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Biochem/physiol Actions
Orally active, potent and selective human cytomegalovirus DNA terminase complex inhibitor that interfers with HCMV DNA cleavage and packaging.
Letermovir (AIC246) is an orally active, potent and selective human cytomegalovirus (HCMV) DNA terminase complex inhibitor that blocks HCMV replication (EC50 = 0.9-3.1 nM among 17 clinial HCMV isolates; EC50 = 1.6-3.9 nM against 6 AD169-derived drug-resistant variants) by interfering with viral DNA cleavage/packaging. Letermovir exhibits little potency toward MCMV (Smith), RCMV (Maastricht), VZV (Oka), HSV-1 (166v VP22-GFP), HSV-2 (01-6332), HHV-6 (typeA-GS) or EBV (B95-8) (MCMV EC50 = 4.5 µM, all other EC50 >10 µM).
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | FC(F)(F)c1cc(c(cc1)OC)N2[C@H](c3c(c(ccc3)F)N=C2N4CCN(CC4)c5cc(ccc5)OC)CC(=O)O |
| InChI | 1S/C29H28F4N4O4/c1-40-20-6-3-5-19(16-20)35-11-13-36(14-12-35)28-34-27-21(7-4-8-22(27)30)23(17-26(38)39)37(28)24-15-18(29(31,32)33)9-10-25(24)41-2/h3-10,15-16,23H,11-14,17H2,1-2H3,(H,38,39)/t23-/m0/s1 |
| InChI key | FWYSMLBETOMXAG-QHCPKHFHSA-N |
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