Clamikalant sodium (HMR 1098) is a non-selective and ATP-sensitive potassium (KATP) channel blocker. Can be used for the study of arrhythmias.

Physicochemical Properties

Molecular Formula	C19H21CLN3NAO5S2
Molecular Weight	493.96
Exact Mass	493.051
CAS #	261717-22-0
PubChem CID	23697157
Appearance	White to off-white solid powder
LogP	4.779
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	8
Heavy Atom Count	31
Complexity	695
Defined Atom Stereocenter Count	0
InChi Key	SUEVHDKFEXAKAF-UHFFFAOYSA-M
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
Chemical Name	sodium;(5-chloro-2-methoxybenzoyl)-[2-[4-methoxy-3-(methylcarbamothioylsulfamoyl)phenyl]ethyl]azanide
HS Tariff Code	2934.99.9001
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)

Biological Activity

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].
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].
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.
References	[1]. Roles of endothelial nitric oxide synthase (eNOS) and mitochondrial permeability transition pore (MPTP) in epoxyeicosatrienoic acid (EET)-induced cardioprotection against infarction in intact rat hearts. J Mol Cell Cardiol. 2013 Ju. [2]. Improved myocardial function with supplement of levosimendan to Celsior solution. J Cardiovasc Pharmacol. 2014 Sep;64(3):256-65. [3]. Sarcolemmal ATP-sensitive potassium channel protects cardiac myocytes against lipopolysaccharide-induced apoptosis. Int J Mol Med. 2016 Sep;38(3):758-66.

Solubility Data

Solubility (In Vitro)

DMSO: 50 mg/mL (101.22 mM)

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. 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. 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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

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.