1. Anti-infection
  2. HCV
  3. Alisporivir

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

Cat. No.: HY-12559 Purity: 98.67%
Handling Instructions

Alisporivir (DEB-025; 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

Alisporivir Chemical Structure

CAS No. : 254435-95-5

Size Price Stock Quantity
1 mg USD 960 In-stock
Estimated Time of Arrival: December 31
5 mg USD 3000 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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

In Vitro

DEB025 binds to CypA, a peptidyl-prolyl cis-trans isomerase which is a crucial cofactor for HCV replication[1]. Alisporivir (Debio-025) is an analogue of cyclosporine A and 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 ribavirin 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].

In Vivo

Combination treatment with alisporivir and ribavirin does not protect against SARS-CoV infection in a mouse model[3].

Clinical Trial
Molecular Weight

1216.64

Formula

C₆₃H₁₁₃N₁₁O₁₂

CAS No.

254435-95-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (82.19 mM)

*"≥" means soluble, but saturation unknown.

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

*All of the co-solvents are provided by MCE.
References
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. HCV protein expression in these cells is induced by withdrawal of tetracycline from the culture medium. The effect of tetracycline on the naive U2 OS cell line is tested measuring mitochondria-related respiration and reactive oxygen species (ROS) production, which remains unchanged[2].

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

References

Purity: 98.67%

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Alisporivir
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