FuBIG
FuBIG is an iminoguanidine derivative with neuroprotective effects. FuBIGL inhibits L-LDH activation and reduces lactate production. FuBIGL exerts protective effects on inflammatory nerve cells, upregulates the expressions of AMPK, pAMPK and FOXO3, and activates the AMPK pathway in cells. FuBIG exerts anti-inflammatory effects by reducing pro-inflammatory cytokines (IL-6, IL-1β, TNF-α) and increasing the anti-inflammatory cytokine IL-10. FuBIG maintains mitochondrial membrane potential, alleviates mitochondrial dysfunction, reduces ROS production, and relieves oxidative stress. FuBIG upregulates Bcl-2, downregulates Bax and Caspase-3, and inhibits cell apoptosis (apoptosis). FuBIG improves metabolic disorders in diabetic mice, decreases the levels of LDL-C, ALT and AST, and increases HDL-C level simultaneously. FuBIG can be used in the research of diabetic neuroinflammation.
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- Formel: C8H12N8O
- Molecular Weight:236.23
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
FuBIG (3d) (0.3 mM; 48 h) potently reduces the excessive activation of L-LDH induced by LPS (HY-D1056) in SH-SY5Y and THLE-2 cells, restores its activity to near baseline levels, and decreases lactate accumulation[1].
FuBIG (0-1600 μM; 48 h) exerts a protective effect against LPS-induced cell death in SH-SY5Y cells and BV2 cells (with an EC50 of 222.3 μM for SH-SY5Y cells and an EC50 of 198.1 μM for BV2 cells), and maintains a cell survival rate of over 85% at a concentration of 1 mM[1].
FuBIG (0.3 mM; 12-24 h) can be transported into THLE-2 cells via OCT1[1].
FuBIG (0.3 mM; 48 h) activates the AMPK pathway in LPS-induced BV2 cells by upregulating the protein expression of AMPK, pAMPK and FOXO3[1].
FuBIG (0.3 mM; 48 h) exerts anti-inflammatory effects in LPS-induced BV2 cells by reducing pro-inflammatory cytokines (IL-6, IL-1β, TNF-α) and increasing the anti-inflammatory cytokine IL-10[1].
FuBIG (0.3 mM; 48 h) maintains mitochondrial membrane potential, alleviates LPS-induced mitochondrial dysfunction, reduces cellular ROS production, and mitigates oxidative stress in LPS-stimulated BV2 cells[1].
FuBIG (0.3 mM; 48 h) inhibits LPS-induced apoptosis of SH-SY5Y cells by upregulating the anti-apoptotic protein Bcl-2 and downregulating the pro-apoptotic proteins Bax, Caspase-3, and activated Caspase-3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS-induced SH-SY5Y human neuroblastoma cells, BV2 mouse microglial cells
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Concentration:1 mM/ (50, 100, 200, 400, 800, and
1600 μM) -
Incubation Time:48 h
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Result:Maintained >85% cell viability in LPS-induced SH-SY5Y and BV2 cells at 1 mM.
Achieved an EC50 of 222.3 μM in LPS-induced SH-SY5Y cells.
Achieved an EC50 of 198.1 μM in LPS-induced BV2 cells.
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Cell Line:LPS-induced BV2 mouse microglial cells
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Concentration:0.3 mM
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Incubation Time:48 h
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Result:Upregulated AMPK protein expression to levels comparable to metformin-treated cells.
Upregulated pAMPK protein expression to levels comparable to metformin-treated cells.
Upregulated FOXO3 protein expression to levels comparable to metformin-treated cells.\nReduced IL-6 protein expression and fluorescence intensity.
Reduced IL-1β protein expression.
Reduced TNF-α protein expression.
Increased IL-10 protein expression.
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Cell Line:LPS-induced SH-SY5Y human neuroblastoma cells
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Concentration:0.3 mM
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Incubation Time:48 h
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Result:Upregulated anti-apoptotic protein Bcl-2 expression.
Downregulated pro-apoptotic protein Bax expression.
Downregulated pro-apoptotic protein Caspase-3 expression.
Downregulated pro-apoptotic protein Cleaved Caspase-3 expression and fluorescence intensity.
| Species | Dose | Route | AUC0-t | AUC0-∞ | Cmax | Tmax | T1/2 |
|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.v. | 226.29 mg·h/L | 228.79 mg·h/L | 87.55 mg/L | 0.083 h | 4.106 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (female, 5-week-old, high-fat diet + streptozotocin-induced type 2 diabetes)[1]
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Dosage:10 mg/kg
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Administration:i.v.; daily; 21 days
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Result:Limited diabetic mice weight gain to 5.57 g.
Reduced fasting blood glucose by 19.7% (from 21.927 to 17.566 mmol/L).
Reduced the area under the oral glucose tolerance test curve by 24.2% (2542 min mmol/L vs.
3353 min mmol/L in untreated diabetic mice).
Increased serum HDL-C to 1.12 mmol/L.
Decreased serum LDL-C to 0.98 mmol/L.
Reduced serum AST to 109.50 U/L.
Reduced serum ALT to 65.67 U/L.
Chemical Information
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Molecular Weight 236.23
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Formel C8H12N8O
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SMILES
N=C(N/N=C/C1=CC=C(O1)/C=N/NC(N)=N)N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
FuBIG Related Classifications
HY-182469 Related Classifications
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- FuBIG
- Lactate Dehydrogenase
- AMPK
- FOXO
- Interleukin Related
- Reactive Oxygen Species (ROS)
- TNF Receptor
- Bcl-2 Family
- Caspase
- Apoptosis
- apoptosis
- BV2 cells
- diabetic mice
- organic cation transporter 1
- LPS-induced cells
- SH-SY5Y cells
- AMPK pathway
- diabetic neuroinflammation
- L-LDH
- THLE-2 cells
- C57BL/6J mice
- Inhibitor
- inhibitor
- inhibit