| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 500mg |
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| Targets |
KR-32568 targets sodium-hydrogen exchanger isoform-1 (NHE-1), a membrane transporter that regulates intracellular pH by exchanging extracellular sodium for intracellular hydrogen ions. NHE-1 plays a critical role in myocardial ischemia-reperfusion injury, where its activation leads to intracellular sodium and calcium overload, contributing to cell death. KR-32568 is a preclinical NHE-1 inhibitor with an IC50 of 0.23 μM.
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| ln Vitro |
KR-32568 (10 nM–1 μM) prevents acidification caused by NHE-1.-produced distal floating in concentration-suspended form with an IC50 value of 24 nM in rabbit rich trap cells[1].
In vitro, KR-32568 is an NHE-1 inhibitor with an IC50 of 0.23 μM. It inhibits the sodium-hydrogen exchanger, preventing intracellular sodium and calcium overload. These in vitro properties make KR-32568 a valuable tool for studying NHE-1 function and its role in ischemia-reperfusion injury and cardioprotection. |
| ln Vivo |
KR-32568 (0.1-1.0 mg/kg; iv; once) exerts effective cardioprotective effects, such as reducing infarct size and significantly reducing the total number of premature ventricular contractions [1].
In vivo, KR-32568 has demonstrated quantified cardioprotection in ischemia-reperfusion models. By inhibiting NHE-1, it reduces intracellular sodium and calcium overload during ischemia and reperfusion, protecting the heart from injury. These in vivo effects support its potential for treating myocardial ischemia-reperfusion injury and other conditions involving NHE-1 dysregulation. |
| Enzyme Assay |
The in vitro enzyme/receptor binding assay for KR-32568 involves measuring its inhibition of NHE-1 activity. This can be assessed using cells expressing NHE-1 or using membrane preparations. NHE-1 activity is measured by monitoring intracellular pH changes using fluorescent pH indicators (e.g., BCECF) or by measuring sodium-dependent proton efflux. The compound is incubated with cells or membranes at various concentrations, and the IC50 for NHE-1 inhibition is calculated.
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| Cell Assay |
The in vitro cell-based assay for KR-32568 involves culturing cells expressing NHE-1 (e.g., cardiomyocytes or fibroblasts) and treating them with the compound to assess effects on intracellular pH regulation. Cells are loaded with a pH-sensitive fluorescent dye (e.g., BCECF) and subjected to an acid load (e.g., ammonium chloride pulse). The rate of pH recovery (sodium-dependent proton efflux) is measured in the presence or absence of KR-32568. Cell viability is assessed using MTT or LDH release assays.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (350-380 g) underwent 30 minutes ischemia/2.5 hrs (hrs (hours)) reperfusion cardiac injury [1]
Doses: 0.1 mg/kg and 1.0 mg/kg Route of Administration: intravenous (iv) (iv)injection; Experimental Results: Produces effective cardioprotective effects in rats. In vivo animal studies for KR-32568 are conducted in rodent models of myocardial ischemia-reperfusion injury. Rats or mice undergo temporary coronary artery occlusion followed by reperfusion. KR-32568 is administered intravenously or orally before or during ischemia. Infarct size is measured by TTC staining, and cardiac function is assessed by echocardiography. Biomarkers of cardiac injury (e.g., troponin) are measured in blood samples. Standard protocols for ischemia-reperfusion models are employed. |
| ADME/Pharmacokinetics |
KR-32568 has a molecular weight of 261.25 and a molecular formula of C13H12FN3O2. It is a small molecule NHE-1 inhibitor with an IC50 of 0.23 μM. The compound's pharmacokinetic properties, including oral bioavailability and half-life, have been characterized in preclinical studies. It can be formulated for in vivo administration. Detailed PK parameters are available from preclinical studies.
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| Toxicity/Toxicokinetics |
The toxicity profile of KR-32568 has been evaluated in preclinical studies. As an NHE-1 inhibitor, its primary safety concerns would relate to effects on cardiac function and electrolyte balance. Standard toxicology assessments would include acute and sub-chronic toxicity studies in rodents and dogs, with endpoints including clinical signs, body weight, clinical pathology, and histopathology. No significant toxicity has been reported in available literature.
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| References |
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| Additional Infomation |
KR-32568 is a research compound and has not been approved for clinical use. It is a preclinical NHE-1 inhibitor with an IC50 of 0.23 μM that has demonstrated quantified cardioprotection in ischemia-reperfusion models. KR-32568 is a valuable tool for studying NHE-1 function and its role in myocardial ischemia-reperfusion injury and cardioprotection.
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| Molecular Formula |
C13H12FN3O2
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|---|---|
| Molecular Weight |
261.256
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| Exact Mass |
261.091
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| Elemental Analysis |
C, 59.77; H, 4.63; F, 7.27; N, 16.08; O, 12.25
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| CAS # |
852146-73-7
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| PubChem CID |
11368995
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| Appearance |
White to off-white solid powder
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| Density |
1.38g/cm3
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| Boiling Point |
444.1ºC at 760 mmHg
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| Flash Point |
222.4ºC
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| Index of Refraction |
1.617
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| LogP |
3.208
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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 |
2
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| Heavy Atom Count |
19
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| Complexity |
371
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DTLDHYBZLVASJQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H12FN3O2/c1-7-2-3-8(14)6-9(7)10-4-5-11(19-10)12(18)17-13(15)16/h2-6H,1H3,(H4,15,16,17,18)
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| Chemical Name |
N-(aminoiminomethyl)-5-(5-fluoro-2-methylphenyl)-2-furancarboxamide
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| Synonyms |
KR-32568; KR 32568; KR32568;
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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 (~382.78 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.57 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 (9.57 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8276 mL | 19.1380 mL | 38.2760 mL | |
| 5 mM | 0.7655 mL | 3.8276 mL | 7.6552 mL | |
| 10 mM | 0.3828 mL | 1.9138 mL | 3.8276 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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