| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
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| ln Vitro |
Zetomipzomib maleate is an immunoproteasome selective inhibitor [3]. Additionally, constitutive proteasome β5 subunit (IC50=688 nM) and MECL-1 subunit (IC50=623 nM) are inhibited by methotrimib maleate. LMP7 and LMP2 in MOLT-4 cells are selectively inhibited by methotrimib maleate. Peripheral blood mononuclear cells (PBMCs) and methotrimib maleate (250 nM) exhibit a similar cytokine inhibitory profile [1].
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| ln Vivo |
In an anti-collagen antibody-induced arthritis (CAIA) animal, methotrimib maleate (5 mg/kg; intravenously; repeated doses on days 6, 8, 11, and 13) has demonstrated effectiveness[1].
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| Animal Protocol |
Animal/Disease Models: 7-8 week old female balb/c (Bagg ALBino) mouse (CAIA model)[1]
Doses: Iv; Dosing was repeated on days 6, 8, 11, and 13 until for 15 day Route of Administration: 5 mg/kg Experimental Results: demonstrated efficacy in the anticollagen antibody induced arthritis (CAIA) model. |
| 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.
[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. |
| Molecular Formula |
C34H46N4O12
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|---|---|
| Molecular Weight |
702.75
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| CAS # |
2170983-62-5
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| Related CAS # |
Zetomipzomib;1629677-75-3
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| SMILES |
C(/C(=O)O)=C/C(=O)O.C([C@@]1(OC1)C)(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)CN1CCOCC1)[C@@H](C1C=CC(OC)=CC=1)O)CC1=CCCC1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 250 mg/mL (355.75 mM)
H2O: 50 mg/mL (71.15 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.96 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 100 mg/mL (142.30 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4230 mL | 7.1149 mL | 14.2298 mL | |
| 5 mM | 0.2846 mL | 1.4230 mL | 2.8460 mL | |
| 10 mM | 0.1423 mL | 0.7115 mL | 1.4230 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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