AlvelestatNE inhibitor CAS# 848141-11-7 |
- Sivelestat sodium salt
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Quality Control & MSDS
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| Cas No. | 848141-11-7 | SDF | Download SDF |
| PubChem ID | 46861623 | Appearance | Powder |
| Formula | C25H22F3N5O4S | M.Wt | 545.53 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | AZD9668 | ||
| Solubility | DMSO : ≥ 33 mg/mL (60.49 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 6-methyl-5-(2-methylpyrazol-3-yl)-N-[(5-methylsulfonylpyridin-2-yl)methyl]-2-oxo-1-[3-(trifluoromethyl)phenyl]pyridine-3-carboxamide | ||
| SMILES | CC1=C(C=C(C(=O)N1C2=CC=CC(=C2)C(F)(F)F)C(=O)NCC3=NC=C(C=C3)S(=O)(=O)C)C4=CC=NN4C | ||
| Standard InChIKey | QNQZWEGMKJBHEM-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C25H22F3N5O4S/c1-15-20(22-9-10-31-32(22)2)12-21(23(34)30-13-17-7-8-19(14-29-17)38(3,36)37)24(35)33(15)18-6-4-5-16(11-18)25(26,27)28/h4-12,14H,13H2,1-3H3,(H,30,34) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Alvelestat is an orally bioavailable inhibitor of neutrophil elastase (NE) with pIC50 value of 7.9 | |||||
| Targets | NE | |||||
| IC50 | (pIC50=7.9,Ki=4.9 nM) | |||||
Alvelestat Dilution Calculator
Alvelestat Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.8331 mL | 9.1654 mL | 18.3308 mL | 36.6616 mL | 45.827 mL |
| 5 mM | 0.3666 mL | 1.8331 mL | 3.6662 mL | 7.3323 mL | 9.1654 mL |
| 10 mM | 0.1833 mL | 0.9165 mL | 1.8331 mL | 3.6662 mL | 4.5827 mL |
| 50 mM | 0.0367 mL | 0.1833 mL | 0.3666 mL | 0.7332 mL | 0.9165 mL |
| 100 mM | 0.0183 mL | 0.0917 mL | 0.1833 mL | 0.3666 mL | 0.4583 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Alvelestat is an orally bioavailable inhibitor of neutrophil elastase (NE) with pIC50 value of 7.9[1].
The reversible NE inhibitor, alvelestat, is developed for treating the neutrophil-driven inflammatory lung diseases such as bronchiectasis and chronic obstructive pulmonary diseas. Alvelestat shows high affinity with human NE with a Ki value of 9.4nM. It is more than 600-fold selective for human NE over other serine proteases. In the whole-blood and cell- associated and explosive-release assays, alvelestat shows pIC50 values of 7.36, 7.32 and 7.3, respectively. In the acute lung injury model, administration of alvelestat significantly reduces the levels of hemoglobin and BAL hydroxyproline induced by human NE. In the smoke-induced airway inflammation model, alvelestat reduces both BAL neutrophils and IL-1β markedly. Furthermore, alvelestat can relieve inflammation and inhibit smoke-induced increases in lavage neutrophils and macrophages in a model of chronic smoke-induced inflammation and emphysema [1].
References:
[1] Stevens T, Ekholm K, Gränse M, et al. AZD9668: pharmacological characterization of a novel oral inhibitor of neutrophil elastase. Journal of Pharmacology and Experimental Therapeutics, 2011, 339(1): 313-320.
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Neutrophil extracellular traps contribute to the pathogenesis of acid-aspiration-induced ALI/ARDS.[Pubmed:29416730]
Oncotarget. 2017 Nov 28;9(2):1772-1784.
Background: Acute lung injury/acute respiratory distress syndrome (ALI/ARDS) is a manifestation of systemic inflammation in the lungs, but the factors that trigger inflammation in ALI/ARDS are unclear. We hypothesized that neutrophil extracellular traps (NETs) contribute to the pathogenesis of acid aspiration-induced ALI/ARDS. Results: Analysis of bronchial aspirates from ARDS patients showed that NETs were significantly correlated with the degree of ARDS (r = -0.5846, p = 0.0359). NETs in bronchoalveolar lavage fluid of acid-aspiration mice were significantly higher (141.6 +/- 23.08) at 3 h after injury than those in the sham group (1234 +/- 101.9; p = 0.003, n = 5 per group). Exogenous NETs aggravated lung injury, while Alvelestat and DNase markedly attenuated the intensity of ARDS. Materials and Methods: We investigated whether NETs are involved in the severity of gastric aspiration-induced ARDS. Then, a hydrochloric acid aspiration-induced ALI murine model was used to assess whether NETs are pathogenic and whether targeting NETs is protective. Exogenous NETs were administered to mice. Alvelestat can inhibit neutrophil elastase (NE), which serves an important role in NET formation, so we investigated whether Alvelestat could protect against ALI in cell and mouse models. Conclusions: NETs may contribute to ALI/ARDS by promoting tissue damage and systemic inflammation. Targeting NETs by Alvelestat may be a potential therapeutic strategy.
