DG-041
目录号: PL10154 纯度: ≥99%
CAS No. :861238-35-9
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中文名称
DG-041
英文名称
DG-041
英文别名
DG-041;3-[1-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methylindol-7-yl]-N-(4,5-dichlorothiophen-2-yl)sulfonylprop-2-enamide
Cas No.
861238-35-9
分子式
C23H15N2O3FS2Cl4
分子量
592.32
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
DG-041 是一种有效,高亲和力,选择性的 EP3 受体拮抗剂,在结合和 FLIPR 试验中,IC50 分别为 4.6 nM 和 8.1 nM。DG-041 抑制 PGE2 促进血小板聚集。DG-041 可以穿过血脑屏障。
生物活性
DG-041 is a potent, high affinity and selective EP 3 receptor antagonist with IC 50 s of 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively. DG-041 inhibits PGE2 facilitation of platelet aggregation. DG-041 crosses the blood-brain barrier.
性状
Solid
IC50 & Target[1][2]
EP3 4.6-8.1 nM (IC50)
体外研究(In Vitro)
DG-041 was a less potent antagonist of the DP1 (IC50=131 nM), EP1 (IC50=486 nM), and TP receptors (IC50=742 nM). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
DG-041 (1.78 mg/kg for intravenous or 9.62 mg/kg for oral) has t 1/2 of 2.7 hours, 4.06 hours and C max of 9.46 μM, 2.74 μM for intravenous and oral administration, respectively. DG-041 has CL of 1250 mL/h/kg for intravenous. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Singh J, et al. Antagonists of the EP3 receptor for prostaglandin E2 are novel antiplatelet agents that do not prolong bleeding. ACS Chem Biol. 2009 Feb 20;4(2):115-26.
[2]. Hategan G, et al. Heterocyclic 1,7-disubstituted indole sulfonamides are potent and selective human EP3 receptorantagonists. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6797-800.
溶解度数据
In Vitro: DMSO : 250 mg/mL (422.07 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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