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Firsocostat (GS-0976, ND-630)

Name: Firsocostat (GS-0976, ND-630)
Brand: Selleck Chemicals
SKU: S8893
Rating: 5 (5 reviews)

Synonyms: NDI-010976

Catalog No.S8893 Purity:99.97%

Firsocostat (GS-0976, ND-630) is a reversible inhibitor of acetyl CoA carboxylase (ACC) with IC50s of 2.1 nM,6.1 nM for hACC1 and hACC2,respectively.

Firsocostat (GS-0976, ND-630) Chemical Structure

CAS No. 1434635-54-7

Purity & Quality Control

Batch: S889301 DMSO]100 mg/mL]false]Ethanol]4 mg/mL]false]Water]Insoluble]false Purity: 99.97%

99.97

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Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
HepG2	Function assay		Inhibition of fatty acid synthesis in human HepG2 cells, IC50<0.1μM	25333641
VERO-E6	Toxicity assay	48 hrs	Toxicity CC50 against VERO-E6 cells determined at 48 hours by high content imaging (same conditions as 2_LEY without exposure to 0.01 MOI SARS CoV-2 virus), CC50=0.11μM	ChEMBL
VERO-E6	Function assay	48 hrs	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of VERO-E6 cells after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging, IC50=0.38μM	ChEMBL
Click to View More Cell Line Experimental Data

Biological Activity

Description

Firsocostat (GS-0976, ND-630) is a reversible inhibitor of acetyl CoA carboxylase (ACC) with IC50s of 2.1 nM,6.1 nM for hACC1 and hACC2,respectively.

Targets

hACC1 ^[1] (Cell-free assay)	hACC2 ^[1] (Cell-free assay)
2.1 nM	6.1 nM

In vitro
In vitro	When ND-630 and [¹⁴C]acetate were administered to Hep-G2 cells for 4 h, ND-630 inhibited FASyn with EC50 values of 66 nM in cells cultured in medium containing. When ND-630 and[¹⁴C]palmitate were administered to C2C12 cells for 6 h, ND-630 increased both the release of [¹⁴C]O₂ and the production of[¹⁴C]acid-soluble material.^[1]
Cell Research	Cell lines	HepG2 cells
	Concentrations	2.1 nM (ACC1); 6.1 nM (ACC2)
	Incubation Time	1 h
	Method	Cells were treated with varying concentrations of ND-630.

In Vivo
In vivo	When administered chronically to rats with diet-induced obesity, ND-630 reduces hepatic steatosis, improves insulin sensitivity, reduces weight gain without affecting food intake, and favorably affects dyslipidemia.^[1]
Animal Research	Animal Models	Male Sprague–Dawley rats
	Dosages	10 mg/kg
	Administration	o.g.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT02891408	Completed	Nonalcoholic Steatohepatitis (NASH)	Gilead Sciences	September 23 2016	Phase 1

References

[1] Harriman G,et al.Proc Natl Acad Sci U S A.2016 29;113(13):E1796-805.

Chemical Information & Solubility

Molecular Weight	569.63	Formula	C₂₈H₃₁N₃O₈S
CAS No.	1434635-54-7	SDF	--
Smiles	CC1=C(SC2=C1C(=O)N(C(=O)N2CC(C3=CC=CC=C3OC)OC4CCOCC4)C(C)(C)C(=O)O)C5=NC=CO5
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (175.55 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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