XN methyl pyrazole
XN methyl pyrazole (XP) is an orally active, blood-brain barrier permeable uncoupler/proton carrier. XN methyl pyrazole uncouples oxidative phosphorylation, depolarizes mitochondrial transmembrane potential, increases energy expenditure, spontaneous activity levels, and cortical inosine monophosphate levels. XN methyl pyrazole reduces plasma purine and energy metabolite levels, improves glucose tolerance, and decreases weight gain, while avoiding potential estrogenic side effects. XN methyl pyrazole can be used in studies related to diet-induced obesity and insulin resistance.
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- CAS No.: 2820169-36-4
- Formule: C22H24N2O4
- Masse moléculaire:380.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
XN methyl pyrazole (0-50 μM; 24 h) does not reduce the viability of HepG2 or C2C12 cells at concentrations below 50 μM after 24 h incubation[1].
XN methyl pyrazole (1-15 μM; 1 h) acts as a protonophore to depolarize the mitochondrial transmembrane potential in C2C12 cells at concentrations from 1 to 15 μM after 1 h incubation, uncoupling oxidative phosphorylation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (9-week-old male, diet-induced obesity via 12-week high-fat diet)[1]
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Dosage:30 mg/kg
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Administration:p.o.; once daily; 11 weeks
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Result:Reduced final body weight to 37.87 g compared to 40.42 g in controls.
Improved glucose tolerance compared to controls.
Reduced homeostatic model assessment of insulin resistance (HOMA-IR) by 77.9% to 10.94.
Increased mean energy expenditure by 20−27% compared to controls.
Increased respiratory exchange ratio compared to controls.
Increased total movement compared to controls.
Increased locomotor movement by 75-135% compared to controls.
Increased percent ambulatory time compared to controls.
Decreased plasma concentrations of purine metabolites (adenosine monophosphate, inosine monophosphate, inosine, hypoxanthine, xanthine) and creatine relative to controls.
Increased cortical inosine monophosphate abundance by 76% compared to controls.
Caused no significant changes in plasma triglycerides, total cholesterol, inflammatory cytokines (MCP-1, IL-6), or liver enzyme (AST, ALT) activities relative to controls.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2820169-36-4
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Masse moléculaire 380.44
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Formule C22H24N2O4
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SMILES
OC1=CC(OC)=C(C2=NN(C)C(C3=CC=C(O)C=C3)=C2)C(O)=C1C/C=C(C)\C
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Synonyms
XP
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
XN methyl pyrazole Related Classifications
HY-139994 Related Classifications
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