	>1 x 10^-4 M Compound: Indinavir sulfate	Cytotoxicity against human CEM-SS cells after 5 days by MTT assay Cytotoxicity against human CEM-SS cells after 5 days by MTT assay	[PMID: 17950955]
CEM-SS	IC₅₀	≤10 nM Compound: Indinavir sulfate	Antiviral activity against HIV1 LAI infected in human CEM-SS cells assessed as reverse transcriptase activity after 5 days by MTT assay Antiviral activity against HIV1 LAI infected in human CEM-SS cells assessed as reverse transcriptase activity after 5 days by MTT assay	[PMID: 17950955]
HepG2	EC₅₀	14.1 μM Compound: Idinavir Sulfate	Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis	[PMID: 20966043]
HepG2	EC₅₀	15.8 μM Compound: Idinavir Sulfate	Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis	[PMID: 20966043]
MT4	IC₅₀	22 nM Compound: Indinavir sulfate	Antiviral activity against HTLV1 3B infected in human MT4 cells assessed as reverse transcriptase activity after 5 days by MTT assay Antiviral activity against HTLV1 3B infected in human MT4 cells assessed as reverse transcriptase activity after 5 days by MTT assay	[PMID: 17950955]
MT4	CC₅₀	>1 x 10^-4 M Compound: Indinavir sulfate	Cytotoxicity against human MT4 cells after 4 days by MTT assay Cytotoxicity against human MT4 cells after 4 days by MTT assay	[PMID: 17950955]

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 157810-81-6
Appearance Solid
Masse moléculaire 711.87
Formule C₃₆H₄₉N₅O₈S
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
Synonyms

MK-639; L735524
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

-20°C, sealed storage, away from moisture

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

Publications (8)

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Journal Impact Factor

Signal Transduct Target Ther

Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. [Abstract]

2021 May 29;6(1):212. PMID: 34052830
Nat Commun

Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease. [Abstract]

2020 Sep 4;11(1):4417. PMID: 32887884
Front Pharmacol

Prediction of Synergistic Drug Combinations for Prostate Cancer by Transcriptomic and Network Characteristics. [Abstract]

2021 Apr 12;12:634097. PMID: 33986671
Int J Antimicrob Agents

Efficacy of antiretroviral compounds against Toxoplasma gondii in vitro. [Abstract]

2019 Dec;54(6):814-819. PMID: 31479744
Antiviral Res

HIV protease inhibitor attenuated astrocyte autophagy involvement in inflammation via p38 MAPK pathway. [Abstract]

2022 Dec:208:105463. PMID: 36372295
Antimicrob Agents Chemother

Discovery of M Protease Inhibitors Encoded by SARS-CoV-2. [Abstract]

2020 Aug 20;64(9):e00872-20. PMID: 32669265
Toxicol In Vitro

Evaluating variations in bilirubin glucuronidation activity by protease inhibitors in canine and human primary hepatocytes cultured in a 3D culture system. [Abstract]

2023 Dec:93:105689. PMID: 37660998
bioRxiv

2020 Apr.

Solvant et solubilité

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.4048 mL

7.0238 mL

14.0475 mL

5 mM

0.2810 mL

1.4048 mL

2.8095 mL

10 mM

0.1405 mL

0.7024 mL

1.4048 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 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) .

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Chavan S, et al. The HIV protease inhibitor Indinavir inhibits cell-cycle progression in vitro in lymphocytes of HIV-infected and uninfected individuals. Blood. 2001 Jul 15;98(2):383-9. [Content Brief]

[2]. Esposito V, et al. Evaluation of antitumoral properties of the protease inhibitor indinavir in a murine model of hepatocarcinoma. Clin Cancer Res. 2006 Apr 15;12(8):2634-9. [Content Brief]

[3]. Liu F, et al. Kinetic, stability, and structural changes in high-resolution crystal structures of HIV-1 protease with drug-resistant mutations L24I, I50V, and G73S. J Mol Biol. 2005 Dec 9;354(4):789-800. [Content Brief]

[4]. Hall DC Jr, et al. A search for medications to treat COVID-19 via in silico molecular docking models of the SARS-CoV-2 spike glycoprotein and 3CL protease. Travel Med Infect Dis. 2020 May-Jun;35:101646. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
DMSO	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.

Indinavir sulfate

8 Cited Publications

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Indinavir sulfate

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Publications Citing Use of MedChemExpress (MCE) Indinavir sulfate

Voir tous les produits spécifiques à Isoform HIV

Voir tous les produits spécifiques à Isoform MMP

Activité biologique

Chemical Information

Publications (8)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Indinavir sulfate Related Classifications

HY-B0689A Related Classifications