1. Cell Cycle/DNA Damage Epigenetics PI3K/Akt/mTOR Metabolic Enzyme/Protease Apoptosis NF-κB Immunology/Inflammation
  2. Sirtuin AMPK PGC-1α Apoptosis Reactive Oxygen Species (ROS)
  3. MitoPBN

MitoPBN is a AMPK/SIRT3/PGC-1α axis modulator, reactive oxygen species scavenger and mitochondrial function enhancer. MitoPBN increases the phosphorylation level of AMPK, restores SIRT3 expression and reverses the down-regulation of PGC-1α, thereby promoting mitochondrial biogenesis. MitoPBN regulates glucose metabolism, reduces blood glucose by inhibiting hepatic gluconeogenesis and increasing hepatic glucose uptake, while scavenging mitochondrial superoxide anion/hydrogen peroxide, maintaining membrane potential and increasing ATP production. MitoPBN also reduces cell apoptosis, improves sperm motility, survival rate and membrane integrity, but may induce reductive stress in cryopreserved sperm at high concentrations. MitoPBN is widely applicable to research related to diabetes and type 2 diabetes.

For research use only. We do not sell to patients.

MitoPBN

MitoPBN Chemical Structure

CAS No. : 652968-37-1

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Description

MitoPBN is a AMPK/SIRT3/PGC-1α axis modulator, reactive oxygen species scavenger and mitochondrial function enhancer. MitoPBN increases the phosphorylation level of AMPK, restores SIRT3 expression and reverses the down-regulation of PGC-1α, thereby promoting mitochondrial biogenesis. MitoPBN regulates glucose metabolism, reduces blood glucose by inhibiting hepatic gluconeogenesis and increasing hepatic glucose uptake, while scavenging mitochondrial superoxide anion/hydrogen peroxide, maintaining membrane potential and increasing ATP production. MitoPBN also reduces cell apoptosis, improves sperm motility, survival rate and membrane integrity, but may induce reductive stress in cryopreserved sperm at high concentrations. MitoPBN is widely applicable to research related to diabetes and type 2 diabetes[1][2][3].

IC50 & Target

SIRT3

 

In Vitro

MitoPBN (40 μmol/l; 24 h) upregulates the AMPK/SIRT3/PGC-1α axis in STZ-treated primary mouse hepatocytes by increasing phosphorylated PGC-1α, phosphorylated AMPK, total AMPK, SIRT3, and NRF1 protein levels[1].
MitoPBN (40 μmol/l; 24 h) restores mitochondrial number in H2O2-stressed primary mouse hepatocytes, which was reduced by oxidative stress[1].
MitoPBN (100-150 μmol/L; ≥7 days) supplementation of isolated Ghezel ram sperm cryopreservation extender significantly improves post-thaw sperm motility, membrane integrity, mitochondrial activity, viability, antioxidant capacity, and ATP content while reducing ROS levels, abnormal sperm, and apoptosis, with 150 μmol/L being the optimal concentration[2].
MitoPBN (1-100 μmol/l; 3 h) potently scavenges peroxyl and carbon-centered free radicals in a cell-free in vitro system, as demonstrated by H2O2 consumption and adduct formation[3].
MitoPBN (5-20 μmol/l; 24 h) protects STZ-stressed L02 liver cells from cytotoxicity, with greater efficiency than PBN, and liposomal encapsulation as Nano-MitoPBN significantly reduces the effective protective concentration[3].
MitoPBN (40 μmol/l) inhibits hypoxia-induced mitophagy in L02 liver cells by reducing protein expression of LC3B and ATG5[3].

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

Cell Viability Assay[3]

Cell Line: Streptozotocin (HY-13753) -stressed L02 human liver cells
Concentration: 5, 20 μm
Incubation Time: 24 h
Result: Protected L02 cells from Streptozotocin (STZ)-induced cytotoxicity.
Showed lower protective efficiency than Nano-MitoPBN, with 5 μmol/l Nano-MitoPBN achieving a comparable effect to 40 μmol/l free MitoPBN.
Exhibited greater protective efficiency than PBN, requiring a lower concentration to rescue cell survival.
In Vivo

MitoPBN (100-150 μmol/L; added to tris extender for semen dilution prior to cryopreservation) mitigates cryopreservation-induced oxidative stress in Ghezel ram sperm, with the 150 μmol/L dose yielding the greatest improvements in total motility (54.16%), mitochondrial activity (50.26%), and ATP content (116.29 pmol/106 sperm)[2].
Free MitoPBN (2.5 mg/kg; i.p.; daily; 8 weeks) reduces random blood glucose levels and improves oral glucose tolerance in high-fat diet-induced type 2 diabetic C57BL/6J mice[3].

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

Animal Model: Sperm cryopreservation induced Ghezel rams sheep model (sexually mature)[2]
Dosage: 100 µmol/L; 150 µmol/L; 200 µmol/L; 250 µmol/L
Administration: added to tris extender for semen dilution prior to cryopreservation
Result: Effects at 100 µM
Increased total motility to 52.36%, progressive motility to 24.82%, membrane integrity to 50.01%, mitochondrial activity to 46.16%, and sperm viability to 48.99%.
Elevated total antioxidant capacity (TAC) to 1.85 mmol/L and glutathione peroxidase (GPx) activity to 61.16 U/mg.
Decreased ROS levels to 2.95 ×103 cpm/106 sperm, abnormal sperm to 19.23%, and apoptotic sperm to 20.10%.
Increased straight-line velocity (VSL) to 55.24 µm/s and ATP content to 90 pmol/106 sperm.
Effects at 150 µmol/L (Optimal Dose)
Achieved highest total motility (54.16%), progressive motility (26.77%), membrane integrity (52.54%), mitochondrial activity (50.26%), and sperm viability (52.20%).
Maximized TAC to 1.93 mmol/L and GPx activity to 63.36 U/mg.
Reduced ROS levels to their lowest point at 2.80 ×103 cpm/106 sperm, with abnormal sperm at 18.82% and apoptotic sperm at 18.70%.
Reached peak average path velocity (VAP) of 68.82 µm/s, VSL of 55.24 µm/s, and maximum ATP content of 116.29 pmol/106 sperm.
Effects at Higher Concentrations (200 & 250 µmol/L)
200 µmol/L (Diminishing Returns):
Showed increased sperm viability (44.12%) and ATP content, with reduced apoptotic sperm (~25%), but offered no significant improvements in motility, membrane integrity, or antioxidant markers compared to the 100 and 150 µmol/L doses.
250 µmol/L (Ineffective):
Did not provide significant beneficial effects on measured sperm parameters relative to the control group.
Molecular Weight

590.53

Formula

C33H37BrNO2P

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[O-]/[N+](C(C)(C)C)=C\C1=CC=C(OCCCC[P+](C2=CC=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4)C=C1.[Br-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMF : 25 mg/mL (42.33 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6934 mL 8.4670 mL 16.9339 mL
5 mM 0.3387 mL 1.6934 mL 3.3868 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 95.00%

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). 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
DMF 1 mM 1.6934 mL 8.4670 mL 16.9339 mL 42.3348 mL
5 mM 0.3387 mL 1.6934 mL 3.3868 mL 8.4670 mL
10 mM 0.1693 mL 0.8467 mL 1.6934 mL 4.2335 mL
15 mM 0.1129 mL 0.5645 mL 1.1289 mL 2.8223 mL
20 mM 0.0847 mL 0.4233 mL 0.8467 mL 2.1167 mL
25 mM 0.0677 mL 0.3387 mL 0.6774 mL 1.6934 mL
30 mM 0.0564 mL 0.2822 mL 0.5645 mL 1.4112 mL
40 mM 0.0423 mL 0.2117 mL 0.4233 mL 1.0584 mL
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  • 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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