|Description||AZD3839, with the potential to treat Alzheimer’s disease, was reported as a selective BACE1 inhibitor (IC50=4.8μM) for which concentration-dependent lowering of Ab peptides in cellular systems and three pre-clinical species were demonstrated. Phase-I for Alzheimer's disease in United Kingdom (PO) was discontinued in 2012 in UK.|
|Synonyms||4-Fluoro-1-[3-(5-pyrimidinyl)phenyl]-1-[2-(trifluoromethyl)-4-pyridinyl]-1H-isoindol-3-amine; AZD-3839; AZD 3839;(3S)-3-(2-(difluoromethyl)pyridin-4-yl)-7-fluoro-3-(3-(pyrimidin-5-yl)phenyl)isoindolin-1-amine|
|Solubility||Soluble in DMSO, not in water|
|Quality Standard||In-house standard|
|Shelf Life||2 month in rt, long time|
RG7129, developed by Roche, inhibit BACE to treat Alzheimer's disease. Phase-I
TAK-070, under the IUPAC name 2-Naphthaleneethanamine, 6-([1,1'-biphenyl]-4-ylmethoxy)-1,2,3,4-tetrahydro-N,N-dimethyl-, hydrochloride, hydrat...
EGCG, also called Epigallocatechin gallate, under the IUPAC name [(2R,3R)-5,7-dihydroxy-2-(3,4,5-trihydroxyphenyl)-3,4-dihydro-2H-chromen-3-yl] 3,4,5-trihydroxy...
PF-05297909, is a BACE inhibitor developed by Pfizer. Phase 1
VTP-37948, also called BI 1181181, being clinically developed with Boehringer Ingelheim and Vitae Pharmaceuticals, is a is an inhibitor targeted to the catalyti...
Rafabegron is a potent and selective beta3-adrenoceptor agonist.
AZD3839, with the potential to treat Alzheimer’s disease, was reported as a selective BACE1 inhibitor (IC50=4.8μM) for which concentration-dependent lowering of...
AZD3839, also called CHEMBL2177913, as a a potent BACE1 inhibitor it is a clinical candidate for the treatment of Alzheimer's disease. Studies indicate that the...
HPP854, developed by High Point Pharmaceuticals, is a small molecule BACE1 protein inhibitor. Phase 1
BACE-1 Inhibitor is a potent, selective and cell-permeable inhibitor of human β-secretase (BACE-1) binding to the active site of BACE-1. It inhibits secretion o...
LY 2886721 hydrochloride
LY 2886721 hydrochloride is the first oral inhibitor of human β-secretase (BACE-1) with the potential to treat Alzheimer's Disease.
E2609, developed by Eisai Inc, is a novel, small molecule, BACE1 inhibitor that has been shown in nonclinical studies to inhibit the production of Aβ40 and Aβ42...
An inhibitor of β-site amyloid precursor protein-cleaving enzyme (BACE)
CTS-21166, the selective BACE1 inhibitor whose structure is not revealed, reduce brain Aβ levels by over 35% and plaque load by 40%. Phase 1 IC50=1.2–3.6 nM (ce...
LY2811376, under the IUPAC name (4S)-4-(2,4-difluoro-5-pyrimidin-5-ylphenyl)-4-methyl-5,6-dihydro-1,3-thiazin-2-amine, is the first orally available non-peptidi...
This active molecular is a potent BACE1 inhibitor that is a potential target for the treatment of Alzheimer's disease. AMG-8718 produced significantly reduction...
LY2886721, under the IUPAC name N-(3-(2-amino-4a,5,7,7a-tetrahydro-4H-furo(3,4-d)(1,3)thiazin-7a-yl)-4-fluorophenyl)-5-fluoropicolinamide, is the first oral sma...
Lanabecestat, also referred to AZD3293,is an orally active and highly permeable potent inhibitor of human β-secretase 1 in clinical development for the treatmen...
Verubecestat, a iminothiadiazine dioxide compound, is an oral BACE1 inhibitor originated by Merck & Co. It can bind significantly to β-secretase. Verubecestat h...
AZD3293, a spiro compound, has been found to be a β-secretase inhibitor that has good blood-brain barrier penetration and could probably be significant in studi...