RGNCY-0044 (TBTC RXR alpha agonist )
TBTC, a thiophene derivative, is a selective agonist of retinoid X receptor α (RXRα). It can effectively activate the heterodimerization of RXRα, with either liver X receptor α (LXRα) or peroxisome proliferator activated receptor γ (PPARγ), stimulate the expressions of the genes of apoE, ABCA1and ABCG1, and decrease Aβ content both in cells and animal models. In addition, administration of TBTC (30mg/kg/day) in the transgenic APP–PS1 mice could also reduce the formation of senile plaques and improve the daily living activity of the mice. Thus, TBTC may be a potential drug lead compound for the treatment of AD. RXRαLBD KD = 8.86 μM.
Systematic Name: methyl 2-amino-6-(tert-butyl)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylate
Reference: Yanyan Sun, Jun Fan et al. Small molecule TBTC as a new selective retinoid X receptor alpha agonist improves behavioural deficit in Alzheimer's disease model mice. Eur J Pharmacol (2015). 762:202-213.
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Tags: Alzheimer’s, Alzheimers, Alzheimer, RGNCY-0044, TBTC, RXR, Retinoid, LXR, Perosxisome, PPAR, apoE, ABCA, ABCG