An inhibitor of PPIase A
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Alisporivir

Item No. 46121

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
Cyclo[L-alanyl-D-alanyl-N-methyl-L-leucyl-N-methyl-L-leucyl-N-methyl-L-valyl-(2S,3R,4R,6E)-3-hydroxy-4-methyl-2-(methylamino)-6-octenoyl-(2S)-2-aminobutanoyl-N-methyl-D-alanyl-N-ethyl-L-valyl-L-valyl-N-methyl-L-leucyl]
CAS Number
254435-95-5
Synonyms
  • DEB025
  • Debio-025
  • (D-MeAla3-EtVal4)cyclosporine
Molecular Formula
C63H113N11O12
Formula Weight
1216.7
Purity
≥95%
Formulation (Request formulation change)
A solid
SMILES
C/C=C/C[C@@H](C)[C@H]([C@]1([H])N(C([C@@H](N(C([C@@H](N(C([C@@H](N(C([C@H](NC([C@@H](NC([C@@H](N(C([C@@H](NC([C@@H](N(CC)C([C@H](N(C([C@@H](NC1=O)CC)=O)C)C)=O)C(C)C)=O)C(C)C)=O)C)CC(C)C)=O)C)=O)C)=O)C)CC(C)C)=O)C)CC(C)C)=O)C)C(C)C)=O)C)O
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
InChi Key
OLROWHGDTNFZBH-XEMWPYQTSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    Alisporivir is an inhibitor of peptidyl-prolyl cis-trans isomerase A (PPIase A; Ki = 0.34 nM), also known as cyclophilin A (CypA).1 It inhibits viral replication in HIV-1-infected MT-4 cells and isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 0.099 and 0.064 µM, respectively) but does not have immunosuppressive activity in the CD4+ T cell population in isolated human PBMCs. Alisporivir inhibits hepatitis C virus (HCV) replication in a cell-based replicon assay (EC50 = 0.08-0.27 µg/ml) and reduces serum viral titers and viral rebound in a humanized mouse model of HCV infection.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ptak, R.G., Gallay, P.A., Jochmans, D., et al. Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. Antimicrob. Agents Chemother. 52(4), 1302-1317 (2008).

    2. Paeshuyse, J., Kaul, A., De Clercq, E., et al. The non-immunosuppressive cyclosporin DEBIO-025 is a potent inhibitor of hepatitis C virus replication in vitro. Hepatology 43(4), 761-770 (2006).

    3. Bobardt, M., Ramirez, C.M., Baum, M.M., et al. The combination of the NS5A and cyclophilin inhibitors results in an additive anti-HCV inhibition in humanized mice without development of resistance. PLoS One 16(5), e0251934 (2021).