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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2820169-36-4
- 分子式: C22H24N2O4
- 分子量:380.44
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
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.
体内実験
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.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2820169-36-4
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分子量 380.44
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分子式 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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別名
XP
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)