Sivelestat (ONO-5046)
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.
IC50为44 nM。
Sivelestat(ONO-5046)是一种嗜中性粒细胞弹性蛋白酶抑制剂。
人嗜中性粒细胞弹性蛋白酶是一种水解大多数结缔组织成分的蛋白酶,据报道其参与类风湿性关节炎、肺气肿、成人呼吸窘迫综合征以及败血性休克的组织损伤。
体外:研究发现,Sivelestat能够竞争性抑制人嗜中性粒细胞弹性蛋白酶,并能抑制大鼠、兔、小鼠和仓鼠的白细胞弹性蛋白酶。而即使是100 microM的Sivelestat也不能抑制凝血酶、纤溶酶、胰蛋白酶、胰腺激肽释放酶、血浆激肽释放酶、胰凝乳蛋白酶和组织蛋白酶G [1]。
体内:在动物研究中,由盲肠结扎和穿刺引起细菌感染的雄性Sprague-Dawley大鼠外科手术后立即腹腔注射50或100 mg / kg的Sivelestat。结果表明,在未处理的大鼠中,平均动脉压(MAP)和肾小球滤过率(GFR)降低,而血清尿素氮(BUN)和嗜中性粒细胞明胶酶相关脂质运载蛋白(NGAL)水平增加。研究发现,Sivelestat促进脓毒症大鼠的存活,恢复MAP和GFR损伤,并抑制BUN和NGAL水平增加。此外,Sivelestat可抑制大鼠中CLP诱导的巨噬细胞浸润[2]。
临床试验:在日本和韩国,Sivelestat被批准用于急性肺损伤,如全身炎症反应综合征患者的急性呼吸窘迫综合征[3]。
参考文献:
[1] Kawabata K,Suzuki M,Sugitani M,Imaki K,Toda M,Miyamoto T. ONO-5046, a novel inhibitor of human neutrophil elastase. Biochem Biophys Res Commun.1991 Jun 14;177(2):814-20.
[2] Li G,Jia J,Ji K,Gong X,Wang R,Zhang X,Wang H,Zang B. The neutrophil elastase inhibitor, sivelestat, attenuates sepsis-related kidney injury in rats. Int J Mol Med.2016 Sep;38(3):767-75.
[3] Aikawa N,Kawasaki Y. Clinical utility of the neutrophil elastase inhibitor sivelestat for the treatment of acute respiratory distress syndrome. Ther Clin Risk Manag.2014 Aug 5;10:621-9.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 434.46 |
Cas No. | 127373-66-4 |
Formula | C20H22N2O7S |
Solubility | ≥43.4 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | 2-(2-(4-(pivaloyloxy)phenylsulfonamido)benzamido)acetic acid |
SDF | Download SDF |
Canonical SMILES | O=C(O)CNC(C1=CC=CC=C1NS(=O)(C2=CC=C(OC(C(C)(C)C)=O)C=C2)=O)=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。 |
质量控制和MSDS
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