SNT-207858 free base is a selective, blood brain barrier penetrating, potent and orally active antagonist of melanocortin-4 (MC-4) receptor(IC50 of 22 nM (binding) and 11 nM (function), on the MC-4 receptor).
SNT-207858 is a selective, blood brain barrier penetrating, potent and orally active antagonist of melanocortin-4 (MC-4) receptor. SNT207858 has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor.
Q134R, a neuroprotective hydroxyquinoline derivative that suppresses nuclear factor of activated T cell (NFAT) signaling. Q134R can across blood-brain barrier. Q134R has the potential for Alzheimer’s disease (AD) and aging-related disorders research[1]. Q134R (1-10 μM) suppresses NFAT signaling, without inhibiting calcineurin activity. Q134R partially inhibits NFAT activity in primary rat astrocytes, but does not prevent calcineurin-mediated dephosphorylation of a non-NFAT target, either in vivo, or in vitro[1]. Q134R (4 mg kg; orally gavage; twice per day; for 7 days) treatment improves cognitive function in rodent models of AD‐like pathology[1]. [1]. Pradoldej Sompol, et al. Q134R: Small chemical compound with NFAT inhibitory properties improves behavioral performance and synapse function in mouse models of amyloid pathology. Aging Cell. 2021 Jul;20(7):e13416.
The metallo-protein Cu/Zn-superoxide dismutase (SOD1) is a ubiquitous enzyme responsible for scavenging superoxide radicals. Mutations in SOD1, which alter its metal binding capacity and can result in protein misfolding and aggregation, have been linked to familial amyotrophic lateral sclerosis (ALS). Cu-ATSM is an orally bioavailable, blood-brain barrier permeable complex that has traditionally been used in cellular imaging experiments to selectively label hypoxic tissue via its susceptibility to reduction by oxygen-depleted mitochondria. More recently, Cu-ATSM has been reported to improve locomotor function and survival in a transgenic ALS mouse model by delivering copper specifically to cells in the spinal cords of mice producing misfolded SOD1 proteins. Copper chaperone for SOD (CCS) is presumed to utilize the copper from Cu-ATSM to prevent misfolding of the SOD1 protein.
The endocannabinoids, 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide (AEA), are biologically active lipids that regulate diverse neurological and metabolic functions by activating the cannabinoid receptors, central cannabinoid (CB1) and peripheral cannabinoid (CB2). Monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH) hydrolyze 2-AG and AEA, respectively, thus terminating their biological function. IDFP is an organophosphorus compound that dually inhibits MAGL and FAAH with IC50 values of 0.8 and 3 nM, respectively. At 10 mg/kg, IDFP elevates brain levels of 2-AG and AEA more than 10-fold, and decreases levels of arachidonic acid by a similar magnitude.