Verubecestat (MK-8931) Trifluoroacetate

Catalog No.S8173 Batch:S817304

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Technical Data

Formula

C19H18F5N5O5S
Molecular Weight 523.43 CAS No. 2095432-65-6
Solubility (25°C)* In vitro DMSO 100 mg/mL (191.04 mM)
Ethanol 18 mg/mL (34.38 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Verubecestat (MK-8931) Trifluoroacetate is a potent and selective beta-secretase inhibitor and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor.
Targets
BACE2 [1]
(Cell-free assay)		 BACE1 [1]
(Cell-free assay)
0.37 nM(Ki) 1.75 nM(Ki)
In vitro Verubecestat(MK-8931) effectively reduces Aβ40 in cells with a Ki of 7.8 nM and an IC50 of 13 nM[2].
In vivo Verubecestat(MK-8931) dramatically lowers CSF and cortex Aβ40 in both rats and cynomolgus monkeys following a single oral dose. Due to the 20 h half-life of MK-8931 it is ideal for once-a-day dosing[2].

Protocol (from reference)

Selleck's Verubecestat (MK-8931) Trifluoroacetate has been cited by 11 publications

A study of protein-drug interaction based on solvent-induced protein aggregation by fluorescence correlation spectroscopy [ Analyst, 2022, 10.1039/d2an00031h] PubMed: 35253833
Improving Preclinical to Clinical Translation in Alzheimer's Disease Research [ Alzheimers Dement (N Y), 2020, 6(1):e12038] PubMed: 32548237
Pharmacokinetic, Pharmacodynamics, and Transcriptomics Analysis of Verubecestat Treatment in 5XFAD mice [ Alzheimer's Association, 2020, 16-S2] PubMed: None
Inhibition of BACE1 Facilitates Macrophage-based Immunotherapy to Suppress Malignant Growth of Glioblastoma [ Research Square, 2020, 10.21203/rs.3.rs-61939/v1] PubMed: None
Aβ34 is a BACE1-derived degradation intermediate associated with amyloid clearance and Alzheimer's disease progression. [ Nat Commun, 2019, 10(1):2240] PubMed: 31110178
Multiple BACE1 inhibitors abnormally increase the BACE1 protein level in neurons by prolonging its half-life. [ Alzheimers Dement, 2019, 15(9):1183-1194] PubMed: 31416794
Ablation of amyloid precursor protein increases insulin-degrading enzyme levels and activity in brain and peripheral tissues. [ Am J Physiol Endocrinol Metab, 2019, 316(1):E106-E120] PubMed: 30422705
Critical Evaluation of the Pharmacokinetics of Verubecestat in Aged 5XFAD Mice [ Alzheimer's Association, 2019, 15-7S-25] PubMed: None
Distinct apoptotic blocks mediate resistance to panHER inhibitors in HER2+ breast cancer cells [Karakas B Biochim Biophys Acta Mol Cell Res, 2018, 1865(8):1073-1087] PubMed: 29733883
HIV-1 counteracts an innate restriction by amyloid precursor protein resulting in neurodegeneration. [ Nat Commun, 2017, 8(1):1522] PubMed: 29142315

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.