| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
The primary target of Clamikalant sodium is the ATP-sensitive potassium (KATP) channel, specifically the Kir6.2/SUR subunits responsible for potassium efflux. It is a cardioselective KATP channel blocker, with 10- to 50-fold higher potency for blocking KATP channels in cardiac muscle cells compared to pancreatic beta-cells. By blocking KATP channels, Clamikalant sodium prevents potassium efflux, which can modulate cardiac action potential duration and contractility. It is used to study the role of KATP channels in cardiac electrophysiology and pathophysiology, particularly in the context of arrhythmias and cardioprotection.
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| ln Vitro |
Clamikalant sodium (HMR 1098; 40 μM) eliminates the inhibitory effect of Levosimendan on hypothermic preservation-induced calpain activation, cleavage of Bid, and apoptosis, and prevents the improved effect of Levosimendan on left ventricular developed pressure (LVDP) recovery rate[2]. Neonatal rat cardiomyocytes (NRCs) are exposed to clamikant sodium (HMR 1098; 30 µM, 24 hours) which decreases cellular viability and promotes apoptosis [3]. In LPS-exposed NRCs, clamikant sodium (30 µM) raises the Bax protein level and lowers the Bcl-2 protein level[3].
In vitro, Clamikalant sodium (HMR 1098; 40 μM) eliminates the inhibitory effect of Levosimendan on calpain activation, cleavage of Bid, and apoptosis induced by hypothermic preservation. In neonatal rat cardiomyocytes (NRCs), treatment with 30 µM Clamikalant sodium for 24 hours decreases cellular viability and promotes apoptosis. In LPS-exposed NRCs, Clamikalant sodium (30 µM) raises the Bax protein level and lowers the Bcl-2 protein level. The compound is a potent inhibitor of KATP channels and is used to study the role of these channels in various cellular processes. |
| ln Vivo |
Complete elimination of the cardioprotection resulting from epoxyeicosatrienoic acid (EET) treatment is achieved with clamikant sodium (HMR 1098; 6.0 mg/kg; 5 min before EET administration)[1].
In vivo, Clamikalant sodium has been shown to completely eliminate the cardioprotection resulting from epoxyeicosatrienoic acid (EET) treatment in animal models. The compound is administered at a dose of 6.0 mg/kg, 5 minutes before EET administration. This demonstrates the compound's ability to block KATP channels and modulate cardioprotective signaling pathways. Clamikalant sodium is used in the study of arrhythmias and to investigate the role of KATP channels in cardiac physiology and pathophysiology. |
| Enzyme Assay |
In vitro assays for Clamikalant sodium typically involve measuring its inhibition of KATP channel activity using patch-clamp electrophysiology on isolated cardiac myocytes or cell lines expressing recombinant KATP channels (Kir6.2/SUR). The compound is applied at concentrations ranging from 10-100 µM, and the resulting inhibition of potassium current is measured. Functional assays in cardiomyocytes assess the compound's effects on cell viability, apoptosis, and protein expression, as demonstrated in studies measuring Bax and Bcl-2 levels.
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: Neonatal rat cardiomyocytes (NRCs) Tested Concentrations: 30 µM Incubation Duration: 24 hrs (hours) Experimental Results: diminished cellular viability to 42.8±6.3% compared with the LPS group. Western Blot Analysis[3] Cell Types: Neonatal rat cardiomyocytes (NRCs) Tested Concentrations: 30 µM Incubation Duration: 24 hrs (hours) Experimental Results: diminished the Bcl-2 protein level and increased the Bax protein level. Cellular assays for Clamikalant sodium are often performed using neonatal rat cardiomyocytes (NRCs). NRCs are treated with Clamikalant sodium (typically 30-40 µM) for 24 hours. Cell viability is assessed using standard assays such as MTT or trypan blue exclusion. Apoptosis is evaluated by measuring Bax and Bcl-2 protein levels via Western blot analysis. These assays are used to study the role of KATP channels in cardiomyocyte survival, apoptosis, and the response to various stressors, such as LPS exposure or hypothermic preservation. |
| Animal Protocol |
In vivo animal studies for Clamikalant sodium typically involve the administration of the compound to rodent models to study its effects on cardiac function and arrhythmias. The compound can be administered via intravenous injection at doses such as 6.0 mg/kg. In studies of cardioprotection, Clamikalant sodium is administered prior to an ischemic event or before the administration of a cardioprotective agent like EET to block KATP channel-mediated protection. Endpoints include infarct size, cardiac function, arrhythmia incidence, and biochemical markers of injury.
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| ADME/Pharmacokinetics |
Clamikalant sodium (HMR 1098) is a cardioselective KATP channel blocker with a molecular weight of 493.96 g/mol and a logP of 4.779, indicating moderate lipophilicity. It is supplied as a white to off-white solid powder with a purity of ≥98%. For research purposes, the compound is typically stored under recommended conditions as per the Certificate of Analysis. Detailed parameters such as half-life, volume of distribution, and bioavailability are not fully available in the public domain but are characteristic of small molecule KATP channel blockers.
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| Toxicity/Toxicokinetics |
There is no specific toxicity data reported for Clamikalant sodium in the available literature beyond its classification as a research chemical. As a research chemical intended for laboratory use only, it should be handled with standard safety precautions for handling chemical reagents. The compound is not approved for human therapeutic use. Researchers should consult the material safety data sheet (MSDS) for detailed safety and handling information. Any potential toxicity would need to be assessed through formal toxicological studies if the compound were to be developed further.
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| References |
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| Additional Infomation |
KATP channel blocker; structure see first source.
Clamikalant sodium (HMR 1098) is a non-selective, ATP-sensitive potassium (KATP) channel blocker. It has a molecular formula of C19H21ClN3NaO5S2 and a molecular weight of 493.96 g/mol. Clamikalant sodium is a cardioselective KATP channel inhibitor and is used in the study of arrhythmias. It completely eliminates the cardioprotection resulting from EET treatment in vivo. The compound is available with a purity of ≥98% and is a white to off-white solid powder. |
| Molecular Formula |
C19H21CLN3NAO5S2
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| Molecular Weight |
493.96
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| Exact Mass |
493.051
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| CAS # |
261717-22-0
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| PubChem CID |
23697157
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| Appearance |
White to off-white solid powder
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| LogP |
4.779
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
31
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| Complexity |
695
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CNC(=S)NS(=O)(=O)C1=C(C=CC(=C1)CC[N-]C(=O)C2=C(C=CC(=C2)Cl)OC)OC.[Na+]
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| InChi Key |
SUEVHDKFEXAKAF-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C19H22ClN3O5S2.Na/c1-21-19(29)23-30(25,26)17-10-12(4-6-16(17)28-3)8-9-22-18(24)14-11-13(20)5-7-15(14)27-2;/h4-7,10-11H,8-9H2,1-3H3,(H3,21,22,23,24,29);/q;+1/p-1
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| Chemical Name |
sodium;(5-chloro-2-methoxybenzoyl)-[2-[4-methoxy-3-(methylcarbamothioylsulfamoyl)phenyl]ethyl]azanide
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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: 50 mg/mL (101.22 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.06 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 (5.06 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 (5.06 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 | 2.0245 mL | 10.1223 mL | 20.2446 mL | |
| 5 mM | 0.4049 mL | 2.0245 mL | 4.0489 mL | |
| 10 mM | 0.2024 mL | 1.0122 mL | 2.0245 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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