G3335

G3335

Catalog Number:
L002373209APE
Mfr. No.:
APE-C5435
Price:
$244
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          Background

          Kd = 8.34 μMG3335 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.

          [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).

      • Properties
        • Categories
          PPARγ antagonist
          Alternative Name
          L-tryptophyl-L-glutamic acid
          CAS Number
          36099-95-3
          Molecular Formula
          C16H19N3O5
          Molecular Weight
          333.3
          Purity
          98.00%
          Solubility
          insoluble in EtOH; ≥14.35 mg/mL in DMSO; ≥5.76 mg/mL in H2O with ultrasonic
          Storage
          Store at -20°C
          SMILES
          OC(CC[[email protected]@H](C(O)=O)NC([[email protected]@H](N)CC1=CNC2=C1C=CC=C2)=O)=O

          * For Research Use Only

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