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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)

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $88 | In Stock | In Stock | |
| 2 mg | $129 | In Stock | In Stock | |
| 5 mg | $222 | In Stock | In Stock | |
| 10 mg | $372 | In Stock | In Stock | |
| 25 mg | $537 | In Stock | In Stock | |
| 50 mg | $690 | In Stock | In Stock | |
| 100 mg | $955 | In Stock | In Stock | |
| 500 mg | $1,890 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $279 | In Stock | In Stock |
| 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) |
| Targets&IC50 | ACC2:6.1 nM, ACC1:2.1 nM |
| 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. |
| Synonyms | NDI-010976, ND-630, GS-0976 |
| Molecular Weight | 569.63 |
| Formula | C28H31N3O8S |
| Cas No. | 1434635-54-7 |
| Smiles | COc1ccccc1[C@H](Cn1c2sc(c(C)c2c(=O)n(c1=O)C(C)(C)C(O)=O)-c1ncco1)OC1CCOCC1 |
| Relative Density. | 1.42 g/cm3 (Predicted) |
| Storage | 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. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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