Abcam, ab223886, LY2886721, BACE-1 inhibitor

Size: 5mg / 25mg
MW 390.4 Da, Purity >98%. Potent and selective BACE-1 inhibitor (IC 50 = 20.3 nM for recombinant hBACE-1). Human BACE2 is inhibited with an IC 50 of 10.2 nM. Does not inhibit other aspartyl proteases such as cathepsin D, pepsin, and renin. A potential agent to treat Alzheimer's Disease. Inhibits production of Aβ in HEK-293 Swe cells (IC 50 values are 18.5 nM and 19.7 nM for Aβ1-40 and Aβ1-42 respectively) and in PDAPP neuronal cells (IC 50 ~10 nM). Reduces dose-dependently brain levels of Aβ, C99 and sAPPβ in orally administered mouse model and plasma Aβ in dog model. Ppenetrates the blood-brain barrier.
Key facts
CAS number:1262036-50-9,
Purity:>98%,
Form:SolidSee storage information,
Molecular weight:390.4 Da,
Molecular formula:C18H16F2N4O2S,
PubChem:49837968,
Nature:Synthetic,
Solubility:Soluble in DMSO to 20 mMSoluble in Ethanol < 2 mM,
Biochemical name:N-(3-((4aS,7aS)-2-amino-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-fluoropicolinamide,
Biological description:Potent and selective BACE-1 inhibitor (IC50 = 20.3 nM for recombinant hBACE-1). Human BACE2 is inhibited with an IC50 of 10.2 nM. Does not inhibit other aspartyl proteases such as cathepsin D, pepsin, and renin. A potential agent to treat Alzheimer's Disease. Inhibits production of Aβ in HEK-293 Swe cells (IC50 values are 18.5 nM and 19.7 nM for Aβ1-40 and Aβ1-42 respectively) and in PDAPP neuronal cells (IC50 ~10 nM). Reduces dose-dependently brain levels of Aβ, C99 and sAPPβ in orally administered mouse model and plasma Aβ in dog model. Ppenetrates the blood-brain barrier.,
Canonical smiles:C1C2CSC(=NC2(CO1)C3=C(C=CC(=C3)NC(=O)C4=NC=C(C=C4)F)F)N,
Isomeric smiles:C1[C@H]2CSC(=N[C@]2(CO1)C3=C(C=CC(=C3)NC(=O)C4=NC=C(C=C4)F)F)N,
InChi:InChI=1S/C18H16F2N4O2S/c19-11-1-4-15(22-6-11)16(25)23-12-2-3-14(20)13(5-12)18-9-26-7-10(18)8-27-17(21)24-18/h1-6,10H,7-9H2,(H2,21,24)(H,23,25)/t10-,18-/m0/s1,
InChiKey:NIDRNVHMMDAAIK-YPMLDQLKSA-N,
IUPAC Name:N-[3-[(4aS,7aS)-2-amino-4,4a,5,7-tetrahydrofuro[3,4-d][1,3]thiazin-7a-yl]-4-fluorophenyl]-5-fluoropyridine-2-carboxamide

Product details:
This product is manufactured by BioVision, an Abcam company and was previously called 2299 LY2886721. 2299-25 is the same size as the 25 mg size of ab223886.

Properties and Storage Information:
Shipped at conditions-Blue Ice, Appropriate short-term storage conditions--20°C, Appropriate long-term storage conditions--20°C, Storage information-Store in the dark, Store under desiccating conditions

Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
BACE1 also known as beta-site APP cleaving enzyme 1 or beta-secretase plays an important role in the cleavage of amyloid precursor protein (APP). This cleavage results in the production of amyloid-beta peptides which are associated with Alzheimer's disease. BACE1 is a membrane-bound aspartic protease and has a molecular weight of approximately 50100 Da. The enzyme expresses mostly in the brain's neurons and some secretory tissues.
Biological function summary
BACE1 initiates the amyloidogenic pathway of APP processing which involves amyloid-beta generation. BACE1 doesn't function alone but acts as part of a complex that aids in protein substrate recognition and processing. Its activity contributes to physiological processes like myelination and axonal guidance indicating its importance beyond amyloid production.
Pathways
BACE1 is integral to the amyloidogenic pathway which is important in Alzheimer's disease development. It interacts with proteins such as presenilin 1 a part of the gamma-secretase complex that further processes the amyloid-beta precursor. Furthermore BACE1 links to synaptic functions and neural signaling pathways highlighting its multifaceted roles.
BACE1 holds significance in Alzheimer's disease due to its role in amyloid-beta peptide production. This connection has led to the development of BACE1 inhibitors as potential therapeutic agents. Additionally BACE1’s involvement in other neural functions ties it to cognitive impairments. It also relates to APP through its function in Alzheimer's suggesting targeted strategies for treatment could involve modulating BACE1 activity.