(Z)-PUGNAc是一种有效的 O-GlcNAcase 抑制剂，较 E 型 O-GlcNAcase 抑制剂更具效能。
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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
To investigate the effect of PUGNAc on Akt1 glycosylation and phosphorylation. Results showed that PUGNAc treatment led to accumulation of O-GlcNAc proteins and caused hypophosphorylation of Akt T308.
Nat Cell Biol. 2010 Sep;12(9):876-85
Neonatal rat cardiac myocytes (NRCMs)
200 µM
overnight
Inhibition of O-GlcNAcase activity, increased O-GlcNAc levels, and reduced post-hypoxic cardiac myocyte death
Circ Res. 2009 Jan 2;104(1):41-9
vascular smooth muscle cells (VSMCs)
100 μM
24 h
To investigate the effect of PugNAc on vascular reactivity to phenylephrine. PugNAc increased vascular reactivity to phenylephrine, which was abolished by the Rho kinase inhibitor Y-27632
Cardiovasc Res. 2011 Feb 15;89(3):614-22
3T3-L1 adipocytes
100 μM
16 h
Increased O-GlcNAc levels by inhibiting O-GlcNAcase, leading to insulin resistance
Proc Natl Acad Sci U S A. 2002 Apr 16;99(8):5313-8
human retinal micro vascular endothelial cells (HRECs)
200 µM
12 h
To investigate the association between O-GlcNAcylation and ROS generation, it was found that PUGNAc significantly attenuated the production of ROS (P<0.01) and increased the expression levels of antioxidant genes SOD and GPX.
Int J Mol Med. 2015 Oct;36(4):1019-27
(Z)-PUGNAc 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
K18 Gly− transgenic mice
Intraperitoneal injection
7 mg/kg
Fas antibody injection after 48 hours
To investigate the effect of combined PUGNAc and Fas treatment on K18 Gly? mice. Results showed that K18 Gly? mice were more susceptible to PUGNAc/Fas-induced injury, with increased liver hemorrhage, apoptosis, and decreased Akt1 T308 phosphorylation.
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