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G3335

Cat. No. M8539

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G3335 Structure

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Quality Control & Documentation
Biological Activity

G3335 ( L-tryptophyl-L-glutamic acid) is a cell-permeable dipeptide that acts as a selective and reversible PPARγ antagonist with a Kd value of 8.34 μM for PPARγ and much lower activity at other PPAR subtypes. G3335 reversibly and competitively blocks activation of PPARγ by the PPARγ agonist rosiglitazone, and conversely, in rat astrocyte culture higher levels of rosiglitazone reduced harmful effects induced by G3335. At higher concentration G3335 may act as a PPARα agonist, interacting with the PPARα ligand binding domain with a KD of 120 μM. G3335 is reported to reduce hepatic lipid accumulation in lipid-loaded hepatocytes by activation of PPARα.

Chemical Information
Molecular Weight 333.34
Formula C16H19N3O5
CAS Number 36099-95-3
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Letizia Giampietro, et al. PPAR-γ agonist GL516 reduces oxidative stress and apoptosis occurrence in a rat astrocyte cell line

[2] Bolong Zheng, et al. Melatonin alleviates acute spinal cord injury in rats through promoting on progenitor cells proliferation

[3] Matteo Zanardelli, et al. Oxaliplatin neurotoxicity involves peroxisome alterations. PPARγ agonism as preventive pharmacological approach

[4] Lorenzo Di Cesare Mannelli, et al. PPAR- γ impairment alters peroxisome functionality in primary astrocyte cell cultures

[5] Fei Ye, et al. The dipeptide H-Trp-Glu-OH shows highly antagonistic activity against PPARgamma: bioassay with molecular modeling simulation

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