NVR 3-778

NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity.

Product information

CAS Number: 1445790-55-5

Molecular Weight: 432.39

Formula: C18H16F4N2O4S

Chemical Name: 4-fluoro-3-[(4-hydroxypiperidin-1-yl)sulfonyl]-N-(3,4,5-trifluorophenyl)benzamide

Smiles: OC1CCN(CC1)S(=O)(=O)C1=CC(=CC=C1F)C(=O)NC1=CC(F)=C(F)C(F)=C1

InChiKey: KKMFSVNFPUPGCA-UHFFFAOYSA-N

InChi: InChI=1S/C18H16F4N2O4S/c19-13-2-1-10(18(26)23-11-8-14(20)17(22)15(21)9-11)7-16(13)29(27,28)24-5-3-12(25)4-6-24/h1-2,7-9,12,25H,3-6H2,(H,23,26)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO: 10 mM

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:

NVR 3-778 targets HBV core protein and inhibits viral replication. NVR 3-778 inhibits the generation of infectious HBV DNA-containing virus particles with a mean antiviral with an EC50 of 0.40 µM in HepG2.2.15 cells. NVR 3-778 exhibits pan-genotypic antiviral activity and a lack of cross-resistance with nucleos(t)ide inhibitors of HBV replication. NVR 3-778 inhibits pregenomic RNA encapsidation, viral replication, and the production of HBV DNA- and HBV RNA-containing particles. NVR 3-778 also inhibits de novo infection and viral replication in primary human hepatocytes with EC50s of 0.81 µM against HBV DNA and between 3.7µM and 4.8 µM against the production of HBV antigens and intracellular HBV RNA. The EC50 values of NVR 3-778 are increased by 4.5-, 9.3-, and 15.8-fold in the presence of 10%, 20%, and 40% human serum, respectively.

In Vivo:

NVR 3-778 (1.5 mg/kg; i.g.) displays the mean Cmax and AUC0–inf values of 0.56 µg/ml and 3.50 µg·h/ml, respectively, in dogs following oral administration. And the mean oral bioavailability is determined to be 84.6%.

References:

1. Lam AM, et al. Preclinical Characterization of NVR 3-778, a First-in-Class Capsid Assembly Modulator against Hepatitis B Virus. Antimicrob Agents Chemother. 2018 Dec 21;63(1).

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