Home Metabolism Fatty Acid Synthase inhibitor Denifanstat (TVB-2640) For research use only.

Denifanstat (TVB-2640)

Synonyms: ASC-40, FASN-IN-2

Denifanstat (TVB-2640) is an orally bioavailable, pharmacological fatty acid synthase (FAS/FASN) inhibitor with therapeutic potential in patients with NAFLD and nonalcoholic steatohepatitis.

Denifanstat (TVB-2640) Chemical Structure

Denifanstat (TVB-2640) Chemical Structure

CAS No. 1399177-37-7

Purity & Quality Control

Denifanstat (TVB-2640) Related Products

Biological Activity

Description Denifanstat (TVB-2640) is an orally bioavailable, pharmacological fatty acid synthase (FAS/FASN) inhibitor with therapeutic potential in patients with NAFLD and nonalcoholic steatohepatitis.
Targets
FAS [1]
In vitro
In vitro

TVB-2640 markedly inhibits SARS-CoV-2 with EC50s of 4 nM. TVB-2640 could strikingly inhibit SARS-CoV-2 new variants with similar inhibitory effects on the early-lineage SARS-CoV-2 (USA-WA1/2020) virus.[2]
Cell Research Cell lines HEK293T-hACE2, Caco-2, MEF-hACE2 cells
Concentrations 100 nM for HEK293T-hACE2 cells; 2 µM for NCI-H1355, NCI-1437 and Caco-2 cells; 1 µM for MEF-hACE2 cells
Incubation Time 16+24 h
Method

Indicated cells were pre-treated with TVB-2640 from 16 h before infection and then infected with SARS-CoV-2-mNG. Fluorescence images were acquired at 48 hpi. Hoechst 33342 was used for nuclear staining. Assessment of anti-SARS-CoV-2 ability of FAS inhibitors in multiple cell lines. Indicated cells were pre-treated with TVB-2640 and infected with SARS-CoV-2 for 24 h, after infection cells were collected for quantification of intracellular viral RNA by qPCR.

(Data sourced from selleck products)
In Vivo
In vivo

TVB-2640 shows significant in vivo antiviral activity and protects SARS-CoV-2-infected mice for survival.[2]
Animal Research Animal Models K18-hACE2 transgenic mice infected by SARS-CoV-2
Dosages 8 mg kg-1 body weight
Administration i.p.

(Data sourced from selleck products)
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05743621 Recruiting
Prostatic Neoplasms Castration-Resistant
Weill Medical College of Cornell University|Sagimet Biosciences Inc.
 November 20 2023 Phase 1
NCT05835180 Completed
Non-alcoholic Steatohepatitis|Hepatic Impairment|Cirrhosis
Sagimet Biosciences Inc.
 May 1 2023 Phase 1
NCT05657834 Completed
Healthy Volunteers
Sagimet Biosciences Inc.
 November 21 2022 Phase 1
NCT04906421 Completed
Nonalcoholic Fatty Liver Disease
Sagimet Biosciences Inc.
 August 12 2021 Phase 2
NCT04843449 Completed
Healthy
Ascletis Pharmaceuticals Co. Ltd.
 April 4 2021 Phase 1
NCT04352361 Completed
Healthy
Ascletis Pharmaceuticals Co. Ltd.
 April 2 2020 Phase 1

Chemical Information & Solubility

Molecular Weight 439.55 Formula

C27H29N5O
CAS No. 1399177-37-7 SDF --
Smiles CC1=NN=C([NH]1)C2=C(C=C(C)C(=C2)C(=O)N3CCC(CC3)C4=CC=C(C=C4)C#N)C5CCC5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 88 mg/mL ( (200.2 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 88 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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