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  3. DSO-5a

DSO-5a 是一种有效的、选择性的、具有口服活性的 BB3 激动剂。DSO-5a 是一种具有代表性的 DMAKO-00 衍生物化合物。DSO-5a 可通过 BB3 上调 ppar-γ 活性,激活ERK1/2 磷酸化。DSO-5a 可用于糖尿病相关研究。

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DSO-5a Chemical Structure

DSO-5a Chemical Structure

CAS No. : 2195411-63-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target[1]

PPARγ

 

体外研究
(In Vitro)

DSO-5a (50 nM; 60min) 在 hBB3-HEK 细胞中诱导 IP-1 积累,pEC50 值为 8.485,引起强烈的钙反应的 pEC50 值为 7.964[1]
DSO-5a (500 nM; 60min) 在 mBB3-HEK 细胞中诱导 IP-1 积累,pEC50 值为 7.262,引起强烈的钙反应的 pEC50 值为 7.174[1]
DSO-5a (0-100 nM; 8min) 在 hBB3-H1299 和 mBB3-HEK 细胞中引起 ERK1/2 的剂量依赖性激活[1]

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

Western Blot Analysis[1]

Cell Line: hBB3-H1299 cells
Concentration: 0, 1,10,100 nM
Incubation Time: 8 min
Result: Caused a dose-dependent activation of ERK1/2 in hBB3-H1299 cells, which was completely blocked by Bantag-1.
体内研究
(In Vivo)

DSO-5a (3-30 mg/kg; P.O.; 30 分钟) 在 C57BL/6 小鼠中以剂量依赖性方式降低血糖波动[1]
DSO-5a (10 mg/kg/day; P.O.; 2-4 周) 可以降低糖尿病 db/db 小鼠血糖浓度[1]

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

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.
分子量

440.45

Formula

C23H24N2O7

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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