Alvelestat
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Alvelestat是一种口服生物可利用的中性粒细胞弹性蛋白酶（NE）抑制剂，pIC50值为7.9[1]。
可逆的NE抑制剂alvelestat是为治疗中性粒细胞驱动的炎症性肺部疾病如支气管扩张和慢性阻塞性肺疾病研发的。Alvelestat对人类NE具有高亲和性，Ki值为9.4 nM。该物质对人类NE的选择性比对其他丝氨酸蛋白酶强600多倍。在全血和细胞关联及爆炸释放试验中，alvelestat的pIC50值分别为7.36、7.32和7.3。在急性肺损伤模型中，使用alvelestat可显著降低人类NE诱导的血红蛋白和BAL羟脯氨酸水平。在吸烟诱导的气管炎症模型中，alvelestat可显著降低BAL中性粒细胞和IL-1β。此外，alvelestat可在慢性吸烟诱导的炎症和肺气肿模型中减轻炎症，并能抑制吸烟诱导的灌洗中性粒细胞和巨噬细胞增加[1]。
参考文献：
[1] Stevens T, Ekholm K, Grnse 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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 545.53 |
| Cas No. | 848141-11-7 |
| Formula | C25H22F3N5O4S |
| Solubility | ≥27.3 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| 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 |
| SDF | Download SDF |
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | Alvelestat是一种口服生物可利用的中性粒细胞弹性蛋白酶（NE）抑制剂，pIC50值为7.9。 | |||||
| 靶点 | NE | |||||
| IC50 | (pIC50=7.9,Ki=4.9 nM) | |||||
质量控制和MSDS
- 批次:
化学结构
