2365306-62-1
Chemical Structure
Umibecestat hydrochloride
Synonym(s): CNP520 hydrochloride
- CAS No.: 2365306-62-1
- Formula:C19H16Cl2F7N5O2
- Molecular Weight:550.26
IUPAC Name: N-(6-((3R,6R)-5-amino-3,6-dimethyl-6-(trifluoromethyl)-3,6-dihydro-2H-1,4-oxazin-3-yl)-5-fluoropyridin-2-yl)-3-chloro-5-(trifluoromethyl)picolinamide hydrochloride
InChIKey: ZCVGGIWXIQWEQB-MCJVGQIASA-N
SMILES: C[C@@]1(N=C([C@@](C)(OC1)C(F)(F)F)N)C2=C(F)C=CC(NC(C3=C(C=C(C=N3)C(F)(F)F)Cl)=O)=N2.Cl
Biological Activity: Umibecestat hydrochloride (CNP520 hydrochloride) is a selective, orally active BACE inhibitor, with an IC50 of 11 nM for hBACE-1, 10 nM for mouse BACE-1, and 30 nM for hBACE-2. Umibecestat hydrochloride reduces β-Amyloid levels in the brain and cerebrospinal fluid, decreases β-amyloid plaque deposition, and inhibits plaque-associated neuroinflammation. Umibecestat hydrochloride is used in research related to Alzheimer's disease[1][2][3][4].
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Umibecestat hydrochloride | Umibecestat hydrochloride (CNP520 hydrochloride) is a selective, orally active BACE inhibitor, with an IC50 of 11 nM for hBACE-1, 10 nM for mouse BACE-1, and 30 nM for hBACE-2. Umibecestat hydrochloride reduces β-Amyloid levels in the brain and cerebrospinal fluid, decreases β-amyloid plaque deposition, and inhibits plaque-associated neuroinflammation. Umibecestat hydrochloride is used in research related to Alzheimer's disease. | |||||||||||||||||||||
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References
- [1]. Neumann U, et al. The BACE-1 inhibitor CNP520 for prevention trials in Alzheimer's disease. EMBO molecular medicine. 2018 Nov;10(11):e9316. [Content Brief]
- [2]. Machauer R, et al. Discovery of Umibecestat (CNP520): A Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor for the Prevention of Alzheimer's Disease. Journal of medicinal chemistry. 2021 Oct 28;64(20):15262-15279.
- [3]. Imbimbo BP, et al. Investigational BACE inhibitors for the treatment of Alzheimer's disease. Expert opinion on investigational drugs. 2019 Nov;28(11):967-975.
- [4]. Tariot PN, et al. Reversibility of cognitive worsening observed with BACE inhibitor umibecestat in the Alzheimer's Prevention Initiative (API) Generation Studies. Alzheimer's & dementia : the journal of the Alzheimer's Association. 2024 Nov;20(11):7745-7761.
