Begacestat - CAS 769169-27-9
Catalog number: 769169-27-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C9H8ClF6NO3S2
Molecular Weight:
391.74
COA:
Inquire
Targets:
γ-secretase
Description:
Begacestat is a selective thiophene sulfonamide inhibitor of amyloid precursor protein γ-secretase. Begacestat inhibits Abeta production with low nanomolar potency in cellular and cell-free assays of γ-secretase function. In Sep 2010, Phase-I for Alzheimer's disease in USA was discontinued.
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Purity:
98%
Appearance:
Off-White Solid
Synonyms:
5-Chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2-(trifluoromethyl)propyl]-2-thiophenesulfonamide; Begacestat; GSI 953;
Solubility:
DMSO, Methanol
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -21℃ for long term (months to years).
MSDS:
Inquire
Application:
Alzheimer's disease
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Boiling Point:
No Data Available
Melting Point:
153-155℃
InChIKey:
PSXOKXJMVRSARX-SCSAIBSYSA-N
InChI:
1S/C9H8ClF6NO3S2/c10-5-1-2-6(21-5)22(19,20)17-4(3-18)7(8(11,12)13)9(14,15)16/h1-2,4,7,17-18H,3H2/t4-/m1/s1
Canonical SMILES:
C1=C(SC(=C1)Cl)S(=O)(=O)NC(CO)C(C(F)(F)F)C(F)(F)F
Current Developer:
Pfizer
1.Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.
Martone RL1, Zhou H, Atchison K, Comery T, Xu JZ, Huang X, Gong X, Jin M, Kreft A, Harrison B, Mayer SC, Aschmies S, Gonzales C, Zaleska MM, Riddell DR, Wagner E, Lu P, Sun SC, Sonnenberg-Reines J, Oganesian A, Adkins K, Leach MW, Clarke DW, Huryn D, Abou-Gharbia M, Magolda R, Bard J, Frick G, Raje S, Forlow SB, Balliet C, Burczynski ME, Reinhart PH, Wan HI, Pangalos MN, Jacobsen JS. J Pharmacol Exp Ther. 2009 Nov;331(2):598-608. doi: 10.1124/jpet.109.152975. Epub 2009 Aug 11.
The presenilin containing gamma-secretase complex is responsible for the regulated intramembraneous proteolysis of the amyloid precursor protein (APP), the Notch receptor, and a multitude of other substrates. gamma-Secretase catalyzes the final step in the generation of Abeta(40) and Abeta(42) peptides from APP. Amyloid beta-peptides (Abeta peptides) aggregate to form neurotoxic oligomers, senile plaques, and congophilic angiopathy, some of the cardinal pathologies associated with Alzheimer's disease. Although inhibition of this protease acting on APP may result in potentially therapeutic reductions of neurotoxic Abeta peptides, nonselective inhibition of the enzyme may cause severe adverse events as a result of impaired Notch receptor processing. Here, we report the preclinical pharmacological profile of GSI-953 (begacestat), a novel thiophene sulfonamide gamma-secretase inhibitor (GSI) that selectively inhibits cleavage of APP over Notch.
2.ACS chemical neuroscience molecule spotlight on Begacestat (GSI-953).
Hopkins CR1. ACS Chem Neurosci. 2012 Jan 18;3(1):3-4. doi: 10.1021/cn200124u.
A "second generation" γ-secretase, Begacestat (GSI-953), which is more selective against Notch-signaling, has shown promise in recent Phase I clinical trials. Begacestat, a novel, 2,5-disubsitituted thiophene sulfonamide from Wyeth (now Pfizer) is under evaluation for the treatment of Alzheimer's disease.
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CAS 769169-27-9 Begacestat

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