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CMX-2043 (CMX2043) is an analogue of α-Lipoic Acid that can activate cell survival pathways and block oxidative damage. CMX-2043 can activate insulin receptor kinase, soluble tyrosine kinase, and Akt phosphorylation. CMX-2043 shows protection against ischemia-reperfusion injury (IRI) in rat model.
| ln Vitro |
CMX-2043 has a significant ability to absorb peroxyl radicals (15-250 mM; 10 minutes) [1]. Splen tyrosine kinase (Syk) and intimal endothelial cell kinase (Tie2) are both mildly inhibited by CMX-2043 (1.5 μM) [1]. In A549 cells, CMX-2043 (50 μM; 45 minutes) stimulates Akt phosphorylation via the PI3K pathway [1]. In CHO-M1-WT3 cells, CMX-2043 (2.5 mM; 30 minutes) decreases the rise in cytosolic calcium in a concentration-dependent manner [1]. fluorescent imaging [1]
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| ln Vivo |
Myocardial ischemia-reperfusion injury (IRI) as determined by the myocardial infarction to area at risk (MI-AR) ratio and the incidence of arrhythmias measure is decreased by CMX-2043 (50-200 mg/kg, 5 mL; oral; single dose)[2].
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| Cell Assay |
Immunofluorescence[1]
Cell Types: H9c2 (rat cardiomyocytes) Cell Tested Concentrations: 50 μM Incubation Duration: 3 hrs (hours) Experimental Results: Brighter fluorescence intensity in cells compared to control, indicating stronger Akt phosphorylation. |
| Animal Protocol |
Animal/Disease Models: Sprague Dawley rat ischemia-reperfusion injury (IRI) model [2]
Doses: 50, 100 and 200 mg/kg; 5 mL of normal saline solution flavored with 2% vanilla extract. Route of Administration: po (oral gavage); Single dose; Induces IRI 30-60 minutes after treatment Experimental Results: Induces arrhythmia and mortality in rats, reduces the ratio of myocardial infarction to risk area. |
| References | |
| Additional Infomation |
CMX-2043 has been used in trials studying the treatment and prevention of Non STEMI, Unstable Angina, Stable Coronary Artery Disease, and Percutaneous Coronary Intervention.
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| Molecular Formula |
C16H26N2O6S2
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|---|---|
| Molecular Weight |
406.52
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| Exact Mass |
406.123
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| CAS # |
910627-26-8
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| PubChem CID |
49802864
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| Appearance |
White to off-white solid powder
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| LogP |
0.7
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
26
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| Complexity |
517
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| Defined Atom Stereocenter Count |
3
|
| SMILES |
S1[C@@H](CCS1)CCCCC(N[C@H](C(N[C@H](C(=O)O)C)=O)CCC(=O)O)=O
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| InChi Key |
MQXRTCVZPIHBLD-TUAOUCFPSA-N
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| InChi Code |
InChI=1S/C16H26N2O6S2/c1-10(16(23)24)17-15(22)12(6-7-14(20)21)18-13(19)5-3-2-4-11-8-9-25-26-11/h10-12H,2-9H2,1H3,(H,17,22)(H,18,19)(H,20,21)(H,23,24)/t10-,11+,12-/m0/s1
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| Chemical Name |
(4S)-5-[[(1S)-1-carboxyethyl]amino]-4-[5-[(3R)-dithiolan-3-yl]pentanoylamino]-5-oxopentanoic acid
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| Synonyms |
CMX2043 CMX2043 CMX-2043
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| HS Tariff Code |
2934.99.9001
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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 : ~20.83 mg/mL (~51.24 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.12 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 (5.12 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. 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: ≥ 2.08 mg/mL (5.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4599 mL | 12.2995 mL | 24.5990 mL | |
| 5 mM | 0.4920 mL | 2.4599 mL | 4.9198 mL | |
| 10 mM | 0.2460 mL | 1.2300 mL | 2.4599 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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