GSK180
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.
GSK180是一种强效的、选择性的和竞争性的犬尿氨酸-3-单加氧酶(KMO)抑制剂,IC50约为6 nM。[ 1 ]
GSK180抑制原代人肝细胞内源性KMO的作用,效力相似(IC50 = 2.6 μM)。GSK180适合静脉给药。GSK180抑制大鼠KMO的效力比抑制人类酶的作用轻微较弱,IC50为7 μM。GSK180浓度依赖性地从血浆蛋白中置换色氨酸。[ 1 ]
30 mg/kg的GSK180静脉注射给药Kmowt和Kmonull小鼠,用药1 h后的血浆水平分别达到263±98 μM和351±87 μM。GSK180引起Kmowt小鼠犬尿氨酸上升,但在Kmonull小鼠中未检测到犬尿氨酸改变,证实了这种增加源于KMO抑制。GSK180引起kmowt和kmonull小鼠循环色氨酸水平明显降低,表明该化合物具有与KMO抑制无关的附加作用。除大鼠红细胞(血液:血浆比为0.46)外,GSK180与大鼠血浆蛋白轻度结合(1 mM时游离部分7.7%,n = 2),表明最高的游离药物血浆水平(92 μM)超过细胞IC50 12倍。GSK180治疗引起犬尿氨酸和犬尿喹啉酸循环水平的快速提升,随着药物水平下降重新回到基线水平。AP强烈的炎性细胞浸润包括MPO阳性嗜中性粒细胞以及ED1抗原阳性和大鼠CD68同源基因阳性的单核细胞,其在诱导AP的大鼠胰腺组织中和接受GSK180治疗的诱导AP大鼠中呈现相同程度。[ 1 ]
参考文献:
[1]. Kynurenine-3-monooxygenase inhibition prevents multiple organ failure in rodent models of acute pancreatitis.Nat Med. 2016 Feb;22(2):202-9.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 276.07 |
Cas No. | 1799725-26-0 |
Formula | C10H7Cl2NO4 |
Solubility | ≥27.6 mg/mL in DMSO; insoluble in H2O; ≥14.04 mg/mL in EtOH with ultrasonic |
Chemical Name | 3-(5,6-dichloro-2-oxobenzo[d]oxazol-3(2H)-yl)propanoic acid |
SDF | Download SDF |
Canonical SMILES | ClC1=C(Cl)C=C2C(N(CCC(O)=O)C(O2)=O)=C1 |
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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