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G3335
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
G3335图片
CAS NO:36099-95-3
规格:98%
分子量:333.3
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
PPARγ antagonist
CAS:36099-95-3
分子式:C16H19N3O5
分子量:333.3
纯度:98%
存储:Store at -20°C

Background:

Kd = 8.34 μM


G3335 is a PPARγ antagonist.


The peroxisome proliferator-activated receptor gamma (PPARgamma) is a key therapeutic drug target for several conditions, such as inflammation, diabetes, hypertension, dyslipidemia, and cancer.


In vitro: Biacore 3000 study based on the surface plasmon resonance technique found that G3335 exhibited a highly specific binding affinity against PPARgamma and was able to block rosiglitazone, a potent PPARgamma agonist, in the stimulation of the interaction between the PPARgamma ligand-binding domain (LBD) and RXRalpha-LBD. Moreover, the yeast two-hybrid assays indicated that G3335 had strong antagonistic activity in perturbing rosiglitazone in the promotion of the PPARgamma-LBD-CBP interaction. In addition, G3335 could competitively bind to PPARgamma against 0.1 microM rosiglitazone to repress reporter-gene expression [1].


In vivo: In a previous study, the effect of rosiglitazone was examined on spinal cord injury (SCI) in rats. The animals were randomly divided into vehicle group, rosiglitazone treated group, and G3335 treated group. Locomotor function recovery was evaluated. Results showed that compared with the vehicle groups, the rosiglitazone could significantly ameliorate locomotor recovery, reduce NF-κB expression, and increase the proliferation of endogenous NPCs. In addition, when the PPAR-γ antagonist G3335 was applied, such effects were abolished [2].


Clinical trial: So far, no clinical study has been conducted.


参考文献:
[1] Ye, F. ,Zhang, Z.S.,Luo, H.B., et al. The dipeptide H-Trp-Glu-OH shows highly antagonistic activity against PPARγ: Bioassay with molecular modeling simulation. ChemBioChem 7, 74-82 (2006).
[2] Meng, Q. Q.,Liang, X.J.,Wang, P., et al. Rosiglitazone enhances the proliferation of neural progenitor cells and inhibits inflammation response after spinal cord injury. Neuroscience Letters 503, 191-195 (2011).