For research use only. Not for therapeutic Use.
ERDRP-0519, an orally bioavailable small-molecule Measles virus (MeV) polymerase inhibitor, prevents measles disease in squirrel monkeys (Saimiri sciureus). ERDRP-0519 inhibits morbilliviruses with nanomolar potency.[1][2][3].
ERDRP-0519 exhibits potency against a panel of Measles virus (MeV) isolates with EC50s of 0.07- 0.3 µM[1]. ERDRP-0519 exhibits potency against MeV and related pathogens of the Morbillivirus genus, such as canine distemper virus (CDV)[3].
A single-dose pharmacokinetic (PK) study is performed in squirrel monkeys by oral (intragastric) delivery of ERDRP-0519 (50 mg/kg) and blood sampling at seven predefined time points after dosing. Serum concentrations peak ~2 h post-administration (Cmax=3.27 µM)[3].
Catalog Number | I026977 |
CAS Number | 1374006-96-8 |
Synonyms | 2-methyl-N-[4-[(2S)-2-(2-morpholin-4-ylethyl)piperidin-1-yl]sulfonylphenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide |
Molecular Formula | C23H30F3N5O4S |
Purity | ≥95% |
InChI | InChI=1S/C23H30F3N5O4S/c1-29-20(16-21(28-29)23(24,25)26)22(32)27-17-5-7-19(8-6-17)36(33,34)31-10-3-2-4-18(31)9-11-30-12-14-35-15-13-30/h5-8,16,18H,2-4,9-15H2,1H3,(H,27,32)/t18-/m0/s1 |
InChIKey | JVZHTUQIMBYDSX-SFHVURJKSA-N |
SMILES | CN1C(=CC(=N1)C(F)(F)F)C(=O)NC2=CC=C(C=C2)S(=O)(=O)N3CCCCC3CCN4CCOCC4 |
Reference | [1]. Stefanie A Krumm, et al. An orally available, small-molecule polymerase inhibitor shows efficacy against a lethal morbillivirus infection in a large animal model. Sci Transl Med. 2014 Apr 16;6(232):232ra52. [2]. Richard K Plemper. Measles Resurgence and Drug Development. Curr Opin Virol. 2020 Apr;41:8-17. [3]. Kevin Wittwer, et al. Small-molecule polymerase inhibitor protects non-human primates from measles and reduces shedding. Nat Commun. 2021 Sep 2;12(1):5233. |