bbb penetration

LY 344864, a specifc receptor agonist, is an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.

BuChE-IN-TM-10 (TM-10) is a potent inhibitor of butyrylcholinesterase (BuChE) with an IC50 of 8.9 nM. It effectively inhibits and disaggregates self-induced Aβ aggregation, exhibits significant antioxidant activity, and demonstrates substantial penetration through the blood-brain barrier (BBB), holding promise as a potential treatment for Alzheimer's disease.

Nav1.1 activator 1 is a highly potent activator of Nav1.1 with BBB penetration.

Flucopride (Compound 4a) acts as an acetylcholinesterase inhibitor (AChE) with an IC50 value of 24 nM and serves as a partial agonist for the human 5-HT4 receptor (5-HT4R) with a Ki of 9.6 nM for (h)5-HT4R. It promotes non-amyloidogenic processing of APP in COS-7 cells transiently expressing (h)5-HT4R with an EC50 of 23.0 nM. Flucopride is also likely to exhibit significant gastrointestinal tract (GIT) penetration and blood-brain barrier (BBB) permeability, as determined in PAMPA experiments.

NRMA-9 is an amide prodrug of small molecule nuclear receptor modulators. It shows high exposure levels in the brain, indicating good penetration of the blood-brain barrier (BBB). NRMA-9 is utilized in research related to central nervous system diseases associated with nuclear receptors, such as Alzheimer's and Parkinson's.

NRMA-I is an amide prodrug of a small molecule nuclear receptor modulator. It demonstrates high brain exposure, indicating effective blood-brain barrier (BBB) penetration. NRMA-I is useful for research into central nervous system diseases related to nuclear receptors, such as Alzheimer's and Parkinson's diseases.

PROTACMAGLdegrader-1 is an orally active PROTAC agent that simultaneously targets both monoacylglycerol lipase (MAGL) and the E3 ubiquitin ligase MDM2. It functions by degrading MAGL and inhibiting the interaction between MDM2 and p53. Additionally, PROTACMAGLdegrader-1 has partial blood-brain barrier (BBB) penetration and can induce apoptosis in glioblastoma stem cells (GSC).

GSK-3β inhibitor 9 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC 50 of 35 nM. GSK-3β inhibitor 9 exhibits good pharmacokinetic profiles including favorable BBB penetration. GSK-3β inhibitor 9 is able to be used for the research of Alzheimer's disease [1].

Compound 16 (hAChE Aβ1-42-IN-1) is a potent inhibitor targeting both hAChE and Aβ1-42 aggregation, demonstrating considerable safety in hepG2 cell lines and excellent brain-blood barrier (BBB) penetration with a broad safety margin. This compound shows promise for Alzheimer's disease (AD) research [1].

BuChE-IN-2 is an excellent inhibitor of butylcholinesterase (BuChE) with IC50 values of 1.28 μM for BuChE and 0.67 μM for NO. It inhibits Aβ aggregation, ROS formation, and Cu2+ chelation, shows proper blood-brain barrier (BBB) penetration, and is suitable for Alzheimer's disease research.