| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
| ln Vitro |
At 8 or 16 hours, ciprofloxacin dramatically reduced cell death indicators such TUNEL positivity and caspase-3 cleavage. The buildup of Na+ and Ca2+ in the cytoplasm is strongly inhibited by carboride. Cariporide inhibits H2+O2+-induced decrease of mitochondrial membrane potential [1]. By blocking Na+/H+ exchange, ciporide (HOE-642) lowers cytosolic Ca2+ in cardiomyocytes, reducing cardiac ischemia/reperfusion injury [2]. Human platelet degranulation, platelet leukocyte aggregation formation, and GPIIb/IIIa receptor (PAC-1) activation are all inhibited by carbariporide (HOE-642) [3].
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| ln Vivo |
Caripoli injection intravenously dramatically lowers cerebral edema, brain swelling, and infarct volume in addition to brain Na+ uptake [4].
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| References |
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| Additional Infomation |
See also: Cariporide Mesylate (annotation moved to).
Drug Indication Investigated for use/treatment in cardiac surgery. Mechanism of Action Cariporide is a selective sodium-hydrogen antiporter inhibitor. The sodium-hydrogen exchanger is an importatn player in the pathophysiology of myocardial ischemia-referfusion injury. The accumulation of hydrogen ions in the myocyte cytoso; during ischemia creates a proton gradiant that promote the efflux of hydrogen ions in exchange for the influx of sodium ions. This sodium buildup can secondary activates the sodium-calcium exchanger to operate in the reverse mode, resulting in a net calcium accumulation in myocyte cytosol, which leads to dysfunction and cell death. By inhibiting sodium-hydrogen exchange, Cariporide can prevent the accumulation of calcium in cytosol, therefore reduce the infarct size. |
| Molecular Formula |
C12H17N3O3S
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|---|---|
| Molecular Weight |
283.34
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| Exact Mass |
283.099
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| CAS # |
159138-80-4
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| Related CAS # |
Cariporide (mesilate);159138-81-5
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| PubChem CID |
151172
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
542.8±60.0 °C at 760 mmHg
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| Flash Point |
282.1±32.9 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.602
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| LogP |
0.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
19
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| Complexity |
461
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IWXNYAIICFKCTM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H17N3O3S/c1-7(2)9-5-4-8(11(16)15-12(13)14)6-10(9)19(3,17)18/h4-7H,1-3H3,(H4,13,14,15,16)
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| Chemical Name |
N-(Diaminomethylidene)-3-methylsulfonyl-4-propan-2-ylbenzamide
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| Synonyms |
Cariporide HOE642 HOE-642 HOE 642
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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) |
DMSO : ≥ 100 mg/mL (~352.92 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.82 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.82 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 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: ≥ 2.5 mg/mL (8.82 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 | 3.5293 mL | 17.6466 mL | 35.2933 mL | |
| 5 mM | 0.7059 mL | 3.5293 mL | 7.0587 mL | |
| 10 mM | 0.3529 mL | 1.7647 mL | 3.5293 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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