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| Size | Price | Stock |
|---|---|---|
| 5mg | $100 | 3-6 Days |
| 10mg | $150 | 3-6 Days |
| 25mg | $240 | 3-6 Days |
| 50mg | $430 | 3-6 Days |
| 100mg | $600 | 3-6 Days |
| 250mg | $950 | 3-6 Days |
| 500mg | $1450 | 3-6 Days |
: Cat #: V2793 CAS #: 2095432-65-6 Purity ≥ 98%
Description: Verubecestat TFA (also known as MK-8931; SCH-900931), the trifluoroacetic acid salt form of MK-8931, is a beta-secretase 1 and BACE1 inhibitor with anti-AD (Alzheimer's disease) activity. It is in Phase 3 clinical trial for treatment of Alzheimer's disease. Amyloidogenic pathway in Alzheimer's disease (AD) involves breakdown of APP by β-secretase followed by γ-secretase and results in formation of amyloid beta plaque. β-secretase has been a promising target for developing novel anti-Alzheimer drugs.MK-8931 binds significantly to β-secretase. target: BACE1. In vitro:MK-8931 can effectively reduce Aβ40 in cells with a Ki of 7.8 nM and an IC50 of 13 nM. Docking revealed that, with respect to their free binding energy, acylguanidine 7a has the lowest binding energy followed by MK-8931 and pioglitazone and binds significantly to β-secretase.
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- Related Biological Data
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- Quality Control Documentation
| Molecular Weight (MW) | 523.43 |
|---|---|
| Molecular Formula | C19H18F5N5O5 |
| CAS No. | 2095432-65-6 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 81 mg/mL (154.74 mM) |
| Water: <1 mg/mL | |
| Ethanol: 2 mg/mL (3.82 mM) | |
| Synonyms | MK-8931 TFA; SCH 900931; MK 8931 trifluoroactice acid; SCH-900931; MK8931; MK-8931-009; SCH900931 TFA |
| Protocol | In Vitro | In vitro activity: Verubecestat(MK-8931) effectively reduces Aβ40 in cells with a Ki of 7.8 nM and an IC50 of 13 nM Kinase Assay: Verubecestat (MK-8931) is a beta-secretase 1/BACE1 inhibitor under investigation for the treatment of Alzheimer's Disease. |
|---|---|---|
| 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. | |
| Animal model | Rats and cynomolgus monkeys |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.9105 mL | 9.5524 mL | 19.1048 mL | 38.2095 mL |
| 5mM | 0.3821 mL | 1.9105 mL | 3.8210 mL | 7.6419 mL |
| 10mM | 0.1910 mL | 0.9552 mL | 1.9105 mL | 3.8210 mL |
| 20mM | 0.0955 mL | 0.4776 mL | 0.9552 mL | 1.9105 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.