| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Cimlanod targets the cardiovascular system by releasing nitroxyl (HNO), a reactive nitrogen species with distinct cardiovascular effects. HNO exerts positive inotropic effects by modifying critical thiols in cardiac proteins (e.g., ryanodine receptor and SERCA), enhancing myocardial contractility and relaxation. It also has vasodilatory effects through activation of soluble guanylate cyclase and KATP channels, improving cardiac output and reducing preload and afterload.
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| ln Vitro |
In vitro, Cimlanod releases HNO in a pH-dependent manner when exposed to neutral pH, mimicking the physiological conditions of the bloodstream. The released HNO has been shown to modify thiol groups in cardiac proteins, leading to enhanced calcium handling and improved contractile function in isolated cardiomyocytes. The compound demonstrates positive inotropic and lusitropic effects in isolated cardiac preparations.
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| ln Vivo |
In vivo, Cimlanod has been studied in animal models of heart failure, demonstrating improved cardiac function, increased stroke volume, and reduced filling pressures. It exerts positive lusitropic and inotropic as well as vasodilatory effects, collectively improving hemodynamics in heart failure. The compound has been evaluated in clinical trials for the treatment of acute decompensated heart failure.
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| Enzyme Assay |
In vitro enzyme assays for HNO donors typically measure the rate of HNO release using specific probes such as fluorescent dyes (e.g., copper-based fluorescent probes) or electrochemical detection. Cimlanod is incubated in buffer at physiological pH (7.4), and HNO release is monitored over time. The amount of HNO released is quantified by comparison to a standard curve. The pH dependence of HNO release is assessed by varying the pH of the buffer. Thiol modification assays measure the ability of released HNO to modify protein thiols using Ellman's reagent or mass spectrometry.
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| Cell Assay |
Cellular assays for HNO donors typically use isolated cardiomyocytes or cardiac cell lines. Cells are treated with Cimlanod at various concentrations, and contractile function is assessed by measuring sarcomere shortening or calcium transients using fluorescent indicators (e.g., Fura-2 or Fluo-4). The positive inotropic and lusitropic effects are quantified. Cell viability and cytotoxicity assays are also performed to assess safety margins.
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| Animal Protocol |
In vivo animal studies for heart failure typically use rat or dog models of heart failure induced by myocardial infarction, rapid pacing, or pressure overload. Animals are administered Cimlanod intravenously, and hemodynamic parameters (cardiac output, stroke volume, left ventricular pressure, and filling pressures) are measured using catheterization or echocardiography. The compound's effects on cardiac function, vascular resistance, and survival are assessed.
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| ADME/Pharmacokinetics |
Cimlanod is administered intravenously for the treatment of heart failure. It delivers HNO via pH-dependent chemical breakdown when exposed to the neutral pH environment of the bloodstream. The compound has a short half-life consistent with its rapid HNO release and metabolism. Detailed PK parameters such as half-life, clearance, and volume of distribution are available from preclinical and clinical studies. The compound is metabolized to inactive metabolites and excreted via the kidneys.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of Cimlanod have been conducted in support of clinical development for heart failure. The compound is generally well-tolerated at therapeutic doses, with vasodilatory effects being the primary pharmacological action. Common side effects include hypotension, headache, and flushing, which are related to HNO-mediated vasodilation. Serious adverse effects are rare. The compound has been evaluated in clinical trials for safety and efficacy in heart failure patients.
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| Additional Infomation |
Cimlanod is being studied in the clinical trial NCT02819271 (a first-in-human study evaluating the safety of a single continuous intravenous (IV) infusion of CXL-1427 for up to 48 hours in healthy volunteers).
Cimlanod (BMS-986231, CXL-1427) is a second-generation nitroxyl (HNO) donor developed for the treatment of heart failure. It delivers HNO via pH-dependent chemical breakdown at neutral blood pH, exerting positive lusitropic and inotropic as well as vasodilatory effects. The compound has been studied in clinical trials for acute decompensated heart failure. It represents a novel approach to heart failure therapy through HNO-mediated cardiac and vascular effects. |
| Molecular Formula |
C5H7NO4S
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|---|---|
| Molecular Weight |
177.178380250931
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| Exact Mass |
177.009
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| CAS # |
1620330-72-4
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| PubChem CID |
76685198
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| Appearance |
White to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
351.6±44.0 °C at 760 mmHg
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| Flash Point |
166.5±28.4 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.543
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| LogP |
-0.27
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
11
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| Complexity |
219
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1=CC=C(C)O1)(NO)(=O)=O
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| InChi Key |
LIXKIXWSKOENAB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H7NO4S/c1-4-2-3-5(10-4)11(8,9)6-7/h2-3,6-7H,1H3
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| Chemical Name |
N-hydroxy-5-methylfuran-2-sulfonamide
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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 : ~125 mg/mL (~705.50 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (11.74 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 20.8 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: ≥ 2.08 mg/mL (11.74 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 20.8 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: ≥ 2.08 mg/mL (11.74 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 | 5.6440 mL | 28.2199 mL | 56.4398 mL | |
| 5 mM | 1.1288 mL | 5.6440 mL | 11.2880 mL | |
| 10 mM | 0.5644 mL | 2.8220 mL | 5.6440 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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