AZ13581837
AZ13581837 is an orally active GPR120 agonist with an EC50 of 5.2 nM for human GPR120. AZ13581837 signals through Gαq, Gαs, and β-arrestin pathways, reduces cAMP production, stimulates GLP-1 secretion, induces glucose lowering, and increases insulin secretion. AZ13581837 can be used for the research of type 2 diabetes.
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。
- CAS 番号: 2896777-27-6
- 分子式: C20H14N2O3S
- 分子量:362.40
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
製品説明
IC50 & Target
[1]|
GLP-1 |
体外実験
AZ13581837 (1×10−9-1×10−4 M) potently activates mouse GPR120 in CHO-mGPR120 cells, inducing a DMR response with an EC50 of 4.3 nM[1].
AZ13581837 (1×10−9-1×10−4 M) induces a Gαq-dependent calcium mobilization response in CHO-hGPR120 cells with an EC50 of 120 nM[1].
AZ13581837 (1×10-9-1×10-4 M; 45 min) stimulates cAMP production in CHO-hGPR120 cells via Gαs signaling, with an EC50 of 60 nM[1].
AZ13581837 (1×10−9-1×10−4 M; 5 h) potently induces β-arrestin recruitment in U2OS-hGPR120 cells, with an EC50 of 5.2 nM[1].
AZ13581837 (10 μM; 30 min) specifically inhibits cAMP production in primary wild-type mouse islet cells, with no effect observed in GPR120 null islet cells[1].
AZ13581837 (10 μM; 2 h) induces significant GPR120-dependent secretion of active GLP-1 from STC-1 enteroendocrine cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:STC-1 mouse enteroendocrine cells
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Concentration:10 μM
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Incubation Time:2 h
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Result:Significantly increased active GLP-1 secretion from STC-1 cells compared to vehicle control, with secreted active GLP-1 levels.
体内実験
AZ13581837 (35 mg/kg; p.o.; single dose 30 minutes prior to glucose bolus) enhances glucose-stimulated insulin secretion and improves glucose elimination in lean female mice via a GLP-1-dependent mechanism[1].
AZ13581837 (35 mg/kg; p.o.; single dose 30 minutes prior to glucose bolus) has glucose-lowering and insulin-stimulating effects dependent on functional GPR120, as no effects are observed in GPR120 null mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (8-week-old male, 27-32 g)[1]
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Dosage:7 mg/kg; 18 mg/kg
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Administration:p.o.; single dose 30 minutes prior to glucose load
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Result:Caused a concentration-dependent reduction in glucose excursions compared to vehicle-treated mice.
Resulted in significantly improved glucose tolerance at 18 mg/kg dose.
Achieved an unbound effective concentration (Ce50) of 0.02 μM, corresponding to exposure levels 1-3 times the in vitro EC50 for mouse GPR120 in the DMR assay.
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Animal Model:C57BL/6JOlaHSd mice (8-week-old female, 20-25 g)[1]
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Dosage:35 mg/kg
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Administration:p.o.; single dose 30 minutes prior to glucose bolus
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Result:Caused a slight but significant reduction in basal blood glucose (7.1 mM.
Significantly elevated insulin levels up to 10 minutes post glucose bolus.
Increased the acute insulin response (AIR) to ~2.4 ng/mL.
Significantly reduced plasma glucose at 20 minutes post glucose bolus.
Increased glucose elimination to ~3.8%/min.
Induced a significant increase in total GLP-1 levels compared to vehicle-treated mice.
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Animal Model:C57BL/6 wild-type mice (female, 22.5-23.0 g); C57BL/6 GPR120 null (female, 22.5 ± 0.7 g)[1]
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Dosage:35 mg/kg
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Administration:p.o.; single dose 30 minutes prior to glucose bolus
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Result:Significantly increased the acute insulin response compared to vehicle controls and increased glucose elimination in wild-type mice.
化学情報
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CAS 番号 2896777-27-6
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分子量 362.40
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分子式 C20H14N2O3S
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SMILES
O=S1(=O)C=2C=CC=CC2CN1C=3C=C(C#C)C=C(OC=4C=NC=CC4)C3
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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 Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Human Islet Cell Culture
The method of preserving islets in vitro, with purified reduced immunogenicity. The steps are islet isolation, islet cell purification, in vitro determination of islet function and islet cell culture.
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
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)