1. Metabolic Enzyme/Protease
  2. Acetyl-CoA Carboxylase
  3. Firsocostat

Firsocostat (Synonyms: ND-630; GS-0976; NDI-010976)

Cat. No.: HY-16901 Purity: 98.61% ee.: 99.93%
Handling Instructions

Firsocostat (ND-630; GS-0976; NDI-010976) is an acetyl-CoA carboxylase (ACC) inhibitor; inhibits human ACC1 and ACC2 with IC50 values of 2.1 and 6.1 nM, respectively.

For research use only. We do not sell to patients.

Firsocostat Chemical Structure

Firsocostat Chemical Structure

CAS No. : 1434635-54-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 338 In-stock
Estimated Time of Arrival: December 31
5 mg USD 270 In-stock
Estimated Time of Arrival: December 31
10 mg USD 450 In-stock
Estimated Time of Arrival: December 31
25 mg USD 650 In-stock
Estimated Time of Arrival: December 31
50 mg USD 850 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1150 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Firsocostat:

Top Publications Citing Use of Products

    Firsocostat purchased from MCE. Usage Cited in: PeerJ. 2019 Dec.

    GS-0976 reduces lipid accumulation and expression of profibrogenic genes. Oil Red O staining is performed in LO2 cells after treatment with the indicated GS-0976 in the presence of 0.8 mM FFA for 24 h. Original magnification , 400 ×.
    • Biological Activity

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    Description

    Firsocostat (ND-630; GS-0976; NDI-010976) is an acetyl-CoA carboxylase (ACC) inhibitor; inhibits human ACC1 and ACC2 with IC50 values of 2.1 and 6.1 nM, respectively.

    IC50 & Target

    IC50: 2.1 nM (hACC1); 6.1 nM (hACC2)[1]

    In Vitro

    Firsocostat (ND-630) inhibits hACC1 (IC50=2.1±0.2 nM) and hACC2 (IC50=6.1±0.8 nM). Inhibition is reversible and highly specific for ACC. Firsocostat inhibits ACC activity by interacting within the phosphopeptide-acceptor and dimerization site of the enzyme to prevent dimerization. Firsocostat inhibits fatty acid synthesis with an EC50 of 66 nM in HepG2 cells without altering the total cell number, cellular protein concentration, and incorporation of acetate into cholesterol[1].

    In Vivo

    Chronical administration of Firsocostat (ND-630) to rats with diet-induced obesity reduces hepatic steatosis, improves insulin sensitivity, reduces weight gain without affecting food intake, and favorably affects dyslipidemia. Chronical administration of Firsocostat Zucker diabetic fatty rats, Firsocostat reduces hepatic steatosis, improves glucose-stimulated insulin secretion, and reduces hemoglobin A1c (0.9% reduction). Firsocostat exhibits an aqueous solubility of 594 μM and human and rat plasma protein binding of 98.5% and 98.6%, respectively. Pharmacokinetic evaluation of Firsocostat in male Sprague-Dawley rats [i.v. 3 mg/kg; orally (p.o.) 10 mg/kg] yields a plasma t1/2 of 4.5 h, bioavailability of 37%, clearance of 33 mL/min/kg, volume of distribution of 1.9 L/kg, oral time of maximum plasma concentration of 0.25 h[1].

    Clinical Trial
    Molecular Weight

    569.63

    Formula

    C₂₈H₃₁N₃O₈S

    CAS No.

    1434635-54-7

    SMILES

    O=C(C(C(C)=C(C1=NC=CO1)S2)=C2N3C[[email protected]](OC4CCOCC4)C5=C(OC)C=CC=C5)N(C(C)(C)C(O)=O)C3=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (87.78 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7555 mL 8.7776 mL 17.5553 mL
    5 mM 0.3511 mL 1.7555 mL 3.5111 mL
    10 mM 0.1756 mL 0.8778 mL 1.7555 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Animal Administration
    [1]

    Rats: Firsocostat is prepared in aqueous saline solution containing 1% Tween 80 and 0.5% methyl cellulose. Eight-week-old male ZDF rats are given either vehicle or Firsocostat (0.5, 1.5, 5 mg/kg) in vehicle by oral gavage b.i.d. for 37 d. Blood glucose is measured by glucometer at baseline and weekly just before dosing. Blood is collected at baseline, after 3 wk of treatment, and at the end of the study, 6 h after dosing and after a 6-h fast, for measurement of the indicated parameters. After 3 wk of treatment, animals received an oGTT (1 g/kg glucose). At the end of the study animals are killed, and liver cholesterol, triglycerides, and free fatty acids are determined[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 98.61% ee.: 99.93%

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    Keywords:

    FirsocostatND-630 GS-0976 NDI-010976ND630ND 630GS0976GS 0976GS-0976NDI010976NDI 010976NDI-010976Acetyl-CoA CarboxylaseACC, Acetyl Coenzyme A CarboxylaseInhibitorinhibitorinhibit

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