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
| Molecular Formula | C15H19N3O3 |
| Molecular Weight | 289.3297 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
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.
Originator
Approval Year
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
| Substance Class |
Chemical
Created
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admin
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Edited
Sat Dec 16 12:07:05 GMT 2023
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| Record UNII |
2OZL368FU0
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| Record Status |
Validated (UNII)
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ACTIVE MOIETY |
MRZ-99030 is a modulator of A.BETA. aggregation which prevents the formation of soluble toxic oligomeric A.BETA. species. The affinity of MRZ-99030 binding to A.BETA.1-42 was determined to be 28.4 +/- 2.9 nM as revealed by surface plasmon resonance measurements. The combined interpretation of extensive results from experiments using dynamic light scattering, atomic force microscopy, CD-spectroscopy, SDS PAGE, Western blots/silver stains and TR-FRET revealed that MRZ-99030 does not prevent direct protein/protein interactions between monomeric A.BETA. species, but rather promotes the formation of large, amorphous/globular A.BETA. species when present at a 10:1 stoichiometric excess to A.BETA.. Since amyloidogenic fibrillar structures are ultimately also not formed MRZ-99030 is believed to trigger a non-amyloidogenic self-propagating/detoxifying pathway and thereby reduces the amount of intermediate toxic soluble oligomeric A.BETA. species.
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ACTIVE MOIETY |
Official Title: Safety and Tolerability of MRZ-99030 Eye Drops in Healthy Volunteers and Glaucoma Patients
Purpose: (1)To assess the safety and tolerability of repeat dose topical administration of MRZ-99030 Ophthalmic Solution with ascending doses in healthy subjects (stage 1) and glaucoma subjects (stage 2). (2)To assess plasma pharmacokinetics and urine concentration of MRZ- 99030 and its metabolite MRZ-9499 after single and repeat dose topical administration of MRZ-99030 Ophthalmic Solution.
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ACTIVE MOIETY |
Originator: Merz Pharmaceuticals GmbH; Class: Antiglaucoma, Neuroprotectant, Small molecule; Mechanism of Action: Protein aggregation modulator; Orphan Drug Status: No; On Fast track: No; New Molecular Entity: Yes; Highest Development Phases: Discontinued for Alzheimer's disease, Glaucoma; Most Recent Events: 01 Dec 2013 Merz Pharmaceuticals completes a phase I trial for Glaucoma in Germany (NCT01714960), 29 Nov 2013 Merz Pharmaceuticals completes enrolment in its phase I trial for Glaucoma in Germany (NCT01714960), 26 Jul 2013 Phase-I development is ongoing in Germany
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