Umibecestat free base

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 572152

CAS#: 1387560-01-1 (free base)

Description: Umibecestat, also known as CNP-520, is a beta-secretase inhibitor and is a drug candidate for prevention trials in Alzheimer's disease. CNP520 has a selectivity, pharmacodynamics, and distribution profile suitable for AD prevention studies. CNP520 reduced brain and cerebrospinal fluid (CSF) Aβ in rats and dogs, and Aβ plaque deposition in APP-transgenic mice. CNP520 reduces Aβ load and neuroinflammation in APP‐transgenic mice

Chemical Structure

Umibecestat free base
CAS# 1387560-01-1 (free base)

Theoretical Analysis

MedKoo Cat#: 572152
Name: Umibecestat free base
CAS#: 1387560-01-1 (free base)
Chemical Formula: C19H15ClF7N5O2
Exact Mass: 513.0802
Molecular Weight: 513.8
Elemental Analysis: C, 44.42; H, 2.94; Cl, 6.90; F, 25.88; N, 13.63; O, 6.23

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 1387560-01-1 (free base)   2365306-62-1 (HCl)   2365306-56-3 (fumarate)   2365306-58-5 (tatrate)   2365306-75-6 (citrate)    

Synonym: Umibecestat; CNP-520; CNP 520; CNP520;

IUPAC/Chemical 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)pyridine-2-carboxamide


InChi Code: 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

SMILES Code: O=C(C1=NC=C(C(F)(F)F)C=C1Cl)NC2=NC([C@]3(C)CO[C@](C(F)(F)F)(C)C(N)=N3)=C(F)C=C2

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 513.8 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Panza F, Lozupone M, Solfrizzi V, Sardone R, Piccininni C, Dibello V, Stallone R, Giannelli G, Bellomo A, Greco A, Daniele A, Seripa D, Logroscino G, Imbimbo BP. BACE inhibitors in clinical development for the treatment of Alzheimer's disease. Expert Rev Neurother. 2018 Nov;18(11):847-857. doi: 10.1080/14737175.2018.1531706. Epub 2018 Oct 24. PubMed PMID: 30277096.

2: Neumann U, Ufer M, Jacobson LH, Rouzade-Dominguez ML, Huledal G, Kolly C, Lüönd RM, Machauer R, Veenstra SJ, Hurth K, Rueeger H, Tintelnot-Blomley M, Staufenbiel M, Shimshek DR, Perrot L, Frieauff W, Dubost V, Schiller H, Vogg B, Beltz K, Avrameas A, Kretz S, Pezous N, Rondeau JM, Beckmann N, Hartmann A, Vormfelde S, David OJ, Galli B, Ramos R, Graf A, Lopez Lopez C. The BACE-1 inhibitor CNP520 for prevention trials in Alzheimer's disease. EMBO Mol Med. 2018 Nov;10(11). pii: e9316. doi: 10.15252/emmm.201809316. PubMed PMID: 30224383; PubMed Central PMCID: PMC6220303.

3: Lopez Lopez C, Caputo A, Liu F, Riviere ME, Rouzade-Dominguez ML, Thomas RG, Langbaum JB, Lenz R, Reiman EM, Graf A, Tariot PN. The Alzheimer's Prevention Initiative Generation Program: Evaluating CNP520 Efficacy in the Prevention of Alzheimer's Disease. J Prev Alzheimers Dis. 2017;4(4):242-246. doi: 10.14283/jpad.2017.37. PubMed PMID: 29181489.

4: Yan R. Stepping closer to treating Alzheimer's disease patients with BACE1 inhibitor drugs. Transl Neurodegener. 2016 Jul 14;5:13. doi: 10.1186/s40035-016-0061-5. eCollection 2016. Review. PubMed PMID: 27418961; PubMed Central PMCID: PMC4944430. @2018 .

Additional Information

The beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) initiates the generation of amyloid-β (Aβ), and the amyloid cascade leading to amyloid plaque deposition, neurodegeneration, and dementia in Alzheimer's disease (AD).