AMPKα1 activator 1
AMPKα1 activator 1 is a selective and orally active AMPKα1 activator with an EC50 of 35.1 nM. AMPKα1 activator 1 shows 176-fold selectivity over AMPKα2. AMPKα1 activator 1 can be used as a cell protectant and a kidney protectant. AMPKα1 activator 1 attenuates elevation of serum creatinine and blood urea nitrogen levels, alleviates kidney damage, and reduces cellular infiltration in renal ischemia-reperfusion injury contexts. AMPKα1 activator 1 can be associated with renal ischemia-reperfusion injury research.
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- Formel: C22H20ClN5O2S
- Molecular Weight:453.94
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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AMPK α1β1γ1 35.1 nM (IC50) |
AMPK α2β1γ1 6200 nM (IC50) |
AMPKα1 activator 1 (22f) (0.25-0.5 μM; 10 h) concentration-dependently regulates oxidative stress, apoptosis, autophagy, and lipid metabolism in H/R-injured NRK-52E cells via AMPKα1 activation[1].
AMPKα1 activator 1 (22f) (0.25-0.5 μM; 10 h) selectively activates AMPKα1 (not AMPKα2) in H/R-injured NRK-52E cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NRK-52E cells (rat renal proximal tubular epithelial cells) subjected to hypoxia-reoxygenation (H/R) injury
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Concentration:0.25-0.5 μM (H/R injury period); 12 μM (Compound C co-treatment)
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Incubation Time:10 h (H/R injury period: 5 h hypoxia + 5 h reoxygenation)
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Result:Concentration-dependently restored viability of H/R-injured NRK-52E cells; reduced viability restoration observed when co-treated with 12 μM Dorsomorphin (Compound C) (HY-13418A).
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Cell Line:H/R-injured NRK-52E cells
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Concentration:0.25-0.5 μM (H/R injury period); 12 μM (Compound C co-treatment)
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Incubation Time:10 h (H/R injury period: 5 h hypoxia + 5 h reoxygenation)
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Result:Concentration-dependently increased p-AMPK/AMPK and p-ACC/ACC ratios; blunted p-AMPK/AMPK and p-ACC/ACC ratio increases observed when co-treated with 12 μM CDorsomorphin (Compound C) (HY-13418A)
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 16-18 g) bearing renal ischemia-reperfusion injury[1]
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Dosage:50, 100 mg/kg
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Administration:p.o.; daily; 4 days
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Result:Dose-dependently attenuated IRI-induced increases in blood urea nitrogen and blood creatinine; significantly attenuated histological kidney damage and immune cell infiltration; dose-dependently up-regulated p-AMPKα1/AMPKα1 in renal tissue; up-regulated CPT1 and LC3B/LC3A protein levels; down-regulated BAX/BCl2 protein levels in renal tissue.
Chemical Information
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Molecular Weight 453.94
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Formel C22H20ClN5O2S
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SMILES
CN1C(S/C(C1=O)=C\C2=NNC3=CC(Cl)=C(C=C32)C4=CC=C(C=C4)N5CCNCC5)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
AMPKα1 activator 1 Related Classifications
HY-181077 Related Classifications
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