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Alisporivir

SKU: orb1707692

Description

Alisporivir (Debio-025) is a cyclophilin A inhibitor with broad-spectrum antiviral activity, effectively suppressing HCV, MERS-CoV, and SARS-CoV replication in vitro and in vivo. Its mechanism involves disrupting the CypA-NS5A interaction, and it has also been shown to enhance antigen-specific CD8+ T cell activation in immunological research.

Research Area

Infectious Disease & Virology, Protein Biochemistry

Images & Validation

Key Properties

CAS Number254435-95-5
MW1216.64
Purity99.95% (May vary between batches)
FormulaC63H113N11O12
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
TargetHCV Protease,SARS-CoV
SolubilityDMSO:40 mg/mL (32.88 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (3.29 mM)

Bioactivity

In Vivo
In the mouse model, the combination of Alisporivir and ICN-1229 failed to achieve preventive efficacy against SARS-CoV infection .
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 . 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) . 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 . 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 .

Storage & Handling

Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Alisporivir, Debio025, Debio-025, DEB 025, DEB025, DEB-025

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Key Properties

No computed properties available.

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Alisporivir (orb1707692)

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% DMSO +
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% Tween 80 +
%

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1 mg
¥ 3,120.00
5 mg
¥ 7,020.00
10 mg
¥ 10,010.00
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