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| Targets |
Cardiogenol C primarily targets the Wnt/β-catenin signaling pathway. Wnt signaling plays a critical role in cardiac development and differentiation. The compound acts as a potent inducer of cardiomyogenesis by modulating this pathway. While the exact molecular mechanism of Cardiogenol C is not fully elucidated, it is known to promote the differentiation of embryonic stem cells into cardiomyocytes. The compound's effect is thought to be mediated through the activation of cardiac-specific transcription factors and the upregulation of cardiac marker genes. Cardiogenol C has been shown to significantly increase the expression of atrial natriuretic factor (ANF, Nppa) and NKX2-5, a key cardiac transcription factor, in P19 and C2C12 cells. It also enhances the expression of the cardiac Nav1.5 sodium channel protein in C2C12 cells. These effects are consistent with the induction of a cardiac gene expression program. The compound's cell permeability allows it to easily enter cells and exert its effects. Its activity is dependent on the activation of the Wnt/β-catenin pathway, which is a key regulator of cardiomyocyte differentiation.
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| ln Vitro |
In P19 cells, Cardiogenol C (1 μM; 7 days) has cardiogenic effects and raises atrial natriuretic factor (ANF, nppa) considerably in P19 cells when compared to untreated control cells [1]. ANF expression was considerably boosted by cardiogenol C (0.01-100 μM; 7 days). Furthermore, this tiny drug greatly boosted the expression of another widely used cardiac marker gene (NKX2-5) in C2C12 cells [2]. In C2C12 cells, cardiogenol C (0.001–100 μM; 7 days) dose-dependently enhances the expression of cardiac Nav1.5 sodium channel protein [2]. Even at a dose of 10 μM, cardiogenol C (0.01-100 μM; 7 days) had no effect on cell proliferation. Moreover, the effects of Cardiogenol C dissolved in DMSO or water can be comparable. On C2C12 cells, the greatest dosage of 100 μM exhibits substantial cytotoxicity [2].
In vitro, Cardiogenol C exhibits potent cardiomyogenic activity. In P19 cells, a mouse embryonal carcinoma cell line that can differentiate into cardiomyocytes, treatment with Cardiogenol C (1 μM; 7 days) significantly increases the expression of atrial natriuretic factor (ANF, Nppa) compared to untreated control cells. The effect is dose-dependent, with ANF expression being considerably boosted by Cardiogenol C at concentrations ranging from 0.01 to 100 μM over a 7-day period. In C2C12 cells, a mouse myoblast cell line, Cardiogenol C also significantly boosts the expression of another widely used cardiac marker gene, NKX2-5. Furthermore, in C2C12 cells, Cardiogenol C (0.001–100 μM; 7 days) dose-dependently enhances the expression of the cardiac Nav1.5 sodium channel protein. Importantly, Cardiogenol C at concentrations up to 10 μM has no effect on cell proliferation in C2C12 cells, indicating that its effects are specific to differentiation rather than general cell growth. However, the highest dose of 100 μM exhibits substantial cytotoxicity. The effects of Cardiogenol C are comparable whether dissolved in DMSO or water, indicating that the solvent does not interfere with its activity. |
| ln Vivo |
Detailed in vivo activity data for Cardiogenol C is limited in the available literature. However, the compound's potent in vitro cardiomyogenic activity suggests that it may have therapeutic potential for cardiac regeneration in vivo. The compound's ability to induce cardiomyogenesis in lineage-committed progenitor cells raises the possibility that it could be used to promote cardiac repair in vivo by stimulating endogenous progenitor cells. However, no specific in vivo studies have been detailed in the public domain. The compound's cell permeability and small molecular size suggest that it could be administered systemically, but its pharmacokinetic properties and tissue distribution have not been reported. The compound's lack of effect on cell proliferation at concentrations up to 10 μM suggests that it may not cause unwanted hyperplasia in vivo. The compound's in vivo efficacy and safety would need to be evaluated in animal models of cardiac injury or disease before it could be considered for therapeutic applications. Currently, Cardiogenol C is primarily a research tool for in vitro studies.
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| Enzyme Assay |
Cell-free receptor binding or enzyme assays are not typically the primary focus for studying Cardiogenol C, as its activity is assessed by monitoring the differentiation of stem cells into cardiomyocytes, which involves complex signaling pathways rather than a single enzyme target. However, the compound's interaction with the Wnt/β-catenin pathway could potentially be studied using cell-free assays that measure the activity of components of this pathway, such as β-catenin stabilization or TCF/LEF transcriptional activity. For example, a cell-free assay could involve incubating cell lysates with the compound and measuring β-catenin levels by Western blot. Alternatively, a reporter gene assay could be used to measure TCF/LEF-dependent transcription in cell lysates. However, these are not standard assays for this compound. The compound's activity is typically evaluated by measuring the expression of cardiac marker genes and proteins in cell culture.
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| Cell Assay |
RT-PCR[2]
Cell Types: C2C12 Cell Tested Concentrations: 0.01 μM; 0.1 μM; 1 μM; 3 μM; 10 μM; 30 μM; 100 μM Incubation Duration: 7 days Experimental Results: Increased ANF and NKX2.5 mRNA levels in a dose-dependent manner. Western Blot Analysis[2] Cell Types: C2C12 Cell Tested Concentrations: 0.001 μM; 0.01μM; 0.1μM; 1μM; 10 μM Incubation Duration: 7 days Experimental Results: Increased cardiac Nav1.5 sodium channel protein levels. Cell proliferation experiment [2] Cell Types: C2C12 cell Tested Concentrations: 0.01 μM; 0.1 μM; 1 μM Incubation Duration: 7 days Experimental Results: 0.01-10 μM treatment had no toxic effect on C2C12 cells. For in vitro cellular assays, the cardiomyogenic activity of Cardiogenol C is typically assessed using mouse embryonic stem cells (ESCs) or lineage-committed progenitor cells such as P19 or C2C12 cells. The cells are seeded in multi-well plates and cultured in differentiation medium. Cardiogenol C is added at various concentrations (e.g., 0.001–100 μM), and the cells are incubated for a period of 7 days. The medium is replaced every 2-3 days with fresh medium containing the compound. After the incubation period, the cells are harvested, and the expression of cardiac marker genes, such as atrial natriuretic factor (ANF, Nppa) and NKX2-5, is analyzed by quantitative real-time PCR (qRT-PCR). The expression of cardiac proteins, such as the cardiac Nav1.5 sodium channel, is analyzed by Western blot. Cell proliferation is assessed using an MTT or resazurin assay. The EC₅₀ for cardiomyocyte induction is determined by plotting the percentage of MHC-positive cells or the level of marker gene expression against the log of compound concentration. These assays provide a measure of the compound's cardiomyogenic potency and its effects on cardiac differentiation. |
| Animal Protocol |
Standardized in vivo animal experiment protocols for Cardiogenol C have not been widely reported in the available literature. Typically, to assess the in vivo efficacy of a cardiomyogenic compound, a murine model of myocardial infarction (MI) or other cardiac injury would be employed. In such a study, immunodeficient or wild-type mice would undergo ligation of the left anterior descending (LAD) coronary artery to induce an MI. After a recovery period, Cardiogenol C would be administered to the mice via various routes, such as intraperitoneal injection, oral gavage, or direct injection into the myocardium. The compound would be given at various doses (e.g., 1-10 mg/kg) on a daily or every-other-day schedule for a period of several weeks. A control group would receive the vehicle alone. Cardiac function would be assessed by echocardiography to measure parameters such as ejection fraction and fractional shortening. At the end of the study, the hearts would be harvested for histological analysis to evaluate infarct size, fibrosis, and the extent of new cardiomyocyte formation. The expression of cardiac markers would be analyzed by immunohistochemistry and qRT-PCR. These studies would provide critical data on the compound's ability to promote cardiac repair and regeneration in vivo. Currently, no such detailed in vivo protocols for Cardiogenol C have been published.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties for Cardiogenol C are not extensively reported in the available literature. As a small molecule with a molecular weight of 296.75 and a logP of 1.667, it is expected to have reasonable cell permeability and oral bioavailability. The compound's moderate lipophilicity (logP 1.667) suggests that it may be well absorbed after oral administration. The compound is soluble in DMSO and water, which is favorable for formulation. However, specific pharmacokinetic parameters such as half-life (t₁/₂), volume of distribution (Vd), clearance (CL), and oral bioavailability (%F) have not been determined experimentally. The compound's metabolism is likely to involve hepatic cytochrome P450 enzymes. The compound's elimination route is unknown. Further studies, including plasma protein binding and metabolic stability assays, are needed to fully characterize the pharmacokinetic profile of this compound. The compound's in vivo activity, if any, would depend on its ability to reach target tissues in sufficient concentrations.
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| Toxicity/Toxicokinetics |
Toxicological data for Cardiogenol C indicates that it is well-tolerated in vitro at concentrations up to 10 μM, with no significant cytotoxic effects observed in C2C12 cells. However, the highest concentration tested (100 μM) exhibited substantial cytotoxicity. No specific acute or chronic toxicity studies in animals have been detailed in the public domain. As a research chemical, standard safety precautions should be observed when handling this compound. The compound's lack of effect on cell proliferation at concentrations up to 10 μM suggests that it may not cause unwanted hyperplasia. However, the potential for off-target effects and long-term toxicity has not been assessed. The compound is not approved for clinical use and should only be used in preclinical research settings.
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| References | |
| Additional Infomation |
2-[[2-(4-methoxyaniline)-4-pyrimidinyl]amino]ethanol is a substituted aniline, belonging to the methoxybenzene class of compounds.
Cardiogenol C is a research tool for studying cardiomyocyte differentiation and cardiac development. Its mechanism of action involves modulation of the Wnt/β-catenin signaling pathway. It is a potent inducer of cardiomyogenesis with an EC₅₀ of 100 nM. It is not approved for clinical use. |
| Molecular Formula |
C13H17CLN4O2
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|---|---|
| Molecular Weight |
296.75300
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| Exact Mass |
296.104
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| CAS # |
671225-39-1
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| Related CAS # |
Cardiogenol C hydrochloride;1049741-55-0
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| PubChem CID |
11345983
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.305g/cm3
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| Boiling Point |
520.3ºC at 760 mmHg
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| Flash Point |
268.5ºC
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| Index of Refraction |
1.667
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| LogP |
2.581
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
19
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| Complexity |
247
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=C(C=C1)NC2=NC=CC(=NCCO)N2
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| InChi Key |
LKBSMPFEKIBRGC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H16N4O2/c1-19-11-4-2-10(3-5-11)16-13-15-7-6-12(17-13)14-8-9-18/h2-7,18H,8-9H2,1H3,(H2,14,15,16,17)
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| Chemical Name |
2-[[2-(4-methoxyanilino)pyrimidin-4-yl]amino]ethanol
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3698 mL | 16.8492 mL | 33.6984 mL | |
| 5 mM | 0.6740 mL | 3.3698 mL | 6.7397 mL | |
| 10 mM | 0.3370 mL | 1.6849 mL | 3.3698 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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