Firsocostat

SKU: orb1300001

Description

Firsocostat (GS-0976) is a potent small molecule inhibitor of acetyl-CoA carboxylase (ACC) that disrupts dimerization, with IC50 values of 2.1 nM for ACC1 and 6.1 nM for ACC2. It is a valuable research tool for investigating lipid metabolism in non-alcoholic steatohepatitis (NASH) and metabolic disorders, with utility in both in vitro and preclinical in vivo models.

Research Area

Cell Biology

Key Properties

• CAS Number: 1434635-54-7
• MW: 569.6
• Purity: >98%
• Formula: C₂₈H₃₁N₃O₈S
• SMILES: COc1ccccc1[C@H](Cn1c2sc(c(C)c2c(=O)n(c1=O)C(C)(C)C(O)=O)-c1ncco1)OC1CCOCC1
• Target: Acetyl-CoA Carboxylase
• Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Bioactivity

• Target IC50:
  ACC2:6.1 nM|ACC1:2.1 nM
• In Vivo:
  ND-630 reduces hepatic steatosis in a rat model of diet-induced obesity and in Zucker diabetic rats. It also improves insulin secretion stimulated by glucose and reduces hemoglobin A1c levels by 0.9% in Zucker diabetic rats.
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• In Vitro:
  Firsocostat inhibited hACC1 with an IC50 of 2.1 ± 0.2 nM and hACC2 with an IC50 of 6.1 ± 0.8 nM .Inhibition was reversible and highly specific for ACC, as evidenced by the absence of an effect of Firsocostat on the activity of 101 enzymes, receptors, growth factors, transporters, and ion channels of the Ricerca DrugMatrix Panel at 10 μM .In addition, because the ACC dimerization site is not conserved among the mammalian carboxylases , Firsocostat lacks the ability to inhibit any of these mechanistically related enzymes and therefore exhibits absolute specificity for ACC inhibition relative to other mammalian carboxylases.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ND-630; NDI-010976; GS-0976

Compound Identifiers

PubChem CID

71528744