生物活性

DMOG (Dimethyloxaloylglycine) is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolyl hydroxylase. Prolyl 4-hydroxylase (P4H) inhibitor; inhibits hypoxia-inducible factor α (HIF-α) prolyl hydroxylase (HIF-PH). Increases levels of HIF-1α; promotes cell survival under hypoxic conditions. DMOG has been observed to upregulate hypoxia inducible factor-1α (HIF-1α) in HMEC-1 cells, attenuating redox factor 1 (REF-1). PHT cells exposed to DMOG were observed to upregulate the follistatin-like 3 (FSTL3) transcription. Attenuation of myocardial injury by DMOG was also demonstrated using a rabbit ischemia reperfusion model. In NGF deprived neurons, DMOG increased cell survival through inhibition of cytochrome c release.

体外研究

体内研究

激酶实验

细胞实验

~100 μM

动物实验

8毫克在0.5毫升生理盐水中腹腔注射

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Baader E, et al. Biochem J. 1994, 300 ( Pt 2), 525-530.
[2] Milkiewicz, M., et al. 2004. J. Physiol. 560: 21-26.
[3] Asikainen, T.M., et al. 2005. Free Radic. Biol. Med. 38: 1002-1013.
[4] Lomb, D.J., et al. 2007. J. Neurochem. 103: 1897-1906.
[5] Loboda, A., et al. 2009. Vascul. Pharmacol. 51: 133-139.
[6] Heinis, M., et al. 2010. Diabetes. 59: 662-669.

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

相关化合物库

使用AMQUAR产品发表文献后请联系我们