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BMS-708163 (Avagacestat), γ-Secretase Inhibitor

BMS-708163 (Avagacestat), γ-Secretase Inhibitor

$89.00
A potent γ-secretase Inhibitor, more selective for APP than Notch, in clinical trials for Alzheimer's disease.
Catalog No. Unit Price Qty
M60032-2s 2 mg solid $89.00
M60032-2 10 mM in DMSO (0.385 mL) $89.00

Details

Product Information
Chemical Name: (R)-2-(4-chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)phenylsulfonamido)-5,5,5-trifluoropentanamide
Molecular Weight: 520.88
Formula: C20H17ClF4N4O4S
Purity: ≥ 98%
CAS#: 1146699-66-2
Solubility: DMSO up to 100 mM
Storage: Powder: 4oC 1 year DMSO: 4oC 3 month -20oC 1 year

Biological Activity:

BMS-708163 (Avagacestat) is a potent, selective and orally bioavailable γ-secretase inhibitor with an IC50 of 0.3 nM for APP cleavage. It is 190-fold more selective for APP than Notch, having an IC50 of 58 nM for Notch. Phase I clinical trial studies showed that in humans, BMS-708163 decreased CSF Aβ40 and Aβ42 approximately 30% following daily dose of 100 mg after 28 days and by 60% at daily dose of 150 mg.


How to Use:

In vitro:  BMS-708163 was used at 1-10 µM in vitro.

In vivo: BMS-708163 was dosed orally in female rats at 10 and 100 mg/kg once per day, and could significantly reduced both plasma and brain Aβ40 levels relative to control for the entire dosing interval.


Reference:

  1. 1.  Gillman K, et al. Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor. (2010) ACS Med. Chem. Lett., 1 (3), pp 120–124
  2. 2.  Mitani Y, et al. Differential effects between γ-secretase inhibitors and modulators on cognitive function in amyloid precursor protein-transgenic and nontransgenic mice. (2012) J Neurosci. 32(6):2037-50.


BMS-708163_spec.pdf


Products are for research use only. Not for human use.

Description

Details

Product Information
Chemical Name: (R)-2-(4-chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)phenylsulfonamido)-5,5,5-trifluoropentanamide
Molecular Weight: 520.88
Formula: C20H17ClF4N4O4S
Purity: ≥ 98%
CAS#: 1146699-66-2
Solubility: DMSO up to 100 mM
Storage: Powder: 4oC 1 year DMSO: 4oC 3 month -20oC 1 year

Biological Activity:

BMS-708163 (Avagacestat) is a potent, selective and orally bioavailable γ-secretase inhibitor with an IC50 of 0.3 nM for APP cleavage. It is 190-fold more selective for APP than Notch, having an IC50 of 58 nM for Notch. Phase I clinical trial studies showed that in humans, BMS-708163 decreased CSF Aβ40 and Aβ42 approximately 30% following daily dose of 100 mg after 28 days and by 60% at daily dose of 150 mg.


How to Use:

In vitro:  BMS-708163 was used at 1-10 µM in vitro.

In vivo: BMS-708163 was dosed orally in female rats at 10 and 100 mg/kg once per day, and could significantly reduced both plasma and brain Aβ40 levels relative to control for the entire dosing interval.


Reference:

  1. 1.  Gillman K, et al. Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor. (2010) ACS Med. Chem. Lett., 1 (3), pp 120–124
  2. 2.  Mitani Y, et al. Differential effects between γ-secretase inhibitors and modulators on cognitive function in amyloid precursor protein-transgenic and nontransgenic mice. (2012) J Neurosci. 32(6):2037-50.


BMS-708163_spec.pdf


Products are for research use only. Not for human use.

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