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LY315920(Varespladib)
Catalog Number: E1KS1110
Amount: 5mg1​ PHYSICAL AND CHEMICAL PROPERTIES
Applications: Reactivity:
产品类型: Unconjugated
发货周期: 现货
说明书:     PDF
总价格:    633.6元
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概述
  • Catalog Number:

    E1KS1110
  • Amount:

    5mg1​ PHYSICAL AND CHEMICAL PROPERTIES
  • Storage/Stability:

    at -20℃ 2 years

2​ Biological Activity
LY315920(Varespladib) is a selective inhibitor of human, group IIA, nonpancreatic secretory PLA2 (sPLA2). In a chromogenic isolated enzyme assay, Varespladib inhibited sPLA2 activity with an IC50 of 9.6 ±1 nM or 7.3 ×10-6 mole fraction, which approached the stiochiometric limit of this assay. [1]Varespladib 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. [1] Human sPLA2-induced release of thromboxane A2 (TXA2) from isolated guinea pig lung bronchoalveolar lavage cells was inhibited by Varespladib with an IC50 of 0.79 mM. [1]Therefore,the use of Varespladib have a beneficial effect in preventing various inflammatory disease states. [1]
3​ References:
Pharmacology of LY315920/S-5920, [[3-(aminooxoacetyl)-2-ethyl-1- (phenylmethyl)-1H-indol-4-yl]oxy] acetate, a potent and selective secretory phospholipase A2 inhibitor: A new class of anti-inflammatory drugs, SPI. Snyder DW, et al. J Pharmacol Exp Ther. 1999 Mar;288(3):1117-24
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.

2​ Biological Activity LY315920(Varespladib) is a selective inhibitor of human, group IIA, nonpancreatic secretory PLA2 (sPLA2). In a chromogenic isolated enzyme assay, Varespladib inhibited sPLA2 activity with an IC50 of 9.6 ±1 nM or 7.3 ×10-6 mole fraction, which approached the stiochiometric limit of this assay. [1]Varespladib 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. [1] Human sPLA2-induced release of thromboxane A2 (TXA2) from isolated guinea pig lung bronchoalveolar lavage cells was inhibited by Varespladib with an IC50 of 0.79 mM. [1]Therefore,the use of Varespladib have a beneficial effect in preventing various inflammatory disease states. [1] 3​ References: Pharmacology of LY315920/S-5920, [[3-(aminooxoacetyl)-2-ethyl-1- (phenylmethyl)-1H-indol-4-yl]oxy] acetate, a potent and selective secretory phospholipase A2 inhibitor: A new class of anti-inflammatory drugs, SPI. Snyder DW, et al. J Pharmacol Exp Ther. 1999 Mar;288(3):1117-24 The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.

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