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GSK180

现货
Catalog No.
A8723
犬尿氨酸-3-单加氧酶(KMO)抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 3,500.00
Ship with 40 days
25mg
¥ 12,000.00
Ship with 40 days

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Background

GSK180 is a potent, selective and competitive inhibitor of kynurenine-3-monooxygenase (KMO) with an IC50 of ~6 nM. [1]

 

GSK180 inhibited endogenous KMO action in primary human hepatocytes with similar potency (IC50 = 2.6 µM). GSK180 is proper for i.v. administration. GSK180 inhibited rat KMO mildly less potently than it did the human enzyme with an IC50 of 7 µM. GSK180 exhibited a concentration-dependent displacement of tryptophan from plasma proteins. [1]

 

GSK180 was dosed to Kmowt and Kmonull mice as a bolus injection at 30 mg/kg, which delivered plasma levels 1 h after dosage of 263 ± 98 µM and 351 ± 87 µM, respectively. GSK180 resulted in a promotion in kynurenine in Kmowt mice, but no change was detected in the Kmonull mice, which confirms that this increase results from the inhibition of KMO. GSK180 caused an evident reduction in circulating tryptophan levels in both Kmowt and Kmonull mice, suggesting that the chemical had an additional effect unrelated to KMO inhibition. GSK180 is excepted from rat erythrocytes (blood:plasma ratio of 0.46), and it is modestly bound to rat plasma proteins (free fraction 7.7% at 1 mM, n = 2), meaning that the top free drug levels in plasma (92 µM) are >12-fold above the IC50 in cells. Treatment with GSK180 resulted in a rapid promotion in the circulating levels of both kynurenine and kynurenic acid, which restablished to baseline as the drug levels dropped. The fierce inflammatory cell infiltrate in AP consisted of MPO-positive neutrophils and monocytes positive for the ED1 antigen, the rat ortholog of CD68, which were present to the same extent in the pancreas tissue of rats with induced AP and rats with induced AP treated with GSK180. [1]

 

Reference:

[1]. Kynurenine-3-monooxygenase inhibition prevents multiple organ failure in rodent models of acute pancreatitis.Nat Med. 2016 Feb;22(2):202-9.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt276.07
Cas No.1799725-26-0
FormulaC10H7Cl2NO4
Solubility≥27.6mg/mL in DMSO
Chemical Name3-(5,6-dichloro-2-oxobenzo[d]oxazol-3(2H)-yl)propanoic acid
SDFDownload SDF
Canonical SMILESClC1=C(Cl)C=C2C(N(CCC(O)=O)C(O2)=O)=C1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

质量控制

化学结构

GSK180