Firsocostat (GS-0976, ND-630)

Catalog No.S8893 Batch:S889301

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Technical Data

Formula

C28H31N3O8S
Molecular Weight 569.63 CAS No. 1434635-54-7
Solubility (25°C)* In vitro DMSO 100 mg/mL (175.55 mM)
Ethanol 4 mg/mL (7.02 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]
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)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    Male Sprague–Dawley rats

  • Dosages

    10 mg/kg

  • Administration

    o.g.

Selleck's Firsocostat (GS-0976, ND-630) has been cited by 5 publications

De novo lipogenesis fuels adipocyte autophagosome and lysosome membrane dynamics [ Nat Commun, 2023, 14(1):1362] PubMed: 36914626
Acetyl-CoA metabolism drives epigenome change and contributes to carcinogenesis risk in fatty liver disease [ Genome Med, 2022, 14(1):67] PubMed: 35739588
Macrophage acetyl-CoA carboxylase regulates acute inflammation through control of glucose and lipid metabolism [ Sci Adv, 2022, 8(47):eabq1984] PubMed: 36417534
LXRα activation and Raf inhibition trigger lethal lipotoxicity in liver cancer [ NAT CANCER, 2021, 2, 201–217] PubMed: None
Metabolic convergence on lipogenesis in RAS, BCR-ABL, and MYC-driven lymphoid malignancies [ Cancer Metab, 2021, 9(1):31] PubMed: 34399819

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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