[CAS NO. 1387560-01-1] Umibecestat
PRODUCTS SPECIFICATIONS [1387560-01-1]
DESCRIPTION [1387560-01-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 513.80 |
| Molecular Formula | C19H15ClF7N5O2 |
| SMILES | O=C(NC1=NC([C@@]2(CO[C@](C)(C(N)=N2)C(F)(F)F)C)=C(C=C1)F)C3=NC=C(C=C3Cl)C(F)(F)F |
Summary
Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC 50 s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively [1] . Umibecestat can be used for the research of alzheimer's disease.
IC50 & Target
IC50: 11 nM (human BACE-1), 10 nM (mouse BACE-1) [1]
In Vitro
Umibecestat (CNP520) is a potent BACE-1 inhibitor that is selective for BACE-1 over other human pepsin-like aspartic proteases, including BACE-2 and cathepsin D [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Umibecestat (CNP520) (1.5-51.3 mg/kg; given by oral gavage; 72 hours) shows a dose-dependent effects on Aβ40 and a long duration of action in both rat brain and CSF
[1]
.
Umibecestat (CNP520) (3.1 mg/kg; oral administration; 7 days) shows a > 75% reduction on Aβ40 and Aβ42 in CSF after dosing and returns slowly to baseline over the next 7 days
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male rats (3-4 months old) [1] |
| Dosage: | 1.5 mg/kg (3 μM/kg)-51.3 mg/kg (100 μM/kg) |
| Administration: | Given by oral gavage; 72 hours |
| Result: | Reduced 89.3±4.5% Aβ40 at the highest dose in brain tissue, and 50% lowering of rat brain Aβ40 (ED50) was 2.4±0.31 mg/kg. Reduced ~50% Aβ40 at a single oral 30 μM/kg (15.4 mg/kg) dose after 24 hours in both rat brain and CSF。 |
| Animal Model: | 3-month-old beagle dogs [1] |
| Dosage: | 3.1 mg/kg (6 μM/kg) |
| Administration: | Oral administration; 7 days |
| Result: | Both Aβ40 and Aβ42 concentrations in CSF showed a > 75% reduction at 12-48 h after dosing and returned slowly to baseline over the next 7 days. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02576639 | Novartis Pharmaceuticals|Novartis |
Alzheimer´s Disease
|
August 10, 2015 | Phase 2 |
| NCT02565511 | Novartis Pharmaceuticals|Banner Alzheimer´s Institute|National Institute on Aging (NIA)|Amgen|Novartis |
Alzheimers Disease
|
November 30, 2015 | Phase 2|Phase 3 |
| NCT03131453 | Novartis Pharmaceuticals|Amgen|Banner Alzheimer´s Institute|Novartis |
Alzheimers Disease
|
August 3, 2017 | Phase 2|Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL ( 194.63 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9463 mL | 9.7314 mL | 19.4628 mL |
| 5 mM | 0.3893 mL | 1.9463 mL | 3.8926 mL |
| 10 mM | 0.1946 mL | 0.9731 mL | 1.9463 mL |