Firsocostat (GS-0976)

Catalog No.S8893 Synonyms: NDI-010976, ND-630

For research use only.

Firsocostat (GS-0976, NDI-010976, 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) Chemical Structure

CAS No. 1434635-54-7

Selleck's Firsocostat (GS-0976) has been cited by 3 Publications

Purity & Quality Control

Choose Selective Acetyl-CoA carboxylase Inhibitors

Biological Activity

Description Firsocostat (GS-0976, NDI-010976, 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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 MX;GeY5kfGmxbjDhd5NigQ>? MXTJcohq[mm2aX;uJI9nKG[jdIT5JIFkcWRic4nueIhme2m|IHnuJIh2dWGwIFjldGczKGOnbHzzMEBKSzVyPECuNe69VQ>? M4Prc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{OzOlQyLz5{NUOzN|Y1OTxxYU6=
VERO-E6 Mlf1WI95cWOrdImgZZN{[Xl? NY\2bG1yPDhiaILz M3ruXHRwgGmlaYT5JGNEPTBiYXfhbY5{fCCYRWLPMWU3KGOnbHzzJIRmfGW{bXnu[YQh[XRiNEigbI92enNiYomgbIlocCClb370[Y51KGmvYXfpcochMHOjbXWgZ49v\Gm2aX;ud{BieyB{X1zFXUB4cXSqb4X0JIV5eG:|dYLlJJRwKDBwMEGgUW9KKFODUmOgR49XNTJidnnyeZMqNCCFQ{WwQVAvOTIQvF2= NIHOdFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PDB5NUS3M{c,S2iHTVLMQE9iRg>?
VERO-E6 M4PFdWZ2dmO2aX;uJIF{e2G7 MX60PEBpenN? MoDvSIV1\XKvaX7heIlwdiCxZjDJR|UxKH[jbIXld{Bnd3JiaX7obYJqfGmxbjDv[kBUSVKVLVPvWk0zKGmwZIXj[YQh[3m2b4TvfIlkcXS7IH;mJHZGWk9vRU[gZ4VtdHNiYX\0[ZIhPDhiaH;1dpMhKGW6cH;zeZJmKHSxIECuNFEhVU:LIGPBVnMhS2:YLUKgeolzfXNiYomgbIlocCClb370[Y51KGmvYXfpcoctKEmFNUC9NE4{QM7:TR?= NHP3PZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PDB5NUS3M{c,S2iHTVLMQE9iRg>?
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]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 569.63
Formula

C28H31N3O8S

CAS No. 1434635-54-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(SC2=C1C(=O)N(C(=O)N2CC(C3=CC=CC=C3OC)OC4CCOCC4)C(C)(C)C(=O)O)C5=NC=CO5

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02891408 Completed Drug: Firsocostat|Drug: Fenofibrate Nonalcoholic Steatohepatitis (NASH) Gilead Sciences September 23 2016 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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