Firsocostat
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.
For research use only. We do not sell to patients.
- Purity: 99.96%
- CAS No.: 1434635-54-7
- Formula: C28H31N3O8S
- Molecular Weight:569.63
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Firsocostat
More- Signal Transduct Target Ther. 2020 Sep 3;5(1):187. [Abstract]
- Adv Funct Mater. 2025 Jan 19.
- Mol Cell. 2026 Jun 2:S1097-2765(26)00317-5. [Abstract]
- Adv Sci (Weinh). 2023 Aug;10(23):e2301094. [Abstract]
- Sci Adv. 2023 Oct 20;9(42):eadj4198. [Abstract]
- Cell Rep Med. 2024 Feb 20;5(2):101401. [Abstract]
- Clin Cancer Res. 2025 May 15;31(10):1975-1987. [Abstract]
- Int J Biol Sci. 2023 Jun 14;19(10):3143-3158. [Abstract]
- J Transl Med. 2025 May 14;23(1):542. [Abstract]
- Cell Rep. 2021 Jul 27;36(4):109460. [Abstract]
- Cell Biol Toxicol. 2025 Feb 3;41(1):39. [Abstract]
- Pharmaceuticals (Basel). 2026 Jan 24;19(2):201. [Abstract]
- FASEB J. 2025 Mar 31;39(6):e70393. [Abstract]
- iScience. 2021 May 25;24(6):102651. [Abstract]
- Sci Rep. 2024 Mar 11;14(1):5885. [Abstract]
- SLAS Discov. 2020 Aug;25(7):709-722. [Abstract]
- PeerJ. 2019 Dec 20;7:e8115. [Abstract]
- bioRxiv. 2025 Aug 26:2025.08.21.671640. [Abstract]
- 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.
Customer Validation & Images
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
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IHC
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Cell Imaging/Staining
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Flow Cytometry
Biological Activity
IC50: 2.1 nM (hACC1); 6.1 nM (hACC2)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
<100 nM
Compound: 46
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Inhibition of fatty acid synthesis in human HepG2 cells
Inhibition of fatty acid synthesis in human HepG2 cells
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[PMID: 25333641] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1434635-54-7
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Appearance Solid
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Molecular Weight 569.63
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Formula C28H31N3O8S
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Color White to light yellow
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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
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Synonyms
ND-630; GS-0976; NDI-010976
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (24)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
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).
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Mol Cell
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.
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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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
iScience
Combined epigenetic and metabolic treatments overcome differentiation blockade in acute myeloid leukemia. [Abstract]2021 May 25;24(6):102651. PMID: 34151238 -
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 -
SLAS Discov
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 ×.
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bioRxiv
2025 Aug 26:2025.08.21.671640. PMID: 40909529 -
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Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: 0.5 mg/mL (0.88 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| 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 |
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