Alisporivir (Synonyms: Debio-025; DEB-025)

Name: Alisporivir
Brand: MedChemExpress
SKU: HY-12559
Rating: 5.0 (14 reviews)

Cat. No.: HY-12559 Purity: 98.85%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

Alisporivir Chemical Structure

CAS No. : 254435-95-5

Size	Price	Stock	Quantity
1 mg	USD 700	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 1400	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 2000	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 3650	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 5480	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 8200	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 14 publication(s) in Google Scholar

14 Publications Citing Use of MCE Alisporivir

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View All Cyclophilin Isoform Specific Products:

View All Isoforms

Cyclophilin A Cyclophilin B Cyclophilin C Cyclophilin D Cyclophilin G Cyclophilin E

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

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]
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]
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]
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]
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]

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

Molecular Weight

1216.64

Formula

C₆₃H₁₁₃N₁₁O₁₂

CAS No.

254435-95-5

Appearance

Solid

Color

White to off-white

SMILES

O[C@@H]([C@](C(N[C@H](C(N([C@@H](C(N([C@H](C(N[C@H](C(N([C@H]1CC(C)C)C)=O)C(C)C)=O)C(C)C)CC)=O)C)C)=O)CC)=O)([H])N(C([C@@H](N(C([C@](N(C([C@@H](N(C([C@@](NC([C@@H](NC1=O)C)=O)([H])C)=O)C)CC(C)C)=O)C)([H])CC(C)C)=O)C)C(C)C)=O)C)[C@H](C)C/C=C/C

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)

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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 (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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.85%

Select Batch:

Data Sheet (279 KB) SDS (252 KB)

COA (253 KB) LCMS (257 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]

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].

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

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]

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

Alisporivir Related Classifications

Infection

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.

Keywords:

Alisporivir254435-95-5Debio-025 DEB-025Debio025Debio 025DEB025DEB 025DEB-025CyclophilinHCVHepatitis C virusInhibitorinhibitorinhibit

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Alisporivir (Synonyms: Debio-025; DEB-025)

Customer Review

Alisporivir Related Antibodies

14 Publications Citing Use of MCE Alisporivir

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

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View All Cyclophilin Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Alisporivir Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Alisporivir Related Classifications

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