| Name | Firsocostat |
| Description | Firsocostat (GS-0976) is an inhibitor of acetyl-CoA carboxylase (ACC) dimerization that inhibits human ACC1 and ACC2 activity (IC50s of 2.1 and 6.1 nM, respectively) |
| 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. |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 31.25 mg/mL (54.86 mM), Sonication is recommended.
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| Keywords | NDI010976 | NDI 010976 | ND630 | ND 630 | Inhibitor | inhibit | GS0976 | GS 0976 | Firsocostat | AcetylCoACarboxylase | Acetyl-CoA Carboxylase | AcetylCoA Carboxylase | ACC, Acetyl Coenzyme A Carboxylase | ACC |
| Inhibitors Related | Alisol A | CMS-121 | Cyhalofop-butyl | Acetyl-CoA Carboxylase-IN-1 | PF-05221304 | Clethodim | Moiramide B | Clodinafop-propargyl | VY-3-135 | Quizalofop-ethyl | TOFA | Tralkoxydim |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | Lipid Metabolism Compound Library | Metabolism Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Human Metabolite Library | Anti-Hypertension Compound Library |
United States
