U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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
Structure of MRZ-99030

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

HIDE SMILES / InChI
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

Curator's Comment: EG-030 is CNS active in animals. No human data available.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P05067|||Q13764|||Q8WZ99
Gene ID: 351.0
Gene Symbol: APP
Target Organism: Homo sapiens (Human)
28.4 nM [Kd]
PubMed

PubMed

TitleDatePubMed
Effect of the Aβ aggregation modulator MRZ-99030 on retinal damage in an animal model of glaucoma.
2014 Nov

Sample Use Guides

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
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.
Name Type Language
MRZ-99030
Common Name English
D-TRYPTOPHYL-2-METHYLALANINE
Systematic Name English
ALANINE, D-TRYPTOPHYL-2-METHYL-
Systematic Name English
2-(((2R)-2-AMINO-3-(1H-INDOL-3-YL)PROPANOYL)AMINO)-2-METHYL-PROPANOIC ACID
Systematic Name English
EG-030
Code English
Code System Code Type Description
FDA UNII
2OZL368FU0
Created by admin on Sat Dec 16 12:07:05 GMT 2023 , Edited by admin on Sat Dec 16 12:07:05 GMT 2023
PRIMARY
PUBCHEM
56649444
Created by admin on Sat Dec 16 12:07:05 GMT 2023 , Edited by admin on Sat Dec 16 12:07:05 GMT 2023
PRIMARY
CAS
1123071-24-8
Created by admin on Sat Dec 16 12:07:05 GMT 2023 , Edited by admin on Sat Dec 16 12:07:05 GMT 2023
PRIMARY