1. Epigenetics PI3K/Akt/mTOR
  2. AMPK
  3. 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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AMPKα1 activator 1

AMPKα1 activator 1 Chemical Structure

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Description

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[1].

IC50 & Target[1]

AMPK α1β1γ1

35.1 nM (IC50)

AMPK α2β1γ1

6200 nM (IC50)

In Vitro

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.

Cell Viability Assay[1]

Cell Line: NRK-52E cells (rat renal proximal tubular epithelial cells) subjected to hypoxia-reoxygenation (H/R) injury
Concentration: 0.25-0.5 μM (H/R injury period); 12 μM (Compound C co-treatment)
Incubation Time: 10 h (H/R injury period: 5 h hypoxia + 5 h reoxygenation)
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).

Western Blot Analysis[1]

Cell Line: H/R-injured NRK-52E cells
Concentration: 0.25-0.5 μM (H/R injury period); 12 μM (Compound C co-treatment)
Incubation Time: 10 h (H/R injury period: 5 h hypoxia + 5 h reoxygenation)
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)
In Vivo

AMPKα1 activator 1 (compound 22f) (50-100 mg/kg; p.o.; daily; 4 days) dose-dependently protects against renal ischemia-reperfusion injury (IRI) in male C57BL/6 mice via selective AMPKα1 activation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male, 16-18 g) bearing renal ischemia-reperfusion injury[1]
Dosage: 50, 100 mg/kg
Administration: p.o.; daily; 4 days
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.
Molecular Weight

453.94

Formula

C22H20ClN5O2S

SMILES

CN1C(S/C(C1=O)=C\C2=NNC3=CC(Cl)=C(C=C32)C4=CC=C(C=C4)N5CCNCC5)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
AMPKα1 activator 1
Cat. No.:
HY-181077
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