DG-041 {[allProObj[0].p_purity_real_show]}

DG-041 质控信息

DG-041 生物活性

描述

DG-041 is a potent, high affinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in binding and FLIPR assays, respectively. DG-041 inhibits the promotion of platelet aggregation by PGE2. DG-041 also crosses the blood-brain barrier[1][2].DG-041 has a weak antagonistic effect on DP1, EP1 and TP receptors with IC50 values of 131 nM, 486 nM and 742 nM, respectively[1].

DG-041 细胞实验

Cell Line human platelets LVIP2.0Zc cells human islet β-cells mouse islet β-cells vascular smooth muscle cells vascular smooth muscle cells	Concentration	Treated Time	Description	References
human platelets	1 μM		EP3 antagonist DG-041 converted platelets of nonresponders to a PGE2-responsive phenotype	Thromb Res. 2010 Jul;126(1):e23-9
LVIP2.0Zc cells	0.1 nM – 10 nM	6 h	DG-041 was found to be a high-affinity, functional antagonist of the mouse EP3 γ receptor.	Prostaglandins Other Lipid Mediat. 2019 Oct;144:106353
human islet β-cells	30 nM	4 days	To assess the effect of DG-041 on human islet β-cell proliferation, results showed that blocking EP3 increased human β-cell proliferation.	Mol Metab. 2017 Apr 5;6(6):548-559
mouse islet β-cells	30 nM	4 days	To assess the effect of DG-041 on mouse islet β-cell proliferation, results showed that blockade of EP3 enhanced β-cell proliferation in young, but not old, mouse islets.	Mol Metab. 2017 Apr 5;6(6):548-559
vascular smooth muscle cells	0.1-10 μmol/L	30 min	DG-041 dose-dependently inhibited AngII-induced intracellular Ca2+ increase	Arterioscler Thromb Vasc Biol. 2012 Dec;32(12):3024-32
vascular smooth muscle cells	1 µM	30 min	DG-041 inhibited AngII-induced phosphorylation of MLC20 and MYPT1	Arterioscler Thromb Vasc Biol. 2012 Dec;32(12):3024-32
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DG-041 动物实验

Species Male C57BL/6 mice	Animal Model Diet-induced obesity model	Administration	Dosage	Frequency	Description	References
Male C57BL/6 mice	Diet-induced obesity model	Subcutaneous injection	20 mg/kg	Twice daily for one week	DG-041 treatment effectively blocked the EP3 receptor and decreased skeletal muscle triglyceride content but had no significant effects on the diabetic phenotype.	Prostaglandins Other Lipid Mediat. 2019 Oct;144:106353
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DG-041 动物研究

Animal study

In male SpragueDawley rats, the t1/2 values of DG-041 (1.78 mg/kg i.v. and 9.62 mg/kg orally) were 2.7 h and 4.06 h, respectively, and the Cmax values of i.v. and orally were 9.46 μM and 2.74 μM, respectively. The CL for intravenous of DG-041 is 1250 ml/h/kg[1].

DG-041 参考文献

DG-041 实验方案

计算器	摩尔计算器 总药量计算器 工作液计算器
存储液制备		1mg	5mg	10mg
	1 mM 5 mM 10 mM	1.69mL 0.34mL 0.17mL	8.44mL 1.69mL 0.84mL	16.88mL 3.38mL 1.69mL

DG-041 技术信息