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4-fluoro-3-((4-hydroxypiperidin-1-yl)sulfonyl)-N-(3,4,5-trifluorophenyl)benzamide

Product Name
4-fluoro-3-((4-hydroxypiperidin-1-yl)sulfonyl)-N-(3,4,5-trifluorophenyl)benzamide
CAS No.
1445790-55-5
Chemical Name
4-fluoro-3-((4-hydroxypiperidin-1-yl)sulfonyl)-N-(3,4,5-trifluorophenyl)benzamide
Synonyms
NVR 3-778 ，S6757;NVR 3-778, 10 mM in DMSO;4-fluoro-3-((4-hydroxypiperidin-1-yl)sulfonyl)-N-(3,4,5-trifluorophenyl)benzamide;Benzamide, 4-fluoro-3-[(4-hydroxy-1-piperidinyl)sulfonyl]-N-(3,4,5-trifluorophenyl)-;NVR 3-778,HBV,virus,assembly,CAM,modulator,inhibit,NVR 3 778,capsid,Hepatitis,chronic,Hepatitis B virus,Inhibitor,NVR 3778
CBNumber
CB43147159
Molecular Formula
C18H16F4N2O4S
Formula Weight
432.39
MOL File
1445790-55-5.mol
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4-fluoro-3-((4-hydroxypiperidin-1-yl)sulfonyl)-N-(3,4,5-trifluorophenyl)benzamide Property

solubility 
DMSO: Soluble: =10 mg/mL
Ethanol: Soluble: =10 mg/mL
form 
Solid
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0087065
Product name
NVR3-778
Purity
≥98.0%
Packaging
5mg
Price
$1100
Updated
2021/12/16
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4-fluoro-3-((4-hydroxypiperidin-1-yl)sulfonyl)-N-(3,4,5-trifluorophenyl)benzamide Chemical Properties,Usage,Production

Description

NVR 3-778 is the first capsid assembly modulator (CAM) that has demonstrated antiviral activity in hepatitis B virus (HBV)-infected patients. NVR 3-778 inhibited the generation of infectious HBV DNA-containing virus particles with a mean antiviral 50% effective concentration (EC50) of 0.40?μM in HepG2.2.15 cells. The antiviral profile of NVR 3-778 indicates pan-genotypic antiviral activity and a lack of cross-resistance with nucleos(t)ide inhibitors of HBV replication.

Uses

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[1].

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%[1].

Animal Model:Dogs[1]
Dosage:1.5?mg/kg (Pharmacokinetic Analysis)
Administration:Oral gavage
Result:The mean Cmax and AUC0–inf values are 0.56?μg/ml and 3.50?μg·h/ml and the oral bioavailability is 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). DOI:10.1128/AAC.01734-18
[2] KLAUS KLUMPP . Efficacy of NVR 3-778, Alone and In Combination With Pegylated Interferon, vs Entecavir In uPA/SCID Mice With Humanized Livers and HBV Infection[J]. Gastroenterology, 2018, 154 3: Pages 652-662.e8. DOI: 10.1053/j.gastro.2017.10.017

4-fluoro-3-((4-hydroxypiperidin-1-yl)sulfonyl)-N-(3,4,5-trifluorophenyl)benzamide Preparation Products And Raw materials

Raw materials

Preparation Products

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4-fluoro-3-((4-hydroxypiperidin-1-yl)sulfonyl)-N-(3,4,5-trifluorophenyl)benzamide Suppliers

China 36 United States 3 Global 39
Zhengzhou Alfachem Co., Ltd.
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1445790-55-5, 4-fluoro-3-((4-hydroxypiperidin-1-yl)sulfonyl)-N-(3,4,5-trifluorophenyl)benzamideRelated Search:


  • 4-fluoro-3-((4-hydroxypiperidin-1-yl)sulfonyl)-N-(3,4,5-trifluorophenyl)benzamide
  • Benzamide, 4-fluoro-3-[(4-hydroxy-1-piperidinyl)sulfonyl]-N-(3,4,5-trifluorophenyl)-
  • NVR 3-778,HBV,virus,assembly,CAM,modulator,inhibit,NVR 3 778,capsid,Hepatitis,chronic,Hepatitis B virus,Inhibitor,NVR 3778
  • NVR 3-778, 10 mM in DMSO
  • NVR 3-778 ，S6757
  • 1445790-55-5