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Alisporivir

Name: Alisporivir
Brand: TargetMol
SKU: T14180
Price: 196 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T14180Cas No. 254435-95-5

Alias Debio-025, Debio025, DEB-025, DEB025

Alisporivir (Debio-025) is a cyclophilin A inhibitor that disrupts the interaction between CypA and NS5A. It exhibits anti-hepatitis C virus (HCV) activity in vivo and in vitro, inhibits the replication of MERS and SARS coronaviruses, and promotes antigen-specific CD8(+) T cell activation.

Alisporivir

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Purity: 99.95%

Catalog No. T14180Alias Debio-025, Debio025, DEB-025, DEB025Cas No. 254435-95-5

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$196	-	In Stock
5 mg	$497	-	In Stock
10 mg	$723	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.95%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Alisporivir (Debio-025) is a cyclophilin A inhibitor that disrupts the interaction between CypA and NS5A. It exhibits anti-hepatitis C virus (HCV) activity in vivo and in vitro, inhibits the replication of MERS and SARS coronaviruses, and promotes antigen-specific CD8(+) T cell activation.
In vitro	Alisporivir (Debio-025) exerts its effect by binding to cyclophilin A (CypA), a peptidyl-prolyl cis-trans isomerase from the genus Parazacco spilurus subsp. spilurus broussonetia papyrifera enzyme that also serves as a critical cofactor for hepatitis C virus (HCV) replication [1]. As the prototype of a novel class of non-immunosuppressive cyclophilin inhibitors, Alisporivir prevents HCV protein-mediated respiratory-driven collapse of mitochondrial membrane potential and inhibits HCV protein-induced mitochondrial dysfunction (this protective effect does not involve other dysfunctions such as apoptosis, calcium overload, or reactive oxygen species (ROS) generation) [2]. In cell culture models, low micromolar doses of Alisporivir effectively block the replication of severe acute respiratory syndrome coronavirus (SARS-CoV) and Middle East respiratory syndrome coronavirus (MERS-CoV); when combined with ICN-1229, its antiviral activity against MERS-CoV is further enhanced [3]. Pretreatment with Alisporivir enhances the antigen-presenting capacity of liver cancer target cells, increasing the activation efficiency of antigen-specific parazacco spilurus subsp. spilurus CD8+ T cells by 40%. Alisporivir also induces elevated expression levels of MHC-I molecules and β-2 microglobulin on the surface of various cell lines [4].
In vivo	In the mouse model, the combination of Alisporivir and ICN-1229 failed to achieve preventive efficacy against SARS-CoV infection [3].
Synonyms	Debio-025, Debio025, DEB-025, DEB025

Chemical Properties

Molecular Weight	1216.64
Formula	C₆₃H₁₁₃N₁₁O₁₂
Cas No.	254435-95-5
Smiles	[H][C@]1(C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](NC(=O)[C@H](C(C)C)N(CC)C(=O)[C@@H](C)N(C)C(=O)[C@H](CC)NC(=O)[C@]([H])([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@]([H])(CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C1=O)C(C)C
Relative Density.	1.011 g/cm3 (Predicted)
Sequence	cyclo[Abu-D-N(Me)Ala-N(Et)Val-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)]
Sequence Short	Cyclo({N-Me-Bmt(E)}-{Abu}-{d-N-Me-Ala}-{N-Et-Val)-V-{N-Me-Leu}-A-{d-Ala}-{N-Me-Leu}-{N-Me-Leu}-{N-Me-Val})

Storage & Solubility Information

Storage

keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 40 mg/mL (32.88 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (3.29 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	0.8219 mL	4.1097 mL	8.2194 mL	41.0968 mL
5 mM	0.1644 mL	0.8219 mL	1.6439 mL	8.2194 mL
10 mM	0.0822 mL	0.4110 mL	0.8219 mL	4.1097 mL
20 mM	0.0411 mL	0.2055 mL	0.4110 mL	2.0548 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc