2. Metabolic Enzyme/Protease
  3. MMP
  4. 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.

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

F81-1144b

F81-1144b Chemical Structure

CAS No. : 306733-22-2

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F81-1144b Related Antibodies

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Description

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[1].

IC50 & Target[1]

MMP-1

5 nM (IC50)

MMP-3

27 nM (IC50)

In Vivo

F81-1144b (50-100 mg/kg; s.c.; once daily; 7 days) dose-dependently reduces serum and hepatic triacylglycerol levels in HSD-induced hypertriglyceridemic rats, with the 100 mg/kg dose normalizing serum TAG, cholesterol, glucose, and insulin levels, and suppressing VLDL-TAG secretion by 45%[1].

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

Animal Model: Wistar rats (7-week-old male; high-sucrose diet-induced hypertriglyceridemia)[1]
Dosage: 50 mg/kg; 100 mg/kg
Administration: s.c.; once daily; 7 days
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.
Molecular Weight

483.60

Formula

C27H37N3O5
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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F81-1144b Related Classifications

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Keywords:

F81-1144b306733-22-2MMPMatrix metalloproteinasesglucosevery low density lipoprotein-triacylglycerolinsulintriacylglycerolcarbohydrate response element-binding proteinMMP-3sterol regulatory element-binding protein-1cMMP-1uncoupling protein 2fatty acid synthesisInhibitorinhibitorinhibit

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