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Varespladib

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Chemical Structure| 172732-68-2 同义名 : 伐瑞拉地 ;LY315920;​Varespladib
CAS号 : 172732-68-2
货号 : A176227
分子式 : C21H20N2O5
纯度 : 99%+
分子量 : 380.394
MDL号 : MFCD00944812
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(276.03 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Varespladib (LY315920) is a potent and selective inhibitor of group IIA secretory phospholipase A2 (sPLA2) with an IC50 of 9 nM. It significantly inhibits sPLA2 activity in serum from various species, including rats, rabbits, guinea pigs, and humans, with IC50 values of 8.1 nM, 5.0 nM, 3.2 nM, and 6.2 nM, respectively[1].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02218125 Healthy Phase 1 Completed - United States, Massachusetts ... 展开 >> Boston, Massachusetts, United States 收起 <<
NCT00522197 Lung Cancer P... 展开 >>recancerous Condition 收起 << Phase 2 Completed - -
NCT03614221 Atopic Dermatitis Phase 2 Not yet recruiting July 31, 2021 Taiwan ... 展开 >> Taipei Chang Gung Memorial Hospital Not yet recruiting Taipei, Taiwan, 10507 Contact: Yin-Ku Lin, MD., PhD.    886-2-24311311 ext 2127    lin1266@cgmh.org.tw    Principal Investigator: Yin-Ku Lin, MD., PhD.          Sub-Investigator: Chun-Bing Chen, MD.          Sub-Investigator: Chin-Yi Yang, MD.          Sub-Investigator: Chun-Wei Lu, MD.          Sub-Investigator: Wen-Hung Chung, MD., PhD.          Sub-Investigator: Chih-Yung Chiu, MD., PhD          Sub-Investigator: Shih-Chi Su, PhD.          Sub-Investigator: Lai-Chu See, PhD.          Linkou Chang Gung Memorial Hospital Not yet recruiting Taoyuan, Taiwan, 33305 Contact: Yin-Ku Lin, MD., PhD    886-2-241-3131 ext 2127    lin1266@cgmh.org.tw    Principal Investigator: Yin-Ku Lin, MD., PhD          Sub-Investigator: Chun-Bing Chen, MD.          Sub-Investigator: Chin-Yi Yang, MD.          Sub-Investigator: Chun-Wei Lu, MD.          Sub-Investigator: Wen-Hung Chung, MD., PhD          Sub-Investigator: Chih-Yung Chu, MD., PhD          Sub-Investigator: Shih-Chi Su, PhD.          Sub-Investigator: Lai-Chu See, PhD. 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.14mL

2.63mL

1.31mL

26.29mL

5.26mL

2.63mL
参考文献

[1]Snyder DW, et al. 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. J Pharmacol Exp Ther. 1999 Mar;288(3):1117-24.

[2]Hori Y, et al. Effect of retinoic acid on gene expression in human conjunctival epithelium: secretory phospholipase A2 mediates retinoic acid induction of MUC16. Invest Ophthalmol Vis Sci. 2005 Nov;46(11):4050-61.