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DMOG

现货
Catalog No.
A4506
细胞通透的竞争性HIF-PH抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 800.00
现货
50mg
¥ 600.00
现货
100mg
¥ 1,000.00
现货
200mg
¥ 1,800.00
现货

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Background

IC50: 9.3 and 3.7 μM for hydroxyproline synthesis inhibition of embryonic chicken lung extracted from tissue and culture medium [1].

Dimethyloxalylglycine (DMOG) is an inhibitor of prolyl-4-hydroxylase domain (PHD) enzymes that regulate the stability of hypoxia-inducible factor (HIF). Localized tissue hypoxia is a feature of infection and inflammation, leading to the upregulation of the transcription factors HIF-1α and NF-κB via inhibition of oxygen sensing hydroxylase enzymes.

In vitro: DMOG acts to stabilize HIF-1a expression under normal oxygen tension in cultured cells at concentrations from 0.1 to 1 mmol/L [2].

In vivo: Pre-treatment with DMOG attenuates systemic LPS-induced activation of the NF-κB pathway. Furthermore, mice treated with DMOG had significantly increased survival in LPS-induced shock. In addition, in vivo DMOG treatment upregulates the expression of IL-10, specifically in the peritoneal B-1 cell population [3].

Clinical trial: Currently no clinical data are available.

References:
[1] Baader E, Tschank G, Baringhaus KH, Burghard H, Günzler V.  Inhibition of prolyl 4-hydroxylase by oxalyl amino acid derivatives in vitro, in isolated microsomes and in embryonic chicken tissues. Biochem J. 1994 Jun 1;300 ( Pt 2):525-30.
[2] Jaakkola P, Mole DR, Tian YM, Wilson MI, Gielbert J, Gaskell SJ, von Kriegsheim A, Hebestreit HF, Mukherji M, Schofield CJ, Maxwell PH, Pugh CW, Ratcliffe PJ.  Targeting of HIF-alpha to the von Hippel-Lindau ubiquitylation complex by O2-regulated prolyl hydroxylation. Science. 2001 Apr 20;292(5516):468-72.
[3] Hams E, Saunders SP, Cummins EP, O'Connor A, Tambuwala MT, Gallagher WM, Byrne A, Campos-Torres A, Moynagh PM, Jobin C, Taylor CT, Fallon PG.  The hydroxylase inhibitor dimethyloxallyl glycine attenuates endotoxic shock via alternative activation of macrophages and IL-10 production by B1 cells. Shock. 2011 Sep;36(3):295-302.

Chemical Properties

StorageStore at -20°C
M.Wt175.14
Cas No.89464-63-1
FormulaC6H9NO5
Solubility≥8.75mg/mL in DMSO, ≥17.8 mg/mL in EtOH with ultrasonic, ≥34.47 mg/mL in H2O with ultrasonic
Chemical Namemethyl 2-[(2-methoxy-2-oxoethyl)amino]-2-oxoacetate
SDFDownload SDF
Canonical SMILESCOC(=O)CNC(=O)C(=O)OC
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

B1细胞

溶解方法

该化合物在DMSO中的溶解度大于8.8 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

1 mM,2 hours

应用

在腹膜M中DMOG上调磷酸化p50(S337)。

动物实验 [1]:

动物模型

BALB/c和C57BL/6小鼠

给药剂量

8 mg/mouse,腹腔注射

应用

LPS诱导休克后,DMOG明显增加生存率。在腹膜B-1细胞中,DMOG上调了IL-10的表达。手术前接受DMOG治疗的小鼠产生疾病症状的严重恶化,死亡率明显升高。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Hams E, Saunders S P, Cummins E P, et al. The hydroxylase inhibitor DMOG attenuates endotoxic shock via alternative activation of macrophages and IL-10 production by B-1 cells[J]. Shock (Augusta, Ga.), 2011, 36(3): 295.

生物活性

描述 DMOG是细胞通透的竞争性HIF-PH抑制剂。
靶点 HIF-PH          
IC50            

质量控制

化学结构

DMOG