Referencia número: HY-16901

Firsocostat

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

24 Cited Publications

Revisión del cliente

Based on 24 publication(s) in Google Scholar

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.

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Pureza: 99.96%
No. CAS: 1434635-54-7
Fòrmula: C₂₈H₃₁N₃O₈S
Peso molecular:569.63

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Firsocostat Chemical Structure

No. CAS: 1434635-54-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (24)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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]

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	<100 nM Compound: 46	Inhibition of fatty acid synthesis in human HepG2 cells Inhibition of fatty acid synthesis in human HepG2 cells	[PMID: 25333641]

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].

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

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 t_1/2 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].

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

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1434635-54-7
Appearance Solid
Peso molecular 569.63
Fòrmula C₂₈H₃₁N₃O₈S
Color White to light yellow
SMILES

O=C(C(C(C)=C(C1=NC=CO1)S2)=C2N3C[C@H](OC4CCOCC4)C5=C(OC)C=CC=C5)N(C(C)(C)C(O)=O)C3=O
Synonyms

ND-630; GS-0976; NDI-010976
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (24)

All Cell Imaging/StainingIn Vivo Efficacy StudyFlow CytometryBio/Physico-chemical AssayIHC

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Journal Impact Factor

Signal Transduct Target Ther

LKB1-AMPK axis negatively regulates ferroptosis by inhibiting fatty acid synthesis. [Abstract]

2020 Sep 3;5(1):187. PMID: 32883948

Firsocostat purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2020 Sep 3;5(1):187. [Abstract]

Inhibitor of ACC1 can suppress Erastin or RSL3-induced ferroptosis. MEFs were treated as indicated for 10 h and cell death was measured by PI staining. Erastin (10 μM), RSL3 (0.5 μM), Firsocostat (ND-630, 5 μM)

Firsocostat purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2020 Sep 3;5(1):187. [Abstract]

Inhibitor of ACC1 can suppress Erastin or RSL3-induced ferroptosis in LKB1 KO MEFs and AMPK DKO MEFs. Cells were treated as indicated for 8 h and cell death was determined by PI staining coupled with flow cytometry. Erastin (10 μM), RSL3 (1 μM), Firsocostat (ND-630, 5 μM).
Adv Funct Mater

2025 Jan 19.
Mol Cell

Reductive death is averted by a conserved de novo lipogenic switch. [Abstract]

2026 Jun 2:S1097-2765(26)00317-5. PMID: 42229415
Adv Sci (Weinh)

MSL1 Promotes Liver Regeneration by Driving Phase Separation of STAT3 and Histone H4 and Enhancing Their Acetylation. [Abstract]

2023 Aug;10(23):e2301094. PMID: 37279389

Firsocostat purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Aug;10(23):e2301094. [Abstract]

Hepatic Ac‐CoA level in young mice, aged mice, and aged mice treated with Firsocostat (10 mg/kg, oral, daily, 28 days) at 0 and 36 h after partial hepatectomy (PH; n = 6 mice per group).

Firsocostat purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Aug;10(23):e2301094. [Abstract]

Serum alanine aminotransferase (ALT) levels in young mice, aged mice, and aged mice treated with Firsocostat (10 mg/kg, oral, daily, 28 days) at 0 and 36 h after PH.

Firsocostat purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Aug;10(23):e2301094. [Abstract]

BrdU and Ki67 staining of liver tissues from young mice, aged mice, and aged mice treated with Firsocostat (10 mg/kg, oral, daily, 28 days) at 36 h after PH. Scale bar, 50 µm.
Cell Rep Med

p63 controls metabolic activation of hepatic stellate cells and fibrosis via an HER2-ACC1 pathway. [Abstract]

2024 Feb 20;5(2):101401. PMID: 38340725
Sci Adv

Hepatoviruses promote very-long-chain fatty acid and sphingolipid synthesis for viral RNA replication and quasi-enveloped virus release. [Abstract]

2023 Oct 20;9(42):eadj4198. PMID: 37862421
Int J Biol Sci

VDAC2 malonylation participates in sepsis-induced myocardial dysfunction via mitochondrial-related ferroptosis. [Abstract]

2023 Jun 14;19(10):3143-3158. PMID: 37416771
Clin Cancer Res

Targeting Acetyl-CoA Carboxylase Suppresses De Novo Lipogenesis and Tumor Cell Growth in Multiple Myeloma. [Abstract]

2025 May 15;31(10):1975-1987. PMID: 40053701
J Transl Med

Mitochondrial dysfunction fuels drug resistance in adult T-cell acute lymphoblastic leukemia. [Abstract]

2025 May 14;23(1):542. PMID: 40369632
Cell Rep

Metabolically controlled histone H4K5 acylation/acetylation ratio drives BRD4 genomic distribution. [Abstract]

2021 Jul 27;36(4):109460. PMID: 34320364
Pharmaceuticals (Basel)

Antitumor Activity of the ACC Inhibitor Firsocostat in Breast Cancer Cell Lines: A Proof-of-Concept In Vitro Study. [Abstract]

2026 Jan 24;19(2):201. PMID: 41754743
Cell Biol Toxicol

UHRF1 promotes calcium oxalate-induced renal fibrosis by renal lipid deposition via bridging AMPK dephosphorylation. [Abstract]

2025 Feb 3;41(1):39. PMID: 39899077
Sci Rep

Digital pathology with artificial intelligence analysis provides insight to the efficacy of anti-fibrotic compounds in human 3D MASH model. [Abstract]

2024 Mar 11;14(1):5885. PMID: 38467661
iScience

Combined epigenetic and metabolic treatments overcome differentiation blockade in acute myeloid leukemia. [Abstract]

2021 May 25;24(6):102651. PMID: 34151238
FASEB J

Activation of SIK2 inhibits gluconeogenesis and alleviates lipogenesis-induced inflammatory response by SIK2-CRTC2-ACC1 in hepatocytes of large yellow croaker (Larimichthys crocea). [Abstract]

2025 Mar 31;39(6):e70393. PMID: 40067199
SLAS Discov

A Framework for Optimizing High-Content Imaging of 3D Models for Drug Discovery. [Abstract]

2020 Aug;25(7):709-722. PMID: 32484408
PeerJ

Comparative RNA-sequencing profiled the differential gene expression of liver in response to acetyl-CoA carboxylase inhibitor GS-0976 in a mouse model of NASH. [Abstract]

2019 Dec 20:7:e8115. PMID: 31879571

Firsocostat purchased from MedChemExpress. Usage Cited in: PeerJ. 2019 Dec 20:7:e8115. [Abstract]

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 ×.
bioRxiv

Plasma membrane accessible cholesterol is regulated by ACC1 and lipid droplets. [Abstract]

2025 Aug 26:2025.08.21.671640. PMID: 40909529
SSRN

2025 May 8.
University of Santiago de Compostela

2025.
bioRxIv

2024 July 09.
Patent

US20230310630A1.
Research Square Print

December 20th, 2022.
Research Square Preprint

2021 Jul.

Solvente y solubilidad

In Vitro:

DMSO : ≥ 50 mg/mL (87.78 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 1% DMSO 99% Saline

Solubility: 0.5 mg/mL (0.88 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocolo

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].

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (282 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Harriman G, et al. Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats. Proc Natl Acad Sci U S A. 2016 Mar 29;113(13):E1796-805. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7555 mL	8.7776 mL	17.5553 mL	43.8881 mL
	5 mM	0.3511 mL	1.7555 mL	3.5111 mL	8.7776 mL
	10 mM	0.1756 mL	0.8778 mL	1.7555 mL	4.3888 mL
	15 mM	0.1170 mL	0.5852 mL	1.1704 mL	2.9259 mL
	20 mM	0.0878 mL	0.4389 mL	0.8778 mL	2.1944 mL
	25 mM	0.0702 mL	0.3511 mL	0.7022 mL	1.7555 mL
	30 mM	0.0585 mL	0.2926 mL	0.5852 mL	1.4629 mL
	40 mM	0.0439 mL	0.2194 mL	0.4389 mL	1.0972 mL
	50 mM	0.0351 mL	0.1756 mL	0.3511 mL	0.8778 mL
	60 mM	0.0293 mL	0.1463 mL	0.2926 mL	0.7315 mL
	80 mM	0.0219 mL	0.1097 mL	0.2194 mL	0.5486 mL

Keywords

Firsocostat

24 Cited Publications

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Firsocostat

Anti-diabetic Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Lipid Metabolism Compound Library

Targeted Diversity Library

Human Metabolite Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Metabolism/Protease Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Firsocostat

Actividad biológica

Chemical Information

Publications (24)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Firsocostat

Anti-diabetic Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Lipid Metabolism Compound Library

Targeted Diversity Library

Human Metabolite Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Metabolism/Protease Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Firsocostat

Actividad biológica

Chemical Information

Publications (24)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Firsocostat Related Classifications

HY-16901 Related Classifications