DSO-5a
DSO-5a is a potent, selective, orally active BB3 agonist. DSO-5a is a representative DMAKO-00 derivative compound. DSO-5a upregulates ppar-γ activity through BB3 and activates ERK1/2 phosphorylation. DSO-5a can be used in diabetes-related research.
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- CAS. Nr.: 2195411-63-1
- Formel: C23H24N2O7
- Molecular Weight:440.45
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Speicherung:
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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PPARγ |
DSO-5a (50 nM; 60min) induces IP-1 accumulation in hBB3-HEK cells with a pEC50 of 8.485 and a strong calcium response with a pEC50 of 7.964[1].
DSO-5a (500 nM; 60min) induces IP-1 accumulation in mBB3-HEK cells with a pEC50 of 7.262 and a strong calcium response with a pEC50 of 7.174[1].
DSO-5a (0-100 nM; 8min) causes a dose-dependent activation of ERK1/2 in hBB3-H1299 and mBB3-HEK cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:hBB3-H1299 cells
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Concentration:0, 1,10,100 nM
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Incubation Time:8 min
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Result:Caused a dose-dependent activation of ERK1/2 in hBB3-H1299 cells, which was completely blocked by Bantag-1.
DSO-5a (10 mg/kg/day; P.O.; 2-4 weeks) reduces the blood glucose concentration of diabetic db/db mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:Oral administration;30 min before glucose challenge (3 g/kg)
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Result:Showed that the change rates of AUC at 3, 10 and 30 mg/kg were 5.03, 16.42 and 28.30%, respectively.
In BB3 knockout mice, DSO-5a failed to inhibit blood glucose drift.
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Animal Model:Diabetic db/db mice[1]
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Dosage:10 mg/kg/day
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Administration:Oral administration; 2-4 weeks
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Result:After two weeks of treatment, the blood glucose excursion of db/db mice was significantly reduced.
After four weeks, fasting blood glucose levels, glycosylated serum protein (GSP), and HOMA-IR were significantly decreased in the DSO-5a treatment group.
Increased the protein expression of PPAR-gamma in white adipose tissue of db/db mice.
Chemical Information
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CAS. Nr. 2195411-63-1
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Molecular Weight 440.45
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Formel C23H24N2O7
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SMILES
C=CC(C)(C(C(C=C1OC)=C(C2=C1/C(C=C/C2=N\O)=N/O)OC)OC(C3=CC=CO3)=O)C
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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)
DSO-5a Related Classifications
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