Molecular Weight(MW): 412.53
Lanabecestat（AZD3293, LY3314814）is an oral beta-secretase 1 cleaving enzyme (BACE) inhibitor with an inhibitory constant Ki of 0.4 nM.
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Kinetic studies of known inhibitors against BACE1. a Time courses of BACE1 activity in the presence of different concentrations of AZD3839. b Time courses of BACE1 activity in the presence of different concentrations of AZD3293. c Plot of kobs as a function of inhibitor concentration for the slow binding inhibitor AZD3293. d Reversibility assays with BACE1 and inhibitors using spin column method. The data of reversibility assays were performed in duplicate.
Anal Bioanal Chem, 2017, 409(28):6635-6642. Lanabecestat（AZD3293, LY3314814） purchased from Selleck.
Purity & Quality Control
Choose Selective BACE Inhibitors
|Description||Lanabecestat（AZD3293, LY3314814）is an oral beta-secretase 1 cleaving enzyme (BACE) inhibitor with an inhibitory constant Ki of 0.4 nM.|
Lanabecestat（AZD3293, LY3314814）is a potent, highly permeable, orally active, blood-brain barrier (BBB) penetrating, BACE1 inhibitor with unique slow off-rate kinetics. When the potency of AZD3293 with respect to secretion of Aβ40 and sAβPPβ is studied in a range of cellular models, the compound displays pM potency in primary neuron cultures from mice and guinea pigs and in SH-SY5Y cells over-expressing AβPP (IC50 = 610 pM, 310 pM, and 80 pM, respectively). AZD3293 is also tested in a panel of more than 350 in vitro radioligand binding and enzyme activity assays, covering a diverse range of receptors, ion channels, transporters, kinases, and enzymes, up to a concentration of 10μM of AZD3293. A few significant responses are observed, but these had at least a 1,000-fold selectivity against BACE1, thus indicating specificity to BACE1. The off-rate of AZD3293 has an estimated t1/2 of approximately 9 h.
|In vivo||In vivo in mice, guinea pigs, and dogs, AZD3293 displays significant dose- and time-dependent reductions in plasma, cerebrospinal fluid, and brain concentrations of Aβ40, Aβ42, and sAβPPβ. In the dog PK study, the bioavailability of AZD3293 is determined to be 80% (F = 0.8). The preclinical data strongly support the clinical development of AZD3293, and patients with AD are currently being recruited into a combined Phase 2/3 study to test the disease-modifying properties of AZD3293.|
|In vitro||DMSO||82 mg/mL (198.77 mM)|
|Ethanol||82 mg/mL (198.77 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03499041||Withdrawn||Drug: LY3314814||Hepatic Impairment||Eli Lilly and Company|AstraZeneca||June 2018||Phase 1|
|NCT03222427||Completed||Drug: LY3314814|Drug: [13C415N3] LY3314814||Healthy||Eli Lilly and Company|AstraZeneca||January 15 2018||Phase 1|
|NCT03019549||Completed||Drug: Lanabecestat|Drug: Rosuvastatin||Healthy||Eli Lilly and Company|AstraZeneca||January 12 2017||Phase 1|
|NCT02663128||Completed||Drug: Lanabecestat||Healthy||Eli Lilly and Company|AstraZeneca||January 2016||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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