Cat. No.: HY-12559

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Alisporivir

(Synonyms: Debio-025; DEB-025)

17 Cited Publications

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Based on 17 publication(s) in Google Scholar

Alisporivir (Debio-025) is a cyclophilin inhibitor molecule with potent anti-hepatitis C virus (HCV) activity.

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

Purity: 99.03%
CAS No.: 254435-95-5
Formula: C₆₃H₁₁₃N₁₁O₁₂
Molecular Weight:1216.64

Storage:

Stored under nitrogen, away from moisture.

Powder -80°C, 2 years , -20°C, 1 year

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

Alisporivir Chemical Structure

CAS No.: 254435-95-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (17)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Alisporivir (Debio-025) is a cyclophilin inhibitor molecule with potent anti-hepatitis C virus (HCV) activity.

All Cyclophilin Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	CC₅₀	>20 μM Compound: ALISPORIVIR	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	3.1 μM Compound: ALISPORIVIR	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1
CHO	IC₅₀	0.8 μM Compound: 3	Inhibition of OATP1B1 (unknown origin) expressed in CHO cells using 8-fluorescein-cAMP substrate by fluorescent photometry Inhibition of OATP1B1 (unknown origin) expressed in CHO cells using 8-fluorescein-cAMP substrate by fluorescent photometry	[PMID: 25310383]
HEK293	IC₅₀	0.11 μM Compound: 3	Inhibition of BSEP (unknown origin) expressed in HEK293 cells using [3H]taurocholic acid substrate Inhibition of BSEP (unknown origin) expressed in HEK293 cells using [3H]taurocholic acid substrate	[PMID: 25310383]
HEK293	IC₅₀	0.18 μM Compound: 3	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using [3H]estradiol-17beta-glucuronide substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using [3H]estradiol-17beta-glucuronide substrate	[PMID: 25310383]
HEK293	IC₅₀	0.22 μM Compound: 3	Inhibition of OATP1B3 (unknown origin) expressed in HEK293 cells using [3H]estradiol-17beta-glucuronide substrate Inhibition of OATP1B3 (unknown origin) expressed in HEK293 cells using [3H]estradiol-17beta-glucuronide substrate	[PMID: 25310383]
HeLa	IC₅₀	>8.2 μM Compound: Debio-025	Antiviral activity against RSV infected in human HeLa cells assessed as inhibition of viral replication Antiviral activity against RSV infected in human HeLa cells assessed as inhibition of viral replication	[PMID: 18212100]
Huh-5-2	CC₅₀	>3 μM Compound: Debio-025	Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay	[PMID: 18625766]
Huh-5-2	EC₅₀	0.06 μM Compound: Debio-025	Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay	[PMID: 18625766]
Huh-7	EC₅₀	116 nM Compound: 3	Antiviral activity against HCV subtype 1b in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene in presence of 40% human serum Antiviral activity against HCV subtype 1b in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene in presence of 40% human serum	[PMID: 25310383]
Huh-7	EC₅₀	46 nM Compound: 3	Antiviral activity against HCV subtype 1b in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene Antiviral activity against HCV subtype 1b in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene	[PMID: 25310383]
Huh-7	EC₅₀	70 nM Compound: 3	Antiviral activity against HCV subtype 1a in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene Antiviral activity against HCV subtype 1a in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene	[PMID: 25310383]
MDCK	IC₅₀	>25 μM Compound: Debio-025	Antiviral activity against BVDV infected in MDCK cells assessed as inhibition of viral replication Antiviral activity against BVDV infected in MDCK cells assessed as inhibition of viral replication	[PMID: 18212100]
MDCK	IC₅₀	>9.9 μM Compound: Debio-025	Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of viral replication Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of viral replication	[PMID: 18212100]
MDCK	IC₅₀	>9.9 μM Compound: Debio-025	Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of viral replication Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of viral replication	[PMID: 18212100]
MDCK	IC₅₀	>9.9 μM Compound: Debio-025	Antiviral activity against influenza B virus infected in MDCK cells assessed as inhibition of viral replication Antiviral activity against influenza B virus infected in MDCK cells assessed as inhibition of viral replication	[PMID: 18212100]
MT4	CC₅₀	20 μM Compound: 3	Cytotoxicity against human MT4 cells by CDCF probe based assay Cytotoxicity against human MT4 cells by CDCF probe based assay	[PMID: 25310383]
MT4	EC₅₀	63 nM Compound: 7, [D-Ala]3[EtVal]4CsA	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 to 6 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 to 6 days by MTT assay	[PMID: 23849880]
MT4	IC₅₀	0.099 μM Compound: Debio-025	Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay	[PMID: 18212100]
PBMC	IC₅₀	0.5 μM Compound: 3	Cytotoxicity against PHA-stimulated human PBMC by 5-bromo-2'-deoxyuridine incorporation assay Cytotoxicity against PHA-stimulated human PBMC by 5-bromo-2'-deoxyuridine incorporation assay	[PMID: 25310383]
PBMC	IC₅₀	0.82 μM Compound: Debio-025	Antiproliferative activity against mouse PBMC with MLR assessed as inhibition of [3H]thymidine incorporation after 18 hrs Antiproliferative activity against mouse PBMC with MLR assessed as inhibition of [3H]thymidine incorporation after 18 hrs	[PMID: 18212100]
PBMC	IC₅₀	840 nM Compound: Alisporivir, DEBIO-025	Immunosuppressive activity in human PBMC isolated from two individuals assessed as inhibition of proliferation using [3H]thymidine by mixed lymphocyte reaction assay Immunosuppressive activity in human PBMC isolated from two individuals assessed as inhibition of proliferation using [3H]thymidine by mixed lymphocyte reaction assay	10.1039/C1MD00227A
Sf9	IC₅₀	18 μM Compound: 3	Inhibition of human MRP2 expressed in Sf9 cells inside out vesicles using CDCF substrate Inhibition of human MRP2 expressed in Sf9 cells inside out vesicles using CDCF substrate	[PMID: 25310383]
Vero	IC₅₀	>16.6 μM Compound: Debio-025	Antiviral activity against Yellow fever virus 17D infected in african green monkey Vero cells assessed as inhibition of viral replication Antiviral activity against Yellow fever virus 17D infected in african green monkey Vero cells assessed as inhibition of viral replication	[PMID: 18212100]
Vero	IC₅₀	>25 μM Compound: Debio-025	Antiviral activity against Coxsackie B3 infected in african green monkey Vero cells assessed as inhibition of viral replication Antiviral activity against Coxsackie B3 infected in african green monkey Vero cells assessed as inhibition of viral replication	[PMID: 18212100]
Vero	IC₅₀	>25 μM Compound: Debio-025	Antiviral activity against Parainfluenza 3 infected in african green monkey Vero cells assessed as inhibition of viral replication Antiviral activity against Parainfluenza 3 infected in african green monkey Vero cells assessed as inhibition of viral replication	[PMID: 18212100]
Vero	IC₅₀	7.7 μM Compound: Debio-025	Antiviral activity against SARS coronavirus infected in african green monkey Vero cells assessed as inhibition of viral replication Antiviral activity against SARS coronavirus infected in african green monkey Vero cells assessed as inhibition of viral replication	[PMID: 18212100]

In Vitro

DEB025 binds to CypA, a peptidyl-prolyl cis-trans isomerase which is a crucial cofactor for HCV replication^[1]. Alisporivir (Debio-025) represents the prototype of a new class of non-immunosuppressive cyclophilin inhibitors. Alisporivir prevents HCV protein-mediated collapse of the respiration-driven mitochondrial membrane potential. Alisporivir prevents HCV protein-mediated mitochondrial dysfunction outside the context of apoptosis, calcium overload, production of ROS, dysfunction^[2]. In cell culture models, low-micromolar doses of alisporivir block SARS-CoV and MERS-CoV replication. Combination treatment with Alisporivir and ICN-1229 increases the anti-MERS-CoV activity in cell culture^[3]. Alisporivir pretreatment stimulates antigen presentation by hepatoma target cells, leading to enhancement of antigen-specific CD8+ T cell activation by 40%. Alisporivir induces an increase of MHC-I and beta-2 microglobulin on the surface of several cell lines^[4].

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

In Vivo

Combination treatment with Alisporivir and ICN-1229 does not protect against SARS-CoV infection in a mouse model^[3].

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

Clinical Trial

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

Chemical Information

CAS No. 254435-95-5
Appearance Solid
Molecular Weight 1216.64
Formula C₆₃H₁₁₃N₁₁O₁₂
Color White to off-white
Synonyms

Debio-025; DEB-025
Sequence

Cyclo({N-Me-Bmt(E)}-{Abu}-{d-N-Me-Ala}-{N-Et-Val)-Val-{N-Me-Leu}-Ala-{d-Ala}-{N-Me-Leu}-{N-Me-Leu}-{N-Me-Val})
Sequence Shortening

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})
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Stored under nitrogen, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

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

Publications (17)

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Journal Impact Factor

Nat Aging

APOE4 accelerates advanced-stage vascular and neurodegenerative disorder in old Alzheimer's mice via cyclophilin A independently of amyloid-β. [Abstract]

2021 Jun;1(6):506-520. PMID: 35291561
Cell Death Differ

Ca2+-mediated mitochondrial inner membrane permeabilization induces cell death independently of Bax and Bak. [Abstract]

2022 Jul;29(7):1318-1334. PMID: 35726022
Cell Rep Med

A preclinical candidate of cyclophilin D inhibition improves alcohol-associated liver injury. [Abstract]

2026 Mar 17;7(3):102654. PMID: 41850244
J Exp Med

Endothelial LRP1 protects against neurodegeneration by blocking cyclophilin A. [Abstract]

2021 Apr 5;218(4):e20202207. PMID: 33533918
Cell Rep

Drug repurposing screens reveal cell-type-specific entry pathways and FDA-approved drugs active against SARS-Cov-2. [Abstract]

2021 Apr 6;35(1):108959. PMID: 33811811
Eur J Pharmacol

Inhibition of mPTP and GSDME-mediated pyroptosis alleviates lung injury in septic mice. [Abstract]

2026 May 13:178967. PMID: 42134760
Antimicrob Agents Chemother

Targeting Artemisinin-Resistant Malaria by Repurposing the Anti-Hepatitis C Virus Drug Alisporivir. [Abstract]

2022 Dec 20;66(12):e0039222. PMID: 36374050
iScience

BRCA1 mediates protein homeostasis through the ubiquitination of PERK and IRE1. [Abstract]

2022 Nov 19;25(12):105626. PMID: 36471805
Biomedicines

Effect of the Non-Immunosuppressive MPT Pore Inhibitor Alisporivir on the Functioning of Heart Mitochondria in Dystrophin-Deficient mdx Mice. [Abstract]

2021 Sep 16;9(9):1232. PMID: 34572419
Cell Signal

Cyclophilin A-FoxO1 signaling pathway in endothelial cell apoptosis. [Abstract]

2019 Sep:61:57-65. PMID: 31063815
J Cell Sci

Cyclophilin A regulates the apoptosis of A549 cells by stabilizing Twist1 protein. [Abstract]

2022 Jan 15;135(2):jcs259018. PMID: 34881782
Kidney360

CyclosporinA derivative as therapeutic candidate for Alport syndrome by inducing mutant type IV collagen secretion. [Abstract]

2023 Jul 1;4(7):909-917. PMID: 37143203
PLoS One

The combination of the NS5A and cyclophilin inhibitors results in an additive anti-HCV inhibition in humanized mice without development of resistance. [Abstract]

2021 May 20;16(5):e0251934. PMID: 34014993
Drug Metab Pharmacokinet

Comprehensive invitro evaluation of the inhibitory effects of relatively high molecular weight peptides on drug-drug interaction-associated four liver transporters and its association with physicochemical properties. [Abstract]

2025 Apr:61:101055. PMID: 40043642
Biochemistry (Mosc)

Alisporivir Normalizes Mitochondrial Function of Primary Mouse Lung Endothelial Cells Under Conditions of Hyperglycemia. [Abstract]

2022 Jul;87(7):605-616. PMID: 36154883
Bull Exp Biol Med

Effect of Alisporivir on Calcium Ion Transport and Mitophagy in Skeletal Muscle and Heart Mitochondria in Dystrophin-Deficient Mice. [Abstract]

2022 Apr;172(6):695-700. PMID: 35501648
bioRxiv

2021 Jan 9.

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (41.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

0.8219 mL

4.1097 mL

8.2194 mL

5 mM

0.1644 mL

0.8219 mL

1.6439 mL

10 mM

0.0822 mL

0.4110 mL

0.8219 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 (stored under nitrogen, 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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.62 mg/mL (2.15 mM); Clear solution

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (2.05 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.

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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[2]

Alisporivir is prepared in DMSO at 4 mM and diluted in cell culture medium at the indicated concentrations (0.1, 0.2, 0.3, 0.4, 0.5 μM). UHCV-32 and UHCVcon-57.3 are U-2 OS human osteosar coma-derived cell lines inducibly expressing the entire open reading frame derived from the HCV H77 prototype and consensus clones, respectively. Cell viability is measured by trypan blue exclusion analysis^[2].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 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)
Handling Instructions (2659 KB)

References

[1]. Coelmont L, et al. DEB025 (Alisporivir) inhibits hepatitis C virus replication by preventing a cyclophilin A induced cis-trans isomerisation in domain II of NS5A. PLoS One. 2010 Oct 27;5(10):e13687. [Content Brief]

[2]. Quarato G, et al. The cyclophilin inhibitor alisporivir prevents hepatitis C virus-mediated mitochondrial dysfunction. Hepatology. 2012 May;55(5):1333-43. [Content Brief]

[3]. de Wilde AH, et al. Alisporivir inhibits MERS- and SARS-coronavirus replication in cell culture, but not SARS-coronavirus infection in a mouse model. Virus Res. 2017 Jan 15;228:7-13. [Content Brief]

[4]. Esser-Nobis K, et al. The cyclophilin-inhibitor alisporivir stimulates antigen presentation thereby promoting antigen-specific CD8(+) T cell activation. J Hepatol. 2016 Jun;64(6):1305-14. [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
DMSO	1 mM	0.8219 mL	4.1097 mL	8.2194 mL	20.5484 mL
	5 mM	0.1644 mL	0.8219 mL	1.6439 mL	4.1097 mL
	10 mM	0.0822 mL	0.4110 mL	0.8219 mL	2.0548 mL
	15 mM	0.0548 mL	0.2740 mL	0.5480 mL	1.3699 mL
	20 mM	0.0411 mL	0.2055 mL	0.4110 mL	1.0274 mL
	25 mM	0.0329 mL	0.1644 mL	0.3288 mL	0.8219 mL
	30 mM	0.0274 mL	0.1370 mL	0.2740 mL	0.6849 mL
	40 mM	0.0205 mL	0.1027 mL	0.2055 mL	0.5137 mL

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Alisporivir

Macrocyclic Compound Library

Peptide Library

Cyclic Peptide Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Alisporivir

All Cyclophilin Isoforms

Biological Activity

Chemical Information

Publications (17)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Alisporivir

Macrocyclic Compound Library

Peptide Library

Cyclic Peptide Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Alisporivir

All Cyclophilin Isoforms

Biological Activity

Chemical Information

Publications (17)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Alisporivir Related Classifications

HY-12559 Related Classifications