| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary molecular target is the sodium-hydrogen exchanger isoform 1 (NHE-1). Cariporide Mesylate selectively inhibits NHE-1, a membrane transporter that exchanges intracellular protons for extracellular sodium ions. During ischemia, NHE-1 activation leads to intracellular sodium accumulation, which in turn causes calcium overload via the sodium-calcium exchanger, contributing to myocardial injury. NHE-1 inhibition protects the myocardium from ischemia-reperfusion injury.
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|---|---|
| ln Vitro |
In vitro, Cariporide Mesylate inhibits NHE-1 activity in cardiac cells and other cell types. Its inhibitory potency is assessed using fluorescent pH indicators or radiolabeled sodium flux assays. It demonstrates cardioprotective effects in isolated cardiomyocyte models of ischemia-reperfusion injury.
|
| ln Vivo |
In vivo, Cariporide Mesylate has been investigated for the prevention of myocardial ischemia-reperfusion injury during cardiac surgery. It reduces myocardial infarct size and improves cardiac function in animal models. Clinical trials have evaluated its efficacy in patients undergoing coronary artery bypass grafting.
|
| Enzyme Assay |
NHE-1 inhibition assays use cells expressing NHE-1 and a fluorescent pH indicator such as BCECF-AM. Cariporide Mesylate is incubated with cells, and the rate of pH recovery after an acid load is measured by fluorescence. IC50 values are determined from dose-response curves.
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| Cell Assay |
Cardiomyocytes or cardiac cell lines are subjected to simulated ischemia-reperfusion injury in the presence of Cariporide Mesylate. Cell viability is measured by MTT or LDH release. Intracellular sodium and calcium levels are measured using fluorescent indicators such as SBFI and Fura-2.
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| Animal Protocol |
Animal models of myocardial ischemia-reperfusion injury use rats, rabbits, or pigs. Cariporide Mesylate is administered intravenously before ischemia or at reperfusion. Myocardial infarct size is measured by triphenyltetrazolium chloride staining. Cardiac function is assessed by echocardiography.
|
| References |
| Molecular Formula |
C13H21N3O6S2
|
|---|---|
| Molecular Weight |
379.44
|
| Exact Mass |
379.087
|
| CAS # |
159138-81-5
|
| Related CAS # |
Cariporide;159138-80-4
|
| PubChem CID |
178019
|
| Appearance |
Typically exists as solid at room temperature
|
| Boiling Point |
542.8ºC at 760mmHg
|
| Flash Point |
282.1ºC
|
| Vapour Pressure |
7.62E-12mmHg at 25°C
|
| LogP |
3.877
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
24
|
| Complexity |
554
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(C1=C(S(=O)(C)=O)C=C(C(NC(N)=N)=O)C=C1)C.CS(=O)(O)=O
|
| InChi Key |
FNDLQABGYJQJPH-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H17N3O3S.CH4O3S/c1-7(2)9-5-4-8(11(16)15-12(13)14)6-10(9)19(3,17)18;1-5(2,3)4/h4-7H,1-3H3,(H4,13,14,15,16);1H3,(H,2,3,4)
|
| Chemical Name |
N-(diaminomethylidene)-3-methylsulfonyl-4-propan-2-ylbenzamide;methanesulfonic acid
|
| Synonyms |
HOE642; Cariporide Mesylate salt; Cariporide Mesylate
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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)
|
| 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
|
|---|---|
| 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 | 2.6355 mL | 13.1773 mL | 26.3546 mL | |
| 5 mM | 0.5271 mL | 2.6355 mL | 5.2709 mL | |
| 10 mM | 0.2635 mL | 1.3177 mL | 2.6355 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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