Firsocostat (ND-630, GS-0976)

製品コードS8893 バッチS889301

化学情報

	Synonyms	NDI-010976	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₈H₃₁N₃O₈S
	分子量	569.63	CAS No.	1434635-54-7
Solubility (25°C)*	体外	DMSO	100 mg/mL (175.55 mM)
		Ethanol	4 mg/mL (7.02 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Firsocostat (GS-0976, ND-630)は、アセチルCoAカルボキシラーゼ（ACC）の可逆的阻害剤であり、hACC1およびhACC2に対するIC50値はそれぞれ2.1 nMおよび6.1 nMです。
in vitro	When ND-630 and [¹⁴C]acetate were administered to Hep-G2 cells for 4 h, ND-630 inhibited FASyn with EC50 values of 66 nM in cells cultured in medium containing. When ND-630 and[¹⁴C]palmitate were administered to C2C12 cells for 6 h, ND-630 increased both the release of [¹⁴C]O₂ and the production of[¹⁴C]acid-soluble material.
in vivo	When administered chronically to rats with diet-induced obesity, ND-630 reduces hepatic steatosis, improves insulin sensitivity, reduces weight gain without affecting food intake, and favorably affects dyslipidemia.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HepG2 cells
	濃度	2.1 nM (ACC1); 6.1 nM (ACC2)
	反応時間	1 h
	実験の流れ	Cells were treated with varying concentrations of ND-630.
動物実験	動物モデル	Male Sprague–Dawley rats
	投薬量	10 mg/kg
	投与方法	o.g.

参考

https://pubmed.ncbi.nlm.nih.gov/26976583/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Acetyl-CoA carboxylase 1 inhibition increases Treg metabolism and graft-versus-host disease treatment efficacy via mitochondrial fusion [ Journal of Clinical Investigation, 2025, e182480]	PubMed: 41026528.0
Glycerol Kinase Drives Hepatic de novo Lipogenesis and Triglyceride Synthesis in Nonalcoholic Fatty Liver by Activating SREBP-1c Transcription, Upregulating DGAT1/2 Expression, and Promoting Glycerol Metabolism [ Adv Sci (Weinh), 2024, 11(46):e2401311]	PubMed: 39418169
De novo lipogenesis fuels adipocyte autophagosome and lysosome membrane dynamics [ Nat Commun, 2023, 14(1):1362]	PubMed: 36914626
De novo lipogenesis fuels adipocyte autophagosome and lysosome membrane dynamics [ Nature Communications, 2023, 1362]	PubMed: 36914626.0
Macrophage acetyl-CoA carboxylase regulates acute inflammation through control of glucose and lipid metabolism [ Science Advances, 2022, eabq1984]	PubMed: 36417534.0
Acetyl-CoA metabolism drives epigenome change and contributes to carcinogenesis risk in fatty liver disease [ Genome Medicine, 2022, 67]	PubMed: 35739588.0
Acetyl-CoA metabolism drives epigenome change and contributes to carcinogenesis risk in fatty liver disease [ Genome Med, 2022, 14(1):67]	PubMed: 35739588
Macrophage acetyl-CoA carboxylase regulates acute inflammation through control of glucose and lipid metabolism [ Sci Adv, 2022, 8(47):eabq1984]	PubMed: 36417534
LXRα activation and Raf inhibition trigger lethal lipotoxicity in liver cancer [ NAT CANCER, 2021, 2, 201–217]	PubMed: None
Metabolic convergence on lipogenesis in RAS, BCR-ABL, and MYC-driven lymphoid malignancies [ Cancer Metab, 2021, 9(1):31]	PubMed: 34399819

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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