beta-Secretase Inhibitor IVA compound that binds to the active site of BACE-1 and potently blocks its proteolytic activity

β-Secretase Inhibitor IV (CAS 797035-11-1)

β-Secretase Inhibitor IV, CAS 797035-11-1 is rated 5.0 out of 5 by 1.
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Synonym: 5HA; 3-N-[(2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-yl]-5-[methyl(methylsulfonyl)amino]-1-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
Application: A compound that binds to the active site of BACE-1 and potently blocks its proteolytic activity
CAS Number: 797035-11-1
Purity: ≥95%
Molecular Weight: 578.72
Molecular Formula: C31H38N4O5S
* Refer to Certificate of Analysis for lot specific data (including water content).
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β-Secretase Inhibitor IV, a cell-permeable isophthalamide compound containing a hydroxyethylamine motif which binds to BACE-1 active site and potently blocks its proteolytic activity. The compound displays greater selectivity over other aspartyl proteases. β-Secretase Inhibitor IV is an inhibitor of BACE and BACE2.


References

Stachel, S.J., et al. 2004. J. Med. Chem. 47, 6447.

Usage :
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Physical State :
Solid
Solubility :
Soluble in DMSO, and methanol.
Storage :
Store at 4° C
Melting Point :
103-105° C
Density :
1.31 g/cm3
Refractive Index :
n20D 1.64 (Predicted)
IC50 :
BACE-1: IC50 = 15 nM (human); sAPP_NF: IC50 = 29 nM (HEK293-APPNFEV cells); BACE-2: IC50 = 0.23 µM ; cathepsin D: IC50 = 7.6 µM ; renin: IC50 = >50 µM
Ki Data :
Beta-secretase 1: Ki= 233 nM (human); Beta secretase 2: Ki= 240 nM (human); Cathepsin D: Ki= 448 nM (human)
pK Values :
pKa: 13.72 (Predicted), pKb: 8.35 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
5287532
SMILES :
C[C@H](C1=CC=CC=C1)NC(=O)C2=CC(=CC(=C2)N(C)S(=O)(=O)C)C(=O)N[C@@H](CC3=CC=CC=C3)[C@@H](CNC4CC4)O

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Jiaranaikulwanitch Jiaranaikulwanitch, J. et al. (PubMed 22781443) modified the tryptoline and tryptamine cores of BACE1 inhibitors previously identified by virtual screening in silico for additional modes of action. These core structures were readily linked to different side chains using 1,2,3-triazole rings as bridges by copper catalyzed azide-alkyne cycloaddition reactions. The neuroprotective effects of the multifunctional compounds 6h, 12c and 12h on A induced neuronal cell death at 1 M were significantly greater than those of the potent single target compound, BACE1 inhibitor IV and were comparable to curcumin. -SCBT Publication Review
Date published: 2015-07-07
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