Zetomipzomib maleate

Name: Zetomipzomib maleate
Brand: TargetMol
SKU: T39653
Rating: 4.5 (1 reviews)

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Catalog No. T39653Cas No. 2170983-62-5

Alias Zetomipzomib maleate, KZR-616 maleate

Zetomipzomib maleate (KZR-616), a novel immunoproteasome inhibitor, effectively and selectively inhibits the LMP7 subunit (hLMP7/mLMP7 IC50: 39/57 nM) and LMP2 subunit (hLMP7/mLMP7 IC50: 131/179 nM) of the immunoproteasome. This compound shows promising potential for research in various autoimmune diseases.

Zetomipzomib maleate

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Catalog No. T39653Alias Zetomipzomib maleate, KZR-616 maleateCas No. 2170983-62-5

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
5 mg	$1,490	Inquiry	Inquiry

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Product Introduction

Bioactivity

Description	Zetomipzomib maleate (KZR-616), a novel immunoproteasome inhibitor, effectively and selectively inhibits the LMP7 subunit (hLMP7/mLMP7 IC50: 39/57 nM) and LMP2 subunit (hLMP7/mLMP7 IC50: 131/179 nM) of the immunoproteasome. This compound shows promising potential for research in various autoimmune diseases.
In vitro	Zetomipzomib maleate also inhibits MECL-1 subunit (IC 50 =623 nM) and constitutive proteasome β5 subunit (IC 50 =688 nM). Zetomipzomib maleate maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. Zetomipzomib maleate (250 nM) shows a comparable cytokine inhibition profile peripheral blood mononuclear cells (PBMC)[1]. Zetomipzomib maleate is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 and PR-924[3].
In vivo	Zetomipzomib maleate, administered intravenously (i.v.) at a dosage of 5 mg/kg, demonstrated effectiveness in the anticollagen antibody induced arthritis (CAIA) model[1]. This study utilized 7-8 week old female BALB/c mice, with dosing repeated on days 6, 8, 11, and 13. The results highlighted zetomipzomib maleate's potential in mitigating CAIA, marking it as efficacious in this specific animal model.
Synonyms	Zetomipzomib maleate, KZR-616 maleate

Chemical Properties

Molecular Weight	702.758
Formula	C₃₄H₄₆N₄O₁₂
Cas No.	2170983-62-5
Smiles	OC(=O)\C=C/C(O)=O.COc1ccc(cc1)[C@@H](O)[C@H](NC(=O)[C@H](C)NC(=O)CN1CCOCC1)C(=O)N[C@@H](CC1=CCCC1)C(=O)[C@@]1(C)CO1

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc