09.10.2015

Three new Neuroscience small molecules – only at REAGENCY

AUTEN-67 MTMR14 inhibitor (RGNCY-0046)

AUTEN-67 is a specific inhibitor of MTMR14, a myotubularin-related phosphatase antagonizing the formation of autophagic membrane structures.  It significantly increases autophagic flux in cell lines and in vivo models. AUTEN-67 promotes longevity and protects neurons from undergoing stress-induced cell death. It also restores nesting behavior in a murine model of Alzheimer disease,without apparent side effects. Therefore, AUTEN-67 can be used as a potent drug candidate to decelerate the aging process and counter various age-dependent degenerative diseases.
 



LDDN-0003499 Src inhibitor (RGNCY-0045)

LDDN-0003499 is a novel small molecule Src family tyrosine kinase inhibitor with anti-inflammatory effects in response to Aβ stimulation of microglia. It produced a dose dependent decrease in basal levels of active, phosphorylated Src and Lyn in BV2 cells (microglial cell line). LDDN-0003499 treatment also attenuated the Aβ-stimulated increase in active, phosphorylated levels of Lyn/Src and TNFα and IL-6 secretion.  This compound also has properties that suggest oral availability and blood brain barrier penetration.  Furthermore, in vitro/in vivo characterization of LDDN-0003499 as well as structural modification may provide a new tool for attenuating microglial-mediated brain inflammatory conditions such as that occurring in AD.
 



TBTC RXR alpha agonist (RGNCY-0044)

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.
 



Reagency is a company started by scientists, aimed at tackling the issues sourcing cutting-edge research compounds currently in  the literature. They provide a way to purchase such custom made compounds without the extortionate bills. Members submit the compounds they want made, and through Reagency they share the cost of synthesis.

Please visit their website to see the current batch of cutting-edge compounds. If you don’t see what you want, submit a request and they will add it to their site and offer it to the Reagency community so everyone can share the cost of synthesis.
 



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