ERDRP-0519

ERDRP-0519 is an orally available polymerase inhibitor. It shows efficacy against a lethal morbillivirus infection in a large animal model. 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..

Product information

CAS Number: 1374006-96-8

Molecular Weight: 529.58

Formula: C23H30F3N5O4S

Chemical Name: 1-methyl-N-(4-{[(2S)-2-[2-(morpholin-4-yl)ethyl]piperidin-1-yl]sulfonyl}phenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide

Smiles: CN1N=C(C=C1C(=O)NC1C=CC(=CC=1)S(=O)(=O)N1CCCC[C@H]1CCN1CCOCC1)C(F)(F)F

InChiKey: JVZHTUQIMBYDSX-SFHVURJKSA-N

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

ERDRP-0519 exhibits potency against a panel of Measles virus (MeV) isolates with EC50s of 0.07- 0.3 µM. ERDRP-0519 exhibits potency against MeV and related pathogens of the Morbillivirus genus, such as canine distemper virus (CDV).

In Vivo:

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).

References:

1. Krumm SA, Yan D, Hovingh ES, Evers TJ, Enkirch T, Reddy GP, Sun A, Saindane MT, Arrendale RF, Painter G, Liotta DC, Natchus MG, von Messling V, Plemper RK. 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. doi: 10.1126/scitranslmed.3008517. PubMed PMID: 24739760; PubMed Central PMCID: PMC4080709.
2. Wittwer K, et al. Small-molecule polymerase inhibitor protects non-human primates from measles and reduces shedding. Nat Commun. 2021 Sep 2;12(1):5233.

Products are for research use only. Not for human use.