Free shipping on all orders over $ 500

Begacestat

Cat. No. M3619
Begacestat Structure
Synonym:

GSI-953

Size Price Availability
10mg USD 200  USD200 Out of stock
50mg USD 800  USD800 Out of stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Begacestat selectively inhibits cleavage of amyloid precursor protein (APP) over Notch. Lowers levels of Aβ42 and Aβ40 (EC50 values are 12.4 and 14.8 nM respectively in cells expressing human recombinant APP). In healthy human volunteers, oral administration of a single dose of GSI-953 produces dose-dependent changes in plasma Abeta levels, which confirms pharmacodynamic activity of GSI-953 in humans.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 391.74
Formula C9H8ClF6NO3S2
CAS Number 769169-27-9
Purity >99%
Solubility DMSO 40 mg/mL
Storage at -20°C
References

[1] Martone RL, et al. J Pharmacol Exp Ther. Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.

Related Gamma-secretase Products
Compound E

Compound E is a cell-permeable, potent, selective inhibitor of γ-secretase and Notch processing.

PF-03084014

PF-03084014 (Nirogacestat) is a potent and selective γ-secretase inhibitor with IC50 of 6.2 nM.

L-685,458

L-685,458 is a potent, selective, structurally novel γ-secretase inhibitor; equipotent inhibitor of both Aβ1-42 and Aβ1-40 production.

YO-01027

YO-01027 (Dibenzazepine, DBZ) is a dipeptidic γ-secretase inhibitor with IC50 of 2.6 nM and 2.9 nM for APPL and Notch cleavage, respectively.

LY900009

LY900009 is a potent Notch inhibitor with IC50 of 0.27 nM.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Begacestat, GSI-953 supplier, Gamma-secretase, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.