1. Neuronal Signaling
  2. Beta-secretase
  3. Verubecestat

Verubecestat (Synonyms: MK-8931)

Cat. No.: HY-16759 Purity: 99.69%
Handling Instructions

Verubecestat (MK-8931) is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat effectively reduces Aβ40 and has the potential for Alzheimer's Disease.

For research use only. We do not sell to patients.

Verubecestat Chemical Structure

Verubecestat Chemical Structure

CAS No. : 1286770-55-5

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Based on 1 publication(s) in Google Scholar

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Description

Verubecestat (MK-8931) is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat effectively reduces Aβ40 and has the potential for Alzheimer's Disease[1][2].

IC50 & Target

Ki: 2.2 nM (BACE1) and 0.38 nM (BACE2)[1]

In Vitro

Verubecestat (MK-8931) is a β-site amyloid precursor protein cleaving enzyme 1/2 (BACE1/2) inhibitor. Verubecestat does not significantly inhibit human CYP isoforms 1A2, 2C9, 2C19, 2D6, and 3A4 (all IC50>40 μM), indicating that the compound is unlikely to be a perpetrator of CYP-mediated drug-drug interactions[1].
Verubecestat has IC50s of 2.1 nM, 0.7 nM, 4.4 nM for Aβ1-40, Aβ1-42, sAPPβ in HEK293 APPSwe/Lon cells[1].

In Vivo

Verubecestat (MK-8931; 3 mg/kg; IV or oral) has a T1/2 of 1.9 hours, a CL of 46 mL/min/kg, a Vss of 5.4 L/kg, a C max of 0.27 μM and a AUC of 1.1 μM•h for Sprague-Dawley (SD) rats[1].
Verubecestat (1 mg/kg; IV) has a T1/2 of 4.9 hours, a CL of 21 mL/min/kg, a Vss of 7.5 L/kg for cynomolgus monkeys[1].
Verubecestat (1 mg/kg; IV) has a T1/2 of 9.7 hours, a CL of 4.3 mL/min/kg, a Vss of 2.7 L/kg for beagle dogs[1].
Verubecestat (30 mg/kg; orally; BID for 5 days) causes a modest (1.4-fold) induction of CYP 3A1 activity but does not significantly alter the expression of CYPs 1A1, 1A2, 2B, 3A2, or 4A in rats[1].
Verubecestat dose-dependently reduces CSF and cortex Aβ40 with ED50 values of 5 and 8 mg/kg, respectively, corresponding to unbound plasma EC50 values of 48 and 81 nM, respectively[1].
Verubecestat (3 and 10 mg/kg; orally) reduces profound, sustained of CSF Aβ40 levels and has peak effects on CSF Aβ lowering (72 and 81% reduction at 3 and 10 mg/kg, respectively) 12 h after dosing[1].

Animal Model: Sprague-Dawley (SD) rats[1]
Dosage: 3 mg/kg (Pharmacokinetic Analysis)
Administration: IV or oral
Result: Had a T1/2 of 1.9 hours, a CL of 46 mL/min/kg, a Vss of 5.4 L/kg, a Cmax of 0.27 μM and a AUC of 1.1 μM•h.
Clinical Trial
Molecular Weight

409.41

Formula

C₁₇H₁₇F₂N₅O₃S

CAS No.

1286770-55-5

SMILES

O=C(C1=NC=C(F)C=C1)NC2=CC=C(F)C([[email protected]@](C3)(C)N=C(N)N(C)S3(=O)=O)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 35 mg/mL (85.49 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4425 mL 12.2127 mL 24.4254 mL
5 mM 0.4885 mL 2.4425 mL 4.8851 mL
10 mM 0.2443 mL 1.2213 mL 2.4425 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.69%

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Keywords:

VerubecestatMK-8931MK8931MK 8931Beta-secretaseBACEβ-SecretaseorallyBACE1BACE2Aβ40Alzheimer'sDiseaseInhibitorinhibitorinhibit

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