![ApexBio/Alvelestat/100mg/B1037](images/ApexBio/B1037.png)
- Sivelestat sodium salt
- ARP 100
AlvelestatNE inhibitor |
Sample solution is provided at 25 µL, 10mM.
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Quality Control & MSDS
- View current batch:
- Purity = 99.67%
- COA (Certificate Of Analysis)
- HPLC (Retest)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
![Alvelestat](images/ApexBio/B1037.png)
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) |
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Alvelestat Dilution Calculator
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Cas No. | 848141-11-7 | SDF | Download SDF |
Synonyms | N/A | ||
Chemical Name | 6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-((5-(methylsulfonyl)pyridin-2-yl)methyl)-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2-dihydropyridine-3-carboxamide | ||
Canonical SMILES | CC(N1C2=CC=CC(C(F)(F)F)=C2)=C(C3=CC=NN3C)C=C(C1=O)C(NCC4=NC=C(S(C)(=O)=O)C=C4)=O | ||
Formula | C25H22F3N5O4S | M.Wt | 545.53 |
Solubility | ≥27.3mg/mL in DMSO | Storage | Store at -20°C |
Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
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. |
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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看有关产前诊断的一个资料,提到:“凡是酶活性能在成纤维细胞中表达均可用绒毛或羊水细胞的酶活性测定进行产前诊断,如溶酶体贮积症。”
不太理解,为什么成纤维细胞中表达的酶就能在绒毛或羊水细胞中测出来呢?绒毛的细胞跟成纤维细胞没什么直接关系吧?或者是因为成纤维细胞脱落到羊水中,破裂,然后就可以检测了?
求各位解答,谢谢。
它只是一个检验科的检验设备,用来化验血液、尿液中的成分浓度,医生据此来诊断疾病,可以查很多项目,如乙肝五项等等,不能直接检查什么疾病。
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