| Identification | Back Directory | [Name]
KZR-616 | [CAS]
1629677-75-3 | [Synonyms]
KZR-616
Zetomipzomib
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]- | [Molecular Formula]
C30H42N4O8 | [MDL Number]
MFCD34469327 | [MOL File]
1629677-75-3.mol | [Molecular Weight]
586.69 |
| Chemical Properties | Back Directory | [Boiling point ]
908.5±65.0 °C(Predicted) | [density ]
1.261±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [pka]
12.70±0.46(Predicted) |
| Hazard Information | Back Directory | [Uses]
Zetomipzomib (KZR-616), a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. Zetomipzomib has the potential for the research of multiple autoimmune diseases[1][2]. | [in vivo]
Zetomipzomib (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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| [storage]
Store at -20°C | [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) 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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