F81-1144b
F81-1144b is a MMP-1 and MMP-3 inhibitor with IC50 values of 5 nM and 29 nM, respectively. F81-1144b reduces serum and hepatic triacylglycerol levels, decreases the secretion of very-low-density lipoprotein-triacylglycerol, inhibits de novo hepatic fatty acid synthesis, and lowers serum insulin and glucose levels. F81-1144b can be used for the research of hypertriglyceridemia.
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- CAS No.: 306733-22-2
- Formule: C27H37N3O5
- Masse moléculaire:483.60
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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
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Activité biologique
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MMP-1 5 nM (IC50) |
MMP-3 27 nM (IC50) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (7-week-old male; high-sucrose diet-induced hypertriglyceridemia)[1]
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Dosage:50 mg/kg; 100 mg/kg
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Administration:s.c.; once daily; 7 days
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Result:Reduced serum TAG levels in a dose-dependent manner, with 100 mg/kg restoring levels to normal diet-fed control values.
Reduced serum cholesterol levels in a dose-dependent manner, with 100 mg/kg restoring levels to normal diet-fed control values.
Returned slightly elevated serum glucose levels to normal values at both 50 mg/kg and 100 mg/kg.
Markedly reduced HSD-elevated serum insulin levels.
Significantly reduced hepatic TAG levels in a dose-dependent manner; did not significantly change hepatic phospholipid levels.
Significantly suppressed hepatic de novo fatty acid synthesis at 100 mg/kg.
Significantly decreased HSD-elevated microsomal glycerol-3-phosphate acyltransferase (GPAT) activity at 100 mg/kg.
Upregulated hepatic gene expression of Lpl, Cd36, Apoa1, Ucp2 in a dose-dependent manner.
Chemical Information
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CAS No. 306733-22-2
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Masse moléculaire 483.60
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Formule C27H37N3O5
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SMILES
O=C([C@H](CC1=CC=C(C=C1)CN)NC([C@@H]([C@H](CCCC2=CC=CC=C2)C(NO)=O)CC(C)C)=O)O
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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)
F81-1144b Related Classifications
HY-125507 Related Classifications
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