BAY-876

製品コードS8452 バッチS845202

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H16F4N6O2
分子量 496.42 CAS No. 1799753-84-6
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 99 mg/mL (199.42 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 80 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. 
Clear solution
5% DMSO 95% Corn oil
0.4mg/ml Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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 BAY-876 is a potent and selective GLUT1 inhibitor (IC50=0.002 μM) with a selectivity factor of >100 against GLUT2, GLUT3, and GLUT4.
in vitro

BAY-876 is a highly-selective GLUT1 inhibitor with selectivity over GLUT2, 3, and 4 of 4700-, 800-, and 135-fold, respectively[1].
in vivo

BAY-876 displays low clearance also in vivo in rat and in dog. The volume of distribution in steady state (Vss) is moderate in both species. Terminal half life is intermediate in rat (2.5 h) and long in dog (22 h) due to the very low clearance. The oral bioavailability (F%) is 85% and 79% in rat and dog, respectively. Preliminary in vivo PK studies of BAY-876 demonstrate that a good oral bioavailability and long terminal half-life is attainable making it an excellent chemical probe to further evaluate the hypothesis of cancer treatment with a very selective GLUT1 inhibitor[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Cell-free assays
濃度 0.002 μM (IC50)
反応時間
実験の流れ
動物実験 動物モデル Male Wistar rats
投薬量 0.3 mg/kg
投与方法 i.v.

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：

GLUT1 promotes NLRP3 inflammasome activation of airway epithelium in lipopolysaccharide-induced acute lung injury [ Am J Pathol, 2024, S0002-9440(24)00116-0] PubMed: 38548270
Disulfidptosis-related signature predicts prognosis and characterizes the immune microenvironment in hepatocellular carcinoma [ Cancer Cell Int, 2024, 24(1):19] PubMed: 38195525
Alanine supplementation exploits glutamine dependency induced by SMARCA4/2-loss [ Nat Commun, 2023, 14(1):2894] PubMed: 37210563
Metabolic classification suggests the GLUT1/ALDOB/G6PD axis as a therapeutic target in chemotherapy-resistant pancreatic cancer [ Cell Rep Med, 2023, 4(9):101162] PubMed: 37597521
Metabolic classification suggests the GLUT1/ALDOB/G6PD axis as a therapeutic target in chemotherapy-resistant pancreatic cancer [ Cell Rep Med, 2023, S2666-3791(23)00315-4] PubMed: 37597521
BMP4 upregulates glycogen synthesis through the SMAD/SLC2A1 (GLUT1) signaling axis in hepatocellular carcinoma (HCC) cells [ Cancer Metab, 2023, 11(1):9] PubMed: 37443106
BMP4 upregulates glycogen synthesis through the SMAD/SLC2A1 (GLUT1) signaling axis in hepatocellular carcinoma (HCC) cells [ Cancer Metab, 2023, 11(1):9] PubMed: 37443106
The Impact of Proinflammatory Cytokines and Imiquimod on GLUT1 in HaCaT Keratinocytes - a Potential Anti-Psoriatic Therapeutic Target [ Cell Physiol Biochem, 2023, 57(2):54-62] PubMed: 36945896
Monosodium urate crystals regulate a unique JNK-dependent macrophage metabolic and inflammatory response [ Cell Rep, 2022, 38(10):110489] PubMed: 35263587
Cancer-specific cytotoxicity of pyridinium-based ionic liquids by regulating hypoxia-inducible factor-1α-centric cancer metabolism [ Ecotoxicol Environ Saf, 2022, 248:114334] PubMed: 36442398

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。