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MCU-i4 is a negative modulator of of the MCU (mitochondrial calcium uniporter), acting by inhibiting IP3-dependent mitochondrial Ca2+-uptake and maintaining the gatekeeping role of their target. MCU-i4 and MCU-i11 represent leading molecules for the development of MICU1-targeting drugs.
| ln Vitro |
MCU-i4 regulates mitochondrial Ca2+ to the intestine for 1 minute, i.e. exerts negative regulation, indicating that the main effect of these compounds is to suddenly and directly regulate MCU complex activity [1]. MCU-i4 has a negative impact on Δψ. MCU-i4 Cellular Differentiation Assay [1]
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| Cell Assay |
Cell Differentiation Assay [1]
Cell Types: Growth medium of 90% confluent C2C12 myoblasts. Vitality has no effect [1]. Tested Concentrations: 10μM. Incubation Duration: 24 hrs (hours). Experimental Results: Myotube width decreases. |
| References |
[1]. Giulia Di Marco, et al. A High-Throughput Screening Identifies MICU1 Targeting Compounds. Cell Rep. 2020 Feb 18;30(7):2321-2331.e6.
[2]. Alessandro Rimessi, et al. Update on Calcium Signaling in Cystic Fibrosis Lung Disease. Front Pharmacol. 2021 Mar 11;12:581645. |
| Molecular Formula |
C23H27N3O2
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|---|---|
| Molecular Weight |
377.488
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| CAS # |
371924-24-2
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| SMILES |
O(C([H])([H])C([H])([H])[H])C(C1=C([H])N=C2C([H])=C([H])C(C([H])([H])[H])=C([H])C2=C1N([H])C1C([H])=C([H])C(=C([H])C=1[H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])=O
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| Chemical Name |
Ethyl 4-((4-(diethylamino)phenyl)amino)-6-methylquinoline-3-carboxylate
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| Synonyms |
MCUi4 MCU-i4 MCU i4
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~12.5 mg/mL (~33.11 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (3.31 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 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: ≥ 1.25 mg/mL (3.31 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 12.5 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6491 mL | 13.2454 mL | 26.4908 mL | |
| 5 mM | 0.5298 mL | 2.6491 mL | 5.2982 mL | |
| 10 mM | 0.2649 mL | 1.3245 mL | 2.6491 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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