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Technical Data
| Formula | C17H17F2N5O3S |
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| Molecular Weight | 409.41 | CAS No. | 1286770-55-5 | |
| Solubility (25°C)* | In vitro | DMSO | 81 mg/mL (197.84 mM) | |
| Ethanol | 41 mg/mL (100.14 mM) | |||
| Water | Insoluble | |||
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* <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) is a potent and selective beta-secretase (also known as Beta-site APP-cleaving enzyme 1) inhibitor. | ||||
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| Targets |
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| 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)
References
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Selleck's Verubecestat (MK-8931) has been cited by 7 publications
| Arc-Mediated Plasticity in the Paraventricular Thalamic Nucleus Promotes Habituation to Stress [ Biol Psychiatry, 2022, 92(2):116-126] | PubMed: 35527070 |
| Arc-Mediated Plasticity in the Paraventricular Thalamic Nucleus Promotes Habituation to Stress [ Biol Psychiatry, 2022, 92(2):116-126] | PubMed: 35527070 |
| A study of protein-drug interaction based on solvent-induced protein aggregation by fluorescence correlation spectroscopy [ Analyst, 2022, 10.1039/d2an00031h] | PubMed: 35253833 |
| Prophylactic evaluation of verubecestat on disease- and symptom-modifying effects in 5XFAD mice [ Alzheimers Dement (N Y), 2022, 8(1):e12317] | PubMed: 35846156 |
| Activity-regulated cytoskeleton-associated protein (Arc/Arg3. 1)-mediated plasticity in the paraventricular thalamic nucleus promotes a fundamental adaptation to [ bioRxiv, 2021, 10.1101/2021.09.10.459826] | PubMed: None |
| 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 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.