Firsocostat (GS-0976, ND-630)

製品コードS8893 バッチS889301

印刷

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (8.78mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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) is a reversible inhibitor of acetyl CoA carboxylase (ACC) with IC50s of 2.1 nM,6.1 nM for hACC1 and hACC2,respectively.
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.^[1]
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.^[1]

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：

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
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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。