RGNCY-0044 (TBTC RXR alpha agonist )

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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.

SMILES: CC(C)(C)C(C1)CCC2=C1SC(N)=C2C(OC)=O

Systematic Name: methyl 2-amino-6-(tert-butyl)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylate

Formula: C14H21NO2S

MWT: 267.39

PMID: 26026644

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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