| Identification | Back Directory | [Name]
D-erythro-3-Pentulose, 4,5-anhydro-1-(1-cyclopenten-1-yl)-1,2-dideoxy-4-C-methyl-2-[[N-[2-(4-morpholinyl)acetyl]-L-alanyl-(βR)-β-hydroxy-O-methyl-L-tyrosyl]amino]-, (2Z)-2-butenedioate (1:1) | [CAS]
2170983-62-5 | [Synonyms]
KZR-616 maleate
Zetomipzomib maleate | [Molecular Formula]
C30H42N4O8.C4H4O4 | [MOL File]
2170983-62-5.mol | [Molecular Weight]
702.76 |
| Hazard Information | Back Directory | [Uses]
Zetomipzomib (KZR-616) maleate, a first-in-class immunoproteasome inhibitor, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP2/mLMP2) subunits of the immunoproteasome. Zetomipzomib maleate has the potential for the research of multiple autoimmune diseases[1][2]. | [in vivo]
Zetomipzomib maleate (5 mg/kg; i.v.; dosing was repeated on days 6, 8, 11, and 13) shows efficacy in the anticollagen antibody induced arthritis (CAIA) model[1]. | Animal Model: | 7-8 week old female BALB/c mice (CAIA model)[1] | | Dosage: | I.v.; Dosing was repeated on days 6, 8, 11, and 13 until for 15 day | | Administration: | 5 mg/kg | | Result: | Showed efficacy in the anticollagen antibody induced arthritis (CAIA) model.
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| [References]
[1] Johnson HWB, et al. Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide). J Med Chem. 2018 Dec 27;61(24):11127-11143. DOI:10.1021/acs.jmedchem.8b01201
[2] Muchamuel T, et al. FRI0296 Kzr-616, a selective inhibitor of the immunoproteasome, blocks the disease progression in multiple models of systemic lupus erythematosus (SLE). Annals of the Rheumatic Diseases 2018;77:685.
[3] Xi J, et al. Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases. Eur J Med Chem. 2019;182:111646. DOI:10.1016/j.ejmech.2019.111646 |
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