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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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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 |
Synonyms | 1387560-01-1 | US8637508, 34 | SCHEMBL10382672 | Umibecestat | WHO 10872 | 6,7-Dihydro-1,2,3,10-tetramethoxy-7-(methylamino)-benzo(alpha)heptalen-9(5H)-one | 2-Pyridinecarboxamide, N-(6-((3R,6R)-5-amino-3,6-dihydro-3,6-dimethyl-6-(trifluoromethyl)-2H-1,4- |
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Specifications & Purity | ≥99% |
Biochemical and Physiological Mechanisms | 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. |
Storage Temp | Protected from light,Store at -80°C |
Shipped In | Ice 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) |
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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 |
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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 |
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Solubility | DMSO : 100 mg/mL (194.63 mM; Need ultrasonic) |
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