Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C15H19N3O3 |
Molecular Weight | 289.3297 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(NC(=O)[C@H](N)CC1=CNC2=C1C=CC=C2)C(O)=O
InChI
InChIKey=SHAXSXUDZJSSCN-LLVKDONJSA-N
InChI=1S/C15H19N3O3/c1-15(2,14(20)21)18-13(19)11(16)7-9-8-17-12-6-4-3-5-10(9)12/h3-6,8,11,17H,7,16H2,1-2H3,(H,18,19)(H,20,21)/t11-/m1/s1
GAL 101 (formerly MRZ 99030 or EG-030) a small-molecule β-amyloid (Aβ) aggregation modulator with neuroprotective activity. It does not directly prevent early protein/protein interactions between monomeric Aβ, but rather promotes the formation of large, non-amyloidogenic, amorphous Aβ aggregates and thereby reduces the amount of intermediate toxic soluble oligomeric Aβ species. In vivo studies demonstrate the neuroprotective potential of MRZ-99030 after systemic and topical administration in animal models of Alzheimer's disease and glaucoma and age-related macular degeneration respectively. Currently, it is in Phase I trial for the treatment of glaucoma.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25637092
Curator's Comment: EG-030 is CNS active in animals. No human data available.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P05067|||Q13764|||Q8WZ99 Gene ID: 351.0 Gene Symbol: APP Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/25634238 |
28.4 nM [Kd] |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25106883
In anaesthetized rats, pre-administration of MRZ-99030 (50 mg/kg s.c.) protected against deficits in hippocampal LTP following i.c.v. injection of oligomeric Aβ1-42.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25637092
MRZ-99030 (100-500 nM) at a 10:1 stoichiometric excess to Aβ clearly reversed the synaptotoxic effects of Aβ1-42 oligomers on CA1-LTP in murine hippocampal slices.
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ACTIVE MOIETY