| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| ln Vitro |
In fibroblasts with knockouts for Mitofusin-1 and Mitofusin-2, mitochondrial elongation is promoted by mitochondrial fusion promoter M1 (5-25 μM; 24 h) [2]. In BRIN-BD11 pancreatic β-cells, mitochondrial fusion promoter M1 (20 μM; 12 h) increases mitochondrial membrane potential from 0.29±0.05-fold to 0.5±0.07-fold, decreases mitochondrial ROS to 1.0±0.44-fold, and restores mitochondrial structure [3]. The impairment of pancreatic beta cell oxygen consumption rate caused by cholesterol exposure is prevented by the mitochondrial fusion promoter M1 (20 μM; 12 h) [3]. In cholesterol-rich pancreatic beta cells, extracellular acidification rate (ECAR) and non-mitochondrial respiration are not impaired by mitochondrial fusion promoter M1 (20 μM; 12 h) [3]. In pancreatic beta cells treated with cholesterol, the mitochondrial fusion promoter M1 (20 μM; 12 hours) reinstates glucose-stimulated insulin secretion (GSIS) [3].
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| ln Vivo |
Rats with myocardial I/R injury are considerably protected from brain damage by the mitochondrial fusion promoter M1 (2 mg/kg; iv)[1].
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| Animal Protocol |
Animal/Disease Models: Male Wistar rats (250-300g) receiving cardiac ischemia/reperfusion (I/R)[1]
Doses: 2 mg/kg Route of Administration: Iv 15 minutes before cardiac I/R injury Experimental Results: Increased brain mitochondrial fusion. Increased blood -brain barrier (BBB) tight junction protein, and decreased macrophage infiltration in the brain. decreased brain mitochondrial dysfunction and apoptosis, but it did not reduce mitochondrial oxidative stress. decreased the expression of Alzheimer's disease (AD)-related proteins. |
| References |
[1]. Surinkaew P, et, al. Mitochondrial Fusion Promoter Alleviates Brain Damage in Rats with Cardiac Ischemia/Reperfusion Injury. J Alzheimers Dis. 2020;77(3):993-1003.
[2]. Wang D, et, al. A small molecule promotes mitochondrial fusion in mammalian cells. Angew Chem Int Ed Engl. 2012 Sep 10;51(37):9302-5. [3]. Asalla S, et, al. Restoring Mitochondrial Function: A Small Molecule-mediated Approach to Enhance Glucose Stimulated Insulin Secretion in Cholesterol Accumulated Pancreatic beta cells. Sci Rep. 2016 Jun 10;6:27513. |
| Molecular Formula |
C14H10CL4N2O
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|---|---|
| Molecular Weight |
364.05
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| CAS # |
219315-22-7
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| SMILES |
ClC1C=C(C=C(C=1NN=C(C)C1C=C(C=CC=1O)Cl)Cl)Cl
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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: 50 mg/mL (137.34 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. Solubility in Formulation 2: 0.5 mg/mL (1.37 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 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. View More
Solubility in Formulation 3: 0.5 mg/mL (1.37 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7469 mL | 13.7344 mL | 27.4688 mL | |
| 5 mM | 0.5494 mL | 2.7469 mL | 5.4938 mL | |
| 10 mM | 0.2747 mL | 1.3734 mL | 2.7469 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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