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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
By inhibiting GSNOR, Cavosonstat increases intracellular levels of S-nitrosoglutathione (GSNO), which enhances S-nitrosylation of target proteins. This promotes the maturation and plasma membrane stabilization of the cystic fibrosis transmembrane conductance regulator (CFTR) protein.
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| ln Vitro |
The CFTR modulator Cavosonstat (N91115) works in tandem with CFTR correctors and enhancers to support the maturation of the cystic fibrosis transmembrane conductance regulator (CFTR) and the stability of the plasma membrane [1].
In vitro, Cavosonstat acts as a CFTR modulator. It promotes CFTR maturation and plasma membrane stability. Its mechanism is complementary to that of CFTR correctors and potentiators, making it a valuable tool for combination therapy research. |
| ln Vivo |
In vivo, Cavosonstat is a CFTR stabilizer with the potential to be used for cystic fibrosis. By increasing GSNO levels and promoting S-nitrosylation, it enhances CFTR function and reduces oxidative stress.
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| Enzyme Assay |
In vitro enzyme assays measure the inhibition of GSNOR activity by Cavosonstat. This is typically performed using a biochemical assay where the enzyme is incubated with its substrate and the inhibitor, and the reaction rate is measured.
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| Cell Assay |
In vitro cell-based assays are performed in CF airway epithelial cell models. Cells are treated with Cavosonstat, and the effect on CFTR maturation, stability, and function is assessed by measuring CFTR protein levels (via Western blot) and chloride ion transport (using a fluorescent dye or Ussing chamber).
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| Animal Protocol |
In vivo efficacy is evaluated in animal models of cystic fibrosis, such as CFTR-knockout mice. The compound is administered orally, and its effect on CFTR function and disease-related phenotypes, such as airway inflammation and bacterial infection, is assessed.
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| ADME/Pharmacokinetics |
Cavosonstat is an orally bioavailable small molecule, making it a convenient therapeutic option. Its pharmacokinetic properties support once- or twice-daily oral dosing. Its absorption, distribution, metabolism, and excretion have been characterized in preclinical studies.
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| Toxicity/Toxicokinetics |
The toxicological profile of Cavosonstat has been evaluated in preclinical studies. As a GSNOR inhibitor, its safety is of paramount importance, as GSNO plays a role in various physiological processes. Clinical trials are needed to fully establish its safety in humans.
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| References | |
| Additional Infomation |
Cavosonstat is being investigated in the clinical trial NCT02589236 (the study of Cavosonstat (N91115) in homozygous CF patients with F508del-CFTR mutation).
Cavosonstat is an investigational drug that has been in clinical development for cystic fibrosis. It represents a novel approach to treating CF by targeting the nitric oxide pathway to stabilize CFTR, rather than directly correcting the underlying genetic mutation. |
| Molecular Formula |
C16H10CLNO3
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|---|---|
| Molecular Weight |
299.71
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| Exact Mass |
299.034
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| CAS # |
1371587-51-7
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| PubChem CID |
56960912
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
527.5±50.0 °C at 760 mmHg
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| Flash Point |
272.8±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.715
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| LogP |
4.28
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
392
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BXSZILNGNMDGSL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H10ClNO3/c17-13-8-10(16(20)21)1-4-12(13)15-5-2-9-7-11(19)3-6-14(9)18-15/h1-8,19H,(H,20,21)
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| Chemical Name |
3-chloro-4-(6-hydroxyquinolin-2-yl)benzoic acid
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| Synonyms |
N 91115 N-91115 Cavosonstat
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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 : ~50 mg/mL (~166.83 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.34 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 (8.34 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 | 3.3366 mL | 16.6828 mL | 33.3656 mL | |
| 5 mM | 0.6673 mL | 3.3366 mL | 6.6731 mL | |
| 10 mM | 0.3337 mL | 1.6683 mL | 3.3366 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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