2. Epigenetics PI3K/Akt/mTOR
  3. AMPK
  4. PXL770

PXL770 is an orally active, direct allosteric AMP-activated protein kinase (AMPK) activator. PXL770 decreases C26:0 levels, improves mitochondrial respiration, reduces expression of proinflammatory genes and induces expression of compensatory transporters (ABCD2/3) in ALD fibroblasts/lymphocytes. PXL770 normalizes plasma VLCFA levels, significantly reduces elevated VLCFA levels in brain and spinal cord in Abcd1 KO mice. PXL770 improves glycemia, dyslipidemia, and insulin resistance in ob/ob and high-fat diet (HFD)-fed mice. PXL770 can be used for the study of X-linked adrenoleukodystrophy (ALD), autosomal dominant polycystic kidney disease and nonalcoholic steatohepatitis (NASH).

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PXL770

PXL770 Chemical Structure

CAS No. : 1523493-53-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

PXL770 Related Antibodies

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NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

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  • Purity & Documentation

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Description

PXL770 is an orally active, direct allosteric AMP-activated protein kinase (AMPK) activator. PXL770 decreases C26:0 levels, improves mitochondrial respiration, reduces expression of proinflammatory genes and induces expression of compensatory transporters (ABCD2/3) in ALD fibroblasts/lymphocytes. PXL770 normalizes plasma VLCFA levels, significantly reduces elevated VLCFA levels in brain and spinal cord in Abcd1 KO mice. PXL770 improves glycemia, dyslipidemia, and insulin resistance in ob/ob and high-fat diet (HFD)-fed mice. PXL770 can be used for the study of X-linked adrenoleukodystrophy (ALD), autosomal dominant polycystic kidney disease and nonalcoholic steatohepatitis (NASH)[1][2][3].

IC50 & Target[2]

AMPK α1β1γ1

16.2 nM (EC50)

AMPK α2β1γ1

1338 nM (EC50)

AMPK α1β2γ1

1.3 μM (EC50)

AMPK α1β1γ2

42.1 nM (EC50)

AMPK α1β1γ2

68.7 nM (EC50)

AMPK α2β1γ3

41.5 nM (EC50)

AMPK α1β1γ3

64 nM (EC50)

In Vitro

PXL770 (0.1-50 μM, 7 d) reduces C26:0 levels (IC50 = 3.1 μM), normalizes C24:0 levels and C26:0/C22:0 ratio in AMN/C-ALD fibroblasts and Abcd1 KO mouse glial cells[1].
PXL770 (25-50 μM, 72 h) improves mitochondrial function in C-ALD fibroblasts and AMN fibroblasts[1].
PXL770 (5-50 μM, 72 h) upregulates ABCD2 and ABCD3 mRNA expression in AMN/C-ALD fibroblasts[1].
PXL770 (10 μM, 72 h) downregulates proinflammatory genes (NFKB, CCL5, CCR3, NOS2) in C-ALD lymphocytes and TNFα/IL1β-stimulated Abcd1 KO mouse glial cells[1].
PXL770 shows in vitro activation effects on different recombinant AMPK heterotrimeric proteins with EC50 values of 16.2 nM (α1β1γ1), 42.1 nM (α1β1γ2), 64 nM (α1β1γ3), 1338 nM (α2β1γ1), 68.7 nM (α2β1γ2), 41.5 nM (α2β1γ3), 1.3 μM (α1β2γ1)[2].
PXL770 (0.5-3.5 μM) inhibits TGF-β-induced activation of human primary hepatic stellate cells (HSCs), reducing ACTA2 and COL1A1 gene expression and procollagen α1 protein secretion[2].
PXL770 (2.6-2.8 μM) inhibits de novo lipogenesis (DNL) in primary human and mouse hepatocytes in a dose-dependent manner, with IC50 values of 2.6 μM (human) and 2.8 μM (mouse)[2].
PXL770 (25-50 μM) activates AMPK in M1-polarized human macrophages (moMacs) and LPS (HY-D1056)-primed human dendritic cells (moDCs) dose-dependently, reducing secretion of pro-inflammatory cytokines (TNF-α, IL-6 in moMacs; TNF-α, IL-6, IL-12p70 in moDCs[2].
PXL770 (50 μM) suppresses IL-1β-induced nuclear factor κB (NF-κB) nuclear activity and LPS-induced IL-1β, IL-6 secretion in epididymal adipose tissue explants of ob/ob mice[2].

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

PXL770 Related Antibodies

Real Time qPCR[1]

Cell Line: C-ALD lymphocytes and TNFα/IL1β-stimulated Abcd1 KO mouse glial cells
Concentration: 10 μM
Incubation Time: 72 h
Result: Downregulated proinflammatory genes (NFKB, CCL5, CCR3, NOS2) in C-ALD lymphocytes and TNFα/IL1β-stimulated Abcd1 KO mouse glial cells.
In Vivo

PXL770 (75 mg/kg, p.o., twice daily, 8 weeks) reduces brain C26:0 levels and C24:0 levels in Abcd1 KO mice[1].
PXL770 (35-75 mg/kg, p.o., twice daily) inhibits hepatic de novo lipogenesis (DNL) in fasted-refed C57BL/6J mice, as shown by reduced 3H2O incorporation into liver lipids[2].
PXL770 (75 mg/kg, p.o., twice daily, 5 days) improves glucose tolerance in ob/ob mice[2].
PXL770 (35-75 mg/kg, p.o., twice daily, 6-8 weeks) increases steady-state glucose infusion rate (SSGIR) and decreases hepatic glucose production rate (GPR) in high-fat diet (HFD)-fed mice[2].

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

Animal Model: 6-8-week-old Abcd1 KO mice[1]
Dosage: 75 mg/kg
Administration: p.o., twice daily, 8 weeks
Result: Normalized plasma C26:0 levels.
Reduced brain C26:0 levels and C24:0 levels.
Animal Model: 6-week-old mice were fed a high-fat diet (60% of energy from fat) for 10 weeks to establish a metabolic syndrome model[2]
Dosage: 35, 75 mg/kg
Administration: p.o., twice daily, 6, 8 weeks
Result: Increased steady-state glucose infusion rate (SSGIR). Decreased hepatic glucose production rate (GPR) during euglycemic hyperinsulinemic clamp. Activated AMPK in liver, adipose tissue, and whole blood. Reduced liver steatosis, inflammation, and hepatocellular ballooning scores. Decreased liver triglyceride (TG) content and plasma alanine aminotransferase (ALT), aspartate aminotransferase (AST) levels. Reduced total liver leukocytes, monocytes, and resident macrophages. Downregulated hepatic profibrogenic gene (TGF-β, PDGF, COL1A1, COL3A1, TIMP1, TIMP2) expression.
Clinical Trial
Molecular Weight

423.91

Formula

C23H18ClNO3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=C(C(O)=C1C3=CC=CC=C3)C(C4=C(O)C(CCCC5)=C5C=C4)=C(Cl)S2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 120 mg/mL (283.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3590 mL 11.7950 mL 23.5899 mL
5 mM 0.4718 mL 2.3590 mL 4.7180 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3 mg/mL (7.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3590 mL 11.7950 mL 23.5899 mL 58.9748 mL
5 mM 0.4718 mL 2.3590 mL 4.7180 mL 11.7950 mL
10 mM 0.2359 mL 1.1795 mL 2.3590 mL 5.8975 mL
15 mM 0.1573 mL 0.7863 mL 1.5727 mL 3.9317 mL
20 mM 0.1179 mL 0.5897 mL 1.1795 mL 2.9487 mL
25 mM 0.0944 mL 0.4718 mL 0.9436 mL 2.3590 mL
30 mM 0.0786 mL 0.3932 mL 0.7863 mL 1.9658 mL
40 mM 0.0590 mL 0.2949 mL 0.5897 mL 1.4744 mL
50 mM 0.0472 mL 0.2359 mL 0.4718 mL 1.1795 mL
60 mM 0.0393 mL 0.1966 mL 0.3932 mL 0.9829 mL
80 mM 0.0295 mL 0.1474 mL 0.2949 mL 0.7372 mL
100 mM 0.0236 mL 0.1179 mL 0.2359 mL 0.5897 mL
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PXL770 Related Classifications

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.

Keywords:

PXL7701523493-53-9PXL 770PXL-770AMPKAMP-activated protein kinaseX-linked adrenoleukodystrophy (ALD)autosomal dominant polycystic kidney diseasenonalcoholic steatohepatitis (NASH)Inhibitorinhibitorinhibit

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