Avagacestat
Tocris Bioscience, part of Bio-Techne | Catalog # 6363
Highly potent γ-secretase inhibitor; orally bioavailable
Key Product Details
Description
Highly potent γ-secretase inhibitor; orally bioavailable
Alternative Names
BMS-708163
Product Description
Avagacestat is a highly potent γ-secretase inhibitor (Aβ40 IC50 = 0.3 nM). Exhibits >137-fold selectivity for amyloid-β precursor protein (APP) processing over Notch. Reduces plasma and brain Aβ40 and Aβ42 levels in vivo. Orally bioavailable.Product Specifications
Molecular Weight
520.89
Formula
C20H17ClF4N4O4S
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
(2R)-2-[[(4-Chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide
CAS Number
1146699-66-2
PubChem ID
46883536
InChI Key
XEAOPVUAMONVLA-QGZVFWFLSA-N
SMILES
NC([C@H](N(S(=O)(C1=CC=C(C=C1)Cl)=O)CC2=C(C=C(C3=NOC=N3)C=C2)F)CCC(F)(F)F)=O
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 52.09 | 100 | |
| Ethanol | 10.42 | 20 |
Preparing Stock Solutions
for Avagacestat
The following data is based on the product molecular weight 520.89
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.92 mL | 9.60 mL | 19.20 mL |
| 5 mM | 0.38 mL | 1.92 mL | 3.84 mL |
| 10 mM | 0.19 mL | 0.96 mL | 1.92 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Albright Pharmacodynamics of selective inhibition of γ-secretase by avagacestat. J.Pharmacol.Exp.Ther. 2013 PMID: 23275065
- Gillman Discovery and evaluation of BMS-708163, a potent, selective and orally bioavailable γ-secretase inhibitor. ACS Med.Chem.Lett. 2010 PMID: 24900185
Product Specific Notices for Avagacestat
For research use only
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