| CAS NO: | 36099-95-3 |
| 包装 | 价格(元) |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Storage | Store at -20°C |
| M.Wt | 333.3 |
| Cas No. | 36099-95-3 |
| Formula | C16H19N3O5 |
| Solubility | insoluble in EtOH; ≥14.35 mg/mL in DMSO; ≥5.76 mg/mL in H2O with ultrasonic |
| Chemical Name | L-tryptophyl-L-glutamic acid |
| Canonical SMILES | OC(CC[C@@H](C(O)=O)NC([C@@H](N)CC1=CNC2=C1C=CC=C2)=O)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 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。溶液形式一般不宜长期储存，请尽快用完。 |
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.
References:
[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).
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