Click Here for 5% Off Your First Aladdin Purchase!

Umibecestat - 99%, high purity , CAS No.1387560-01-1

  • ≥99%
Item Number
U646410
Grouped product items
SKUSizeAvailabilityPrice Qty
U646410-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$214.90
U646410-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$450.90
U646410-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$800.90
View related series
Beta-secretase Neuronal Signaling

Basic Description

SynonymsUmibecestat|1387560-01-1|Umibecestat [INN]|Umibecestat [USAN]|NVP-CNP520-NXA|CNP520-NXA|Umibecestat [USAN:INN]|CNP520|CNP-520|UNII-4612B80545|WHO 10872|4612B80545|2-Pyridinecarboxamide, N-(6-((3R,6R)-5-amino-3,6-dihydro-3,6-dimethyl-6-(trifluoromethyl)-2H
Specifications & Purity≥99%
Biochemical and Physiological MechanismsUmibecestat (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. Umibecestat can be used for the research of alzheimer's disease.
Storage TempProtected from light,Store at -80°C
Shipped InIce chest + Ice pads
Product Description

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 Umibecestat can be used for the research of alzheimer's disease.

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. 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 . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male rats (3-4 months old) 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 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.

Form:Solid

IC50& Target:IC50: 11 nM (human BACE-1), 10 nM (mouse BACE-1)

Associated Targets

CYP2D6 Tclin Cytochrome P450 2D6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CTSE Tchem Cathepsin E 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2C9 Tchem Cytochrome P450 2C9 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CTSD Tchem Cathepsin D 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BACE1 Tchem Beta-secretase 1 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BACE2 Tchem Beta-secretase 2 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

APP Tclin Amyloid-beta A4 protein 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name N-[6-[(3R,6R)-5-amino-3,6-dimethyl-6-(trifluoromethyl)-2H-1,4-oxazin-3-yl]-5-fluoropyridin-2-yl]-3-chloro-5-(trifluoromethyl)pyridine-2-carboxamide
INCHI InChI=1S/C19H15ClF7N5O2/c1-16(7-34-17(2,15(28)32-16)19(25,26)27)13-10(21)3-4-11(30-13)31-14(33)12-9(20)5-8(6-29-12)18(22,23)24/h3-6H,7H2,1-2H3,(H2,28,32)(H,30,31,33)/t16-,17+/m0/s1
InChi Key PSBBWFNMHDUTRH-DLBZAZTESA-N
Canonical SMILES CC1(COC(C(=N1)N)(C)C(F)(F)F)C2=C(C=CC(=N2)NC(=O)C3=C(C=C(C=N3)C(F)(F)F)Cl)F
Isomeric SMILES C[C@]1(CO[C@@](C(=N1)N)(C)C(F)(F)F)C2=C(C=CC(=N2)NC(=O)C3=C(C=C(C=N3)C(F)(F)F)Cl)F
Alternate CAS 1387560-01-1
PubChem CID 88602735
MeSH Entry Terms 2-Pyridinecarboxamide, N-(6-((3R,6R)-5-amino-3,6-dihydro-3,6-dimethyl-6-(trifluoromethyl)-2H-1,4-oxazin-3-yl)-5-fluoro-2-pyridinyl)-3-chloro-5-(trifluoromethyl)-;CNP520;N-(6-((3R,6R)-5-Amino-3,6-dimethyl-6-(trifluoromethyl)-3,6-dihydro-2H-1,4-oxazin-3-yl)
Molecular Weight 513.80

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Chemical and Physical Properties

SolubilityDMSO : 100 mg/mL (194.63 mM; Need ultrasonic)

Related Documents

Solution Calculators