1227163-56-5 Usage
Biological Activity
azd3839 is a novel inhibitor of bace1 with ic50 value of 4.8μm [1].azd3839 has been reported to inhibit human bace1 activity in a biochemical fret assay. in addition, azd3839 has also been reported to inhibit the release of sappβs from human sh-sy5y cells, mouse n2a cells and mouse and guinea pig primary cortical neurons. moreover, azd3839 has been revealed to effectively decrease the cerebrospinal fluid (csf), plasma, and brain aβ levels in guinea pig, mouse and non-human primate. azd3839 has also been revealed to decrease the levels of aβ40 secreted from c57bl/6 mouse primary cortical neurons, n2a cells (mouse neuroblastoma), and dunkin-hartley guinea pig primary cortical neurons, with ic50 values of 50.9, 32.2, and 24.8 nmol/liter, respectively [2].
references
[1] sparve e1, quartino al1, luttgen m1, tunblad k1, teiling-gardlund a1, falting j1, alexander r1, kagstrom j1, sjodin l1, bulgak a1, al-saffar a1, bridgland-taylor m2, pollard c3, swedberg md4, vik t5, paulsson b1. prediction and modeling of effects on the qtc interval for clinical safety margin assessment, based on single ascending dose study data with azd3839. j pharmacol exp ther. 2014 jun 10.[2] jeppsson f1, eketj?ll s, janson j, karlstr?m s, gustavsson s, olsson ll, rades?ter ac, ploeger b, cebers g, kolmodin k, swahn bm, von berg s, bueters t, f?lting j. discovery of azd3839, a potent and selective bace1 inhibitor clinical candidate for the treatment of alzheimer disease. j biol chem. 2012 nov 30;287(49):41245-57.
Check Digit Verification of cas no
The CAS Registry Mumber 1227163-56-5 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,2,7,1,6 and 3 respectively; the second part has 2 digits, 5 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1227163-56:
(9*1)+(8*2)+(7*2)+(6*7)+(5*1)+(4*6)+(3*3)+(2*5)+(1*6)=135
135 % 10 = 5
So 1227163-56-5 is a valid CAS Registry Number.
1227163-56-5Relevant articles and documents
NEW COMPOUNDS 578
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Page/Page column 40, (2010/06/13)
The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
