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NIM811

From Wikipedia, the free encyclopedia
NIM811
Names
Other names
N-Methyl-4-isoleucine cyclosporin
Identifiers
3D model (JSmol)
ChEMBL
UNII
  • CC[C@H]1C(=O)N(CC(=O)N([C@H](C(=O)N[C@H](C(=O)N([C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N1)[C@@H]([C@H](C)C\C=C\C)O)C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)[C@@H](C)CC)C)C
Properties
C62H111N11O12
Molar mass 1202.635 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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NIM811 is a mitochondrial permeability transition inhibitor. Also known as N-methyl-4-isoleucine cyclosporin, it is a substituted cyclosporine analog that binds to cyclophilin; however, this binary complex cannot bind to calcineurin, and therefore lacks immunosuppressive activity.

NIM811 is a form of treatment for patients with the hepatitis C virus (HCV). Studies indicate a strong relationship between a treatment's cyclophilin binding affinity and suppression of HCV activity.[1] NIM811 is also being studied as a potential treatment to genetic muscular diseases such as Ullrich congenital muscular dystrophy (UCMD) and Bethlem myopathy (BM) disease, diseases altering the genes for collagen VI production.[2]

References

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  1. ^ Ma, Sue; Boerner, Joanna E.; TiongYip, ChoiLai; Weidmann, Beat; Ryder, Neil S.; Cooreman, Michael P.; Lin, Kai (2006–2009). "NIM811, a Cyclophilin Inhibitor, Exhibits Potent In Vitro Activity against Hepatitis C Virus Alone or in Combination with Alpha Interferon". Antimicrobial Agents and Chemotherapy. 50 (9): 2976–2982. doi:10.1128/AAC.00310-06. ISSN 0066-4804. PMC 1563518. PMID 16940091.
  2. ^ Bernardi, Paolo; Argenton, Francesco; Bonaldo, Paolo; Braghetta, Paola; Sabatelli, Patrizia; Maraldi, Nadir Mario; Merlini, Luciano; Blaauw, Bert; Tagliavini, Francesca (2014-10-15). "NIM811, a cyclophilin inhibitor without immunosuppressive activity, is beneficial in collagen VI congenital muscular dystrophy models". Human Molecular Genetics. 23 (20): 5353–5363. doi:10.1093/hmg/ddu254. ISSN 0964-6906. PMID 24852368.