B-007
B-007 is an AplnR agonist with G protein-biased signaling (EC50 = 11.6 nM). B-007 activates the G protein pathway while abolishing β-arrestin1 and β-arrestin2 signaling. B-007 serves as a scaffold for development of G protein-biased apelin receptor agonists. B-007 can be used for the research of heart failure.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C32H24F5N5O7S
- 分子量:717.62
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Arrestin アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
Arrestin-2/β-Arrestin 1 |
Arrestin-3/β-Arrestin 2 |
体外実験
B-007 potently activates the AplnR G protein pathway in cell systems expressing the Apelin receptor (AplnR), with an EC50 of 11.6 nM and an Emax of 118.0%[1].
B-007 completely fails to activate the β-arrestin1 or β-arrestin2 pathways of the AplnR in AplnR-expressing cell systems, thereby exhibiting prominent G protein-biased characteristics[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
化学情報
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分子量 717.62
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分子式 C32H24F5N5O7S
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SMILES
COC1=CC=CC(OC)=C1C2=NC(C(NS(C(C3=CC=CC=C3)COC(C4=C(F)C(F)=C(F)C(F)=C4F)=O)(=O)=O)=O)=NN2C5=CN=CC(C)=C5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)