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ChemicalBook CAS DataBase List 2195411-63-1

2195411-63-1 Structure

2195411-63-1

Name	DSO-5a
CAS	2195411-63-1

Synonyms

DSO-5a

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Hazard Information

Uses

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[1].

in vivo

DSO-5a (3-30 mg/kg; P.O.; 30 min) reduces blood glucose excursions in a dose-dependent manner in C57BL/6 mice^[1].
DSO-5a (10 mg/kg/day; P.O.; 2-4 weeks) reduces the blood glucose concentration of diabetic db/db mice^[1].

Animal Model:	C57BL/6 mice^[1]
Dosage:	3 mg/kg; 10 mg/kg; 30 mg/kg
Administration:	Oral administration;30 min before glucose challenge (3 g/kg)
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.

Animal Model:	Diabetic db/db mice^[1]
Dosage:	10 mg/kg/day
Administration:	Oral administration; 2-4 weeks
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.

IC 50

PPARγ

References

[1] Wu L, et al. Discovery of Dimethyl Shikonin Oxime 5a, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Type 2 Diabetes Mellitus. J Med Chem. 2023 Jun 22;66(12):8011-8029. DOI:10.1021/acs.jmedchem.3c00323

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