LY315920(Varespladib)|2mg|K1293-上海高创化学科技有限公司

LY315920(Varespladib)

参考价：¥1518

供货周期：

7天

品牌：

型号：

2mg

货号：

K1293

SKU:K1293		M. Wt:380.39
Formula:C21H20N2O5		Solubility:No
Purity:>99%		Storage:2 years at -20 degrees centigrade
CAS No.:172732-68-2		Synonyms:LY-333013
Chemical NameN/A

Description	LY315920(Varespladib)
Targets	sPLA2
IC50	9 nM
In vitro	LY315920 is a potent, selective inhibitor of recombinant human, group IIA, nonpancreatic secretory PLA2 (sPLA2). LY315920 inhibited sPLA2 activity with an IC50 of 9 nM. LY315920 was 40-fold less active against human, group IB, pancreatic sPLA2 and was inactive against cytosolic PLA2 and the constitutive and inducible forms of cyclooxygenase.
In vivo	LY315920 to transgenic mice expressing the human sPLA2 protein inhibited serum sPLA2 activity in a dose-related manner over a 4-h time course. In a model of acute pancreatitis in rats, the potent inhibitor of secretory phospholipase A2 (sPLA2), S-5920/LY315920Na significantly reduced mortality at 7 days, and strongly abrogated PLA2 activities in both plasma and ascites along with significant reduction of lipase activity, amylase, aspartate aminotransferase, and hemorrhage. Treatment with S-5920/LY315920Na 1 hr after OA infusion, but not 2 hrs after infusion, significantly attenuated the lung injury, as estimated by hypoxemia, decreased lung compliance, pulmonary edema, and vascular permeability.
Clinical Trials	N/A
Features	N/A

Description

LY315920(Varespladib)

Targets

sPLA2

IC50

9 nM

In vitro

LY315920 is a potent, selective inhibitor of recombinant human, group IIA, nonpancreatic secretory PLA2 (sPLA2). LY315920 inhibited sPLA2 activity with an IC50 of 9 nM. LY315920 was 40-fold less active against human, group IB, pancreatic sPLA2 and was inactive against cytosolic PLA2 and the constitutive and inducible forms of cyclooxygenase.

In vivo

LY315920 to transgenic mice expressing the human sPLA2 protein inhibited serum sPLA2 activity in a dose-related manner over a 4-h time course. In a model of acute pancreatitis in rats, the potent inhibitor of secretory phospholipase A2 (sPLA2), S-5920/LY315920Na significantly reduced mortality at 7 days, and strongly abrogated PLA2 activities in both plasma and ascites along with significant reduction of lipase activity, amylase, aspartate aminotransferase, and hemorrhage. Treatment with S-5920/LY315920Na 1 hr after OA infusion, but not 2 hrs after infusion, significantly attenuated the lung injury, as estimated by hypoxemia, decreased lung compliance, pulmonary edema, and vascular permeability.

Clinical Trials

N/A

Features

N/A