Product Name :
KZR-616 maleate
Description:
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=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 maleate has the potential for the research of multiple autoimmune diseases.
CAS:
2170983-62-5
Molecular Weight:
702.75
Formula:
C34H46N4O12
Chemical Name:
(2S, 3R)-N-[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide; (2Z)-but-2-enedioic acid
Smiles :
C[C@H](NC(=O)CN1CCOCC1)C(=O)N[C@@H]([C@H](O)C1C=CC(=CC=1)OC)C(=O)N[C@@H](CC1CCCC=1)C(=O)[C@@]1(C)CO1.OC(=O)/C=C\C(O)=O
InChiKey:
HVKAUVYFVFFXLW-MTOCQVLVSA-N
InChi :
InChI=1S/C30H42N4O8.C4H4O4/c1-19(31-24(35)17-34-12-14-41-15-13-34)28(38)33-25(26(36)21-8-10-22(40-3)11-9-21)29(39)32-23(16-20-6-4-5-7-20)27(37)30(2)18-42-30;5-3(6)1-2-4(7)8/h6,8-11,19,23,25-26,36H,4-5,7,12-18H2,1-3H3,(H,31,35)(H,32,39)(H,33,38);1-2H,(H,5,6)(H,7,8)/b;2-1-/t19-,23-,25-,26+,30+;/m0./s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.Atorvastatin Purity
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 maleate has the potential for the research of multiple autoimmune diseases.|Product information|CAS Number: 2170983-62-5|Molecular Weight: 702.75|Formula: C34H46N4O12|Chemical Name: (2S, 3R)-N-[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide; (2Z)-but-2-enedioic acid|Smiles: C[C@H](NC(=O)CN1CCOCC1)C(=O)N[C@@H]([C@H](O)C1C=CC(=CC=1)OC)C(=O)N[C@@H](CC1CCCC=1)C(=O)[C@@]1(C)CO1.L-Asparaginase Apoptosis OC(=O)/C=C\C(O)=O|InChiKey: HVKAUVYFVFFXLW-MTOCQVLVSA-N|InChi: InChI=1S/C30H42N4O8.PMID:32901528 C4H4O4/c1-19(31-24(35)17-34-12-14-41-15-13-34)28(38)33-25(26(36)21-8-10-22(40-3)11-9-21)29(39)32-23(16-20-6-4-5-7-20)27(37)30(2)18-42-30;5-3(6)1-2-4(7)8/h6,8-11,19,23,25-26,36H,4-5,7,12-18H2,1-3H3,(H,31,35)(H,32,39)(H,33,38);1-2H,(H,5,6)(H,7,8)/b;2-1-/t19-,23-,25-,26+,30+;/m0./s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|KZR-616 maleate also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). KZR-616 maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. KZR-616 (250 nM) shows a comparable cytokine inhibition profile peripheral blood mononuclear cells (PBMC). KZR-616 maleate is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 (HY-13207) and PR-924 (HY-123587).|In Vivo:|KZR-616 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.|Products are for research use only. Not for human use.|
