| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
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Purity: ≥98%
Alisporivir (Debio-025) is a novel and potent cyclophilin inhibitor molecule with anti-hepatitis C virus (HCV) activity. It is non-immunosuppressive cyclosporin that is a potent inhibitor of hepatitis C virus replication in vitro.
| ln Vitro |
CypA, a peptidyl-prolyl cis-trans isomerase and an essential cofactor for HCV replication, is bound by DEB025 [1]. The first member of a novel class of cyclophilin inhibitors that are not immunosuppressive is alisporivir (Debio-025). Alisporivir inhibits the collapse of mitochondrial membrane potential caused by respiration mediated by HCV protein. Together with apoptosis, calcium overload, ROS generation, and malfunction, alisporivir also inhibits HCV protein-mediated mitochondrial dysfunction [2]. Low micromolar dosages of alisporivir prevented SARS-CoV and MERS-CoV from replicating in cell culture experiments. In cell cultures, combination treatment with alisporivir and ICN-1229 boosts anti-MERS-CoV activity [3]. Pretreatment with alisporivir can increase target cells for liver cancer's antigen presentation by 40%, which in turn increases antigen-specific CD8+ T cell activation. On the surface of different cell lines, alisporivir can cause an increase in MHC-I and β-2 microglobulin [4].
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| ln Vivo |
In mouse models, alisporivir and ICN-1229 therapy in combination was ineffective in preventing SARS-CoV infection [3].
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| References |
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| Additional Infomation |
Alisporivir is a homodetic cyclic peptide. It has a role as an anticoronaviral agent.
Alisporivir has been used in trials studying the treatment of Hepatitis C and Chronic Hepatitis C. Alisporivir is a non-immunosuppressive analogue of cyclosporine A and an inhibitor of cyclophilins, with potential antiviral activity. Upon oral administration, alisporivir targets and inhibits human host cyclophilins, thereby inhibiting hepatitis C virus (HCV) replication in hepatocytes. Alisporivir may also inhibit the replication of various coronaviruses. In addition, it may inhibit mitochondrial cyclophilin-D, which regulates mitochondrial permeability transition pore (mPTP) opening. This may prevent cell death and tissue damage. Drug Indication Treatment of chronic hepatitis C |
| Exact Mass |
1215.857
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|---|---|
| CAS # |
254435-95-5
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| PubChem CID |
11513676
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| Appearance |
White to off-white solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
1294.2±65.0 °C at 760 mmHg
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| Flash Point |
736.5±34.3 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.467
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| LogP |
3.84
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
86
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| Complexity |
2360
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| Defined Atom Stereocenter Count |
13
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| SMILES |
O[C@H]([C@H](C)C/C=C/C)[C@H]1C(N[C@@H](CC)C(N(C)[C@H](C)C(N(CC)[C@H](C(N[C@H](C(N(C)[C@H](C(N[C@@H](C)C(N[C@H](C)C(N(C)[C@@H](CC(C)C)C(N(C)[C@H](C(N(C)[C@H](C(N1C)=O)C(C)C)=O)CC(C)C)=O)=O)=O)=O)CC(C)C)=O)C(C)C)=O)C(C)C)=O)=O)=O
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| InChi Key |
OLROWHGDTNFZBH-XEMWPYQTSA-N
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| InChi Code |
InChI=1S/C63H113N11O12/c1-26-29-30-40(16)52(75)51-56(79)66-44(27-2)59(82)68(20)43(19)58(81)74(28-3)49(38(12)13)55(78)67-48(37(10)11)62(85)69(21)45(31-34(4)5)54(77)64-41(17)53(76)65-42(18)57(80)70(22)46(32-35(6)7)60(83)71(23)47(33-36(8)9)61(84)72(24)50(39(14)15)63(86)73(51)25/h26,29,34-52,75H,27-28,30-33H2,1-25H3,(H,64,77)(H,65,76)(H,66,79)(H,67,78)/b29-26+/t40-,41+,42-,43-,44+,45+,46+,47+,48+,49+,50+,51+,52-/m1/s1
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| Chemical Name |
(3S,6S,9S,12R,15S,18S,21S,24S,27R,30S,33S)-25,30-diethyl-33-((1R,2R,E)-1-hydroxy-2-methylhex-4-en-1-yl)-6,9,18-triisobutyl-3,21,24-triisopropyl-1,4,7,10,12,15,19,27,28-nonamethyl-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2,5,8,11,14,17,20,23,26,29,32-undecaone
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| Synonyms |
Debio 025 Debio-025Debio025UNII-VBP9099AA6 UNIL 025 DEB025.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~82.19 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.62 mg/mL (2.15 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Long Term Follow-up Study to Assess Durability of Sustained Virologic Response in Alisporivir-treated Hepatitis C Patients
CTID: NCT02753699
Phase: Phase 3 Status: Completed
Date: 2016-08-26
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