SSTR5 antagonist 7
SSTR5 antagonist 7 is an orally active SSTR5 antagonist, with an IC50 of 6.2 nM against hSSTR5 and an IC50 of 25 nM against mouse-derived SSTR5. SSTR5 antagonist 7 exerts a sustained hypoglycemic effect. SSTR5 antagonist 7 can be used for the research of 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: 1628744-37-5
- 分子式: C29H33ClFN3O4
- 分子量:542.04
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
SSTR5 6.2, 25 nM (IC50) |
体外実験
SSTR5 antagonist 7 (Compound 3p) (preincubated for 15 min, stimulated for 30 min) potently inhibits hSSTR5 (IC50 = 6.2 nM) and mouse-derived SSTR5 (IC50 = 25 nM) in CHO cells stably expressing the corresponding receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J Jcl (male, 9 weeks of age, high-fat diet-fed)[1]
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Dosage:3 mg/kg
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Administration:p.o.; single dose
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Result:Exhibited a persistent glucose-lowering effect comparable to positive control compound 3a at 100 mg/kg.
Reached a plasma concentration of 0.484 μg/mL at 8 hours after dosing.
Reduced blood glucose levels significantly relative to vehicle control at multiple time points after glucose loading.
Achieved a 21% reduction in blood glucose area under the curve (BG-AUC) relative to vehicle.
化学情報
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CAS 番号 1628744-37-5
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分子量 542.04
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分子式 C29H33ClFN3O4
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SMILES
O=C(C1(CCN(CC1)C2=NOC3(CN(C3)CC4=C(OC)C(Cl)=C(C5=CC=C(F)C=C5)C(C6CC6)=C4)C2)C)O
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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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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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)