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Cat. No. Name Size Price Add Cart
KI0279BMS-7081635 mg$299.2
BMS-70816310 mg$563.2
BMS-70816350 mg$1707.2
BMS-708163200 mg$4347.2

Chemical Characteristic

Product NameBMS-708163
SynonymsAvagacestat
CAS No.1146699-66-2
Molecular Weight 520.88
FormulaC20H17ClF4N4O4S
Chemical Name(2R)-2-[(4-chlorophenyl)sulfonyl-[[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide
SmilesC(=O)([C@@H](CCC(F)(F)F)N(Cc1c(cc(cc1)c1nocn1)F)S(=O)(=O)c1ccc(cc1)Cl)N
Chemical Structure

Biological activities

BMS-708163 is a potent and selective γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 and 0.27 nM, respectively. BMS-708163 is used for the treatment of Alzheimer's disease. BMS-708163 potently inhibits the formation of Aβ40 and Aβ42 in H4-8Sw cells. BMS-708163 exhibits potency for inhibition of Notch processing with IC50 values of 58 nM. BMS-708163 exhibits weak potency for inhibition of Cytochrome P-450 (CYP) isoform 2C19 with IC50 value of 20 µM.[1] BMS-708163 has an only 3-fold selectivity for cleavage of an amyloid precursor protein (APP) substrate compared with a Notch substrate. BMS-708163 has a 7-fold selective inhibition for Aβ40 compared with Notch intracellular domain (NICD). Furthermore, an excess of BMS-708163 (1 µM) completely blocks the 163-BPyne labeling of presenilin-1 (PS1) in HeLa cell membrane preparations.[2] In both rats and dogs following iv doses BMS-708163(1 and 10 mg/kg), plasma concentrations of BMS-708163 exhibits a multiexponential decline. The total body clearance of BMS-708163 is low in both species (rat =11.7 mL/min/kg; dog = 4.20 mL/min/kg). Oral bioavailability from solution formulations of BMS-708163 is 105 and 42% in rats and dogs, respectively. In addition, BMS-708163 demonstrats a high brain to plasma ratio (brainconcn/plasmaconcn = 2.4) in dogs. In female rats, BMS-708163 significantly reduces both plasma and brain Aβ40 levels relative to control at 10 and 100 mg/kg for the entire dosing interval. In brain, BMS-708163 demonstrates significant Aβ40 lowering for 8 hours after an oral dose of 1mg/kg. BMS-708163 (ranging from 3 to 100 mg/kg) also significantly lowers cerebrospinal fluid (CSF) Aβ40 levels in rats. In male beagle dogs administered a single oral dose of BMS-708163 (2 mg/kg), Aβ40 measurements from the frontal cortex and CSF shows a rapid and sustained reduction in brain and CSF Aβ40 levels.[1]

Protocols

BMS-708163 is diluted in DMSO. [1]

References

[1] Kevin W. Gillman, et al. Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor. Med Chem Lett. 2010, 1(3): 120-124.
[2] Crump CJ, et al. BMS-708,163 Targets Presenilin and Lacks Notch-Sparing Activity. Biochemistry. 2012, 51(37): 7209-7211.

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