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| Targets |
CMX-2043 targets cellular pathways involved in oxidative stress and ischemia-reperfusion injury. As an R-isomer analogue of α-lipoic acid, it exhibits enhanced antioxidant capacity and Akt kinase activation compared to R-α-lipoic acid. The compound's cytoprotective effects are mediated through its ability to reduce cellular injury and preserve tissue integrity during ischemic events. The R-stereoisomer is critical for its function.
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| 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]
In vitro, CMX-2043 outperforms R-α-lipoic acid in antioxidant capacity and Akt kinase activation. It has shown efficacy in reducing cellular injury in various cell-based models of oxidative stress and ischemia-reperfusion injury. The compound's cytoprotective effects are attributed to its ability to modulate redox signaling and activate survival pathways in stressed cells. |
| 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].
In vivo, CMX-2043 has demonstrated significant efficacy in preclinical models. It shows a 36% reduction in myocardial infarct size and preservation of white matter integrity in traumatic brain injury models. The compound has shown protective effects against ischemia-reperfusion injury in rat models and has advanced to Phase 2 clinical evaluation for cardioprotection and prevention of contrast-induced nephropathy. Clinical data from the SUPPORT-1 trial shows a significant 23% absolute reduction in troponin T elevation during PCI. |
| Enzyme Assay |
As a cytoprotective compound, CMX-2043 is not typically evaluated in cell-free receptor binding assays. Its activity is assessed by measuring its antioxidant capacity and its ability to activate survival kinases such as Akt in cell-free systems. The compound's redox-modulating properties can be measured using standard antioxidant assays such as DPPH or ABTS radical scavenging assays.
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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. In vitro cell-based experiments with CMX-2043 typically involve culturing cells under oxidative stress or hypoxia-reoxygenation conditions to model ischemia-reperfusion injury. Cells are treated with the compound, and cell viability is assessed using MTT or LDH release assays. The activation of survival pathways (e.g., Akt phosphorylation) and the reduction of oxidative stress markers (e.g., ROS levels) are measured to characterize the compound's cytoprotective mechanism. |
| 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. In vivo animal experiments with CMX-2043 have been conducted in rat models of myocardial ischemia-reperfusion injury and traumatic brain injury. In typical protocols, animals undergo surgical induction of ischemia (e.g., coronary artery ligation) followed by reperfusion. CMX-2043 is administered prior to or during reperfusion, and infarct size is measured by histochemical staining. Neurological outcomes are assessed in TBI models. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for CMX-2043. As a synthetic analogue of α-lipoic acid, it is expected to have favorable oral bioavailability and tissue distribution. The compound has a molecular weight of 406.5 g/mol. Its half-life and metabolic profile have not been extensively characterized in the available literature.
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| Toxicity/Toxicokinetics |
In preclinical toxicity studies, CMX-2043 has been well-tolerated at therapeutic doses. No significant toxicity has been reported in animal models. The compound has advanced to Phase 2 clinical evaluation, indicating an acceptable safety profile for further development. Common adverse effects are not well documented.
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| References | |
| Additional Infomation |
CMX-2043 has been used in trials to study the treatment and prevention of non-STEMI, unstable angina, stable coronary artery disease, and percutaneous coronary intervention.
CMX-2043 has a molecular formula of C16H26N2O6S2 and a molecular weight of 406.5 g/mol. It is also known as LIP-EA, R-LIP-EA-OH, and CMX2043. The compound is a next-generation, stereochemically-pure R-isomer analogue of α-lipoic acid. It has shown preclinical efficacy in cardiac IRI and TBI models and has advanced to Phase 2 clinical trials. It is available for research purposes only. |
| 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
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| 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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