1030825-28-5
Chemical Structure
OP-1118
Synonym(s): Fidaxomicin metabolite OP-1118
- CAS No.: 1030825-28-5
- Formula:C48H68Cl2O17
- Molecular Weight:987.95
IUPAC Name: (2S,3R,4R,5R,6S)-6-(((3E,5E,8S,9E,11S,12R,13E,15E,18S)-11-ethyl-8-hydroxy-18-((R)-1-hydroxyethyl)-9,13,15-trimethyl-2-oxo-12-(((2R,3S,4S,5S)-3,4,5-trihydroxy-6,6-dimethyltetrahydro-2H-pyran-2-yl)oxy)oxacyclooctadeca-3,5,9,13,15-pentaen-3-yl)methoxy)-4-hydroxy-5-methoxy-2-methyltetrahydro-2H-pyran-3-yl 3,5-dichloro-2-ethyl-4,6-dihydroxybenzoate
InChIKey: MWZWKUKATWMWGS-FXYIDGSOSA-N
SMILES: O=C(C(C(O)=C1Cl)=C(C(Cl)=C1O)CC)O[C@@H]([C@@H](O[C@@H]2OC/C(C(O[C@](C/C=C(/C=C([C@@H]3O[C@H](OC4(C)C)[C@H]([C@H]([C@@H]4O)O)O)\C)C)([H])[C@H](O)C)=O)=C\C=C\C[C@@H](/C(C)=C/[C@@H]3CC)O)C)[C@H]([C@H]2OC)O
Biological Activity: OP-1118 (Fidaxomicin metabolite OP-1118) is an orally active dual inhibitor of NF-κB and ERK1/2, with low systemic plasma exposure, no accumulation, and primary excretion via feces. By inhibiting the phosphorylation of NF-κB and ERK1/2 and reducing the expression of pro-inflammatory cytokines, OP-1118 exerts significant anti-inflammatory, cytoprotective, anti-apoptotic and antibacterial activities. In Clostridium difficile infection models, OP-1118 effectively blocks toxin-mediated intestinal inflammation, cell rounding, histological damage and apoptosis, and its protective effect can be reversed by PMA (HY-18739)[1][2][3].
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OP-1118 | OP-1118 (Fidaxomicin metabolite OP-1118) is an orally active dual inhibitor of NF-κB and ERK1/2, with low systemic plasma exposure, no accumulation, and primary excretion via feces. By inhibiting the phosphorylation of NF-κB and ERK1/2 and reducing the expression of pro-inflammatory cytokines, OP-1118 exerts significant anti-inflammatory, cytoprotective, anti-apoptotic and antibacterial activities. In Clostridium difficile infection models, OP-1118 effectively blocks toxin-mediated intestinal inflammation, cell rounding, histological damage and apoptosis, and its protective effect can be reversed by PMA (HY-18739). | |||||||||||||||||||||
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References
- [1]. Koon HW, et al. Fidaxomicin and OP-1118 Inhibit Clostridium difficile Toxin A- and B-Mediated Inflammatory Responses via Inhibition of NF-κB Activity. Antimicrob Agents Chemother. 2017;62(1):e01513-17. Published 2017 Dec 21. [Content Brief]
- [2]. Koon HW, et al. Fidaxomicin inhibits Clostridium difficile toxin A-mediated enteritis in the mouse ileum. Antimicrob Agents Chemother. 2014;58(8):4642-4650. [Content Brief]
- [3]. Guery B, et al. Pharmacokinetic analysis of an extended-pulsed fidaxomicin regimen for the treatment of Clostridioides (Clostridium) difficile infection in patients aged 60 years and older in the EXTEND randomized controlled trial[J]. Journal of Antimicrobial Chemotherapy, 2020, 75(4): 1014-1018.
