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Varespladib/伐瑞拉迪 {[allProObj[0].p_purity_real_show]}

货号：A176227 同义名： 伐瑞拉地 / LY315920

Varespladib是一种有效且选择性的非胰腺分泌型磷脂酶A2（sPLA）抑制剂，IC50为7 nM。

Varespladib/伐瑞拉迪 化学结构 CAS号：172732-68-2
Varespladib/伐瑞拉迪 化学结构
CAS号：172732-68-2
Varespladib/伐瑞拉迪 3D分子结构
CAS号：172732-68-2
Varespladib/伐瑞拉迪 化学结构 CAS号：172732-68-2
Varespladib/伐瑞拉迪 3D分子结构 CAS号：172732-68-2
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Varespladib/伐瑞拉迪 纯度/质量文件 产品仅供科研

货号：A176227 标准纯度： {[allProObj[0].p_purity_real_show]}
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Varespladib/伐瑞拉迪 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].
体内研究

Varespladib treatment suppresses the release of thromboxane A2 (TXA2) from isolated guinea pig lung bronchoalveolar lavage cells induced by human sPLA2, with an IC50 of 0.79 μM. The ED50 for Varespladib is 16.1 mg/kg[1].
体外研究

Varespladib (10 μM; 24 and 48 hours; HCjE cells) treatment completely inhibits the RA-induced increase in MUC16 protein in cell lysates at both time points[2].

Varespladib (10 μM; 24 and 48 hours; HCjE cells) treatment markedly reduces RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours[2].

Varespladib/伐瑞拉迪 细胞实验

Cell Line
Concentration Treated Time Description References
HaCaT cells 256 µM 24 h To test the inhibitory effect of Varespladib on the cytotoxicity of D. russelii and B. asper venoms, results showed no inhibition Nat Commun. 2023 Dec 14;14(1):7812.
HaCaT cells 128 µM 24 h To test the inhibitory effect of Varespladib on the cytotoxicity of various snake venoms, results showed no inhibition on any of the six tested venoms Nat Commun. 2023 Dec 14;14(1):7812.
HaCaT cells 22.9 μg/mL 24 h To evaluate the inhibitory effect of Varespladib on cytotoxicity induced by snake venom. Results showed that Varespladib significantly reduced the cytotoxicity of crude venom but had no significant effect on the purified CTx combination. Proc Natl Acad Sci U S A. 2024 May 7;121(19):e2315597121.
Rat citrated plasma 1 mM 30 min Varespladib alone significantly prevented the venom-induced procoagulant action for PT, with approximately 16.4% of decreasing being verified Front Pharmacol. 2022 Jan 12;12:812295.

Varespladib/伐瑞拉迪 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Snake venom-induced dermonecrosis model Intradermal injection 19 µg Single dose, duration of 72 hours To test the inhibitory effect of Varespladib on dermonecrosis induced by B. asper and C. atrox venoms, results showed significant reduction in lesion area Nat Commun. 2023 Dec 14;14(1):7812.
Mice Snake venom-induced dermonecrosis model Intradermal injection 19 μg Single injection, lasting 72 hours To evaluate the inhibitory effect of Varespladib on dermonecrosis induced by snake venom. Results showed that Varespladib significantly reduced dermonecrosis caused by East and West African N. nigricollis and N. pallida venoms. Proc Natl Acad Sci U S A. 2024 May 7;121(19):e2315597121.
Mice Snake envenoming model Intravenous injection 60 µg Single dose, monitored for 6 hours To test the efficacy of Varespladib as a solo therapy in preventing lethality caused by snake venom, results showed that Varespladib failed to fully prevent lethality but prolonged survival time. Nat Commun. 2020 Dec 15;11(1):6094
Mouse Mmp2-/- mice Oral 10 mg/kg Once daily for 2 days To investigate the effect of Varespladib on sPLA2 activity and inflammatory response in MMP-2 deficient mice, results showed that Varespladib significantly reduced sPLA2 activity and inflammatory response. J Am Heart Assoc. 2015 Mar 27;4(4):e001868
Mice ApoE2/2 mice Dietary supplementation 15 mg/kg or 150 mg/kg Once daily for 12 weeks To evaluate the effects of A-002 alone or in combination with pravastatin on atherosclerosis, lipids, and paraoxonase (PON) activity. A-002 significantly reduced atherosclerotic lesion area, increased fibrous cap size, and elevated HDL levels and plasma PON activity. J Lipid Res. 2009 Apr;50(4):623-9
Wistar rats Subcutaneous hemorrhage model Intraperitoneal injection 1 mM Single injection, 24-hour monitoring Varespladib alone or associated with antivenom exhibited a mild protective effect on the venom-induced subcutaneous haemorrhage Front Pharmacol. 2022 Jan 12;12:812295.
Mice Mmp9-/- mice Oral gavage 10 mg/kg Once daily for 5 days To determine the contribution of systemic sPLA2 to the lipid metabolic phenotype of MMP-9 deficiency. Varespladib partially restored the hepatic transcriptional responses to dietary cholesterol in MMP-9-deficient mice. J Am Heart Assoc. 2016 Sep 30;5(10):e004228

Varespladib/伐瑞拉迪 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 <<

Varespladib/伐瑞拉迪 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.

Varespladib/伐瑞拉迪 实验方案

计算器
存储液制备 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

Varespladib/伐瑞拉迪 技术信息

CAS号172732-68-2
分子式C21H20N2O5
分子量 380.39
SMILES Code CCC1=C(C2=C(C=CC=C2N1CC3=CC=CC=C3)OCC(O)=O)C(C(N)=O)=O
MDL No. MFCD00944812
别名 伐瑞拉地 ;LY315920
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Varespladib | 172732-68-2 | LY315920 | LY 315920 | LY-315920 | sPLA2 Inhibitor | Metabolic Enzyme/Protease | Phospholipase | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Varespladib/伐瑞拉迪 纯度/质量文件 | Varespladib/伐瑞拉迪 生物活性 | Varespladib/伐瑞拉迪 临床数据 | Varespladib/伐瑞拉迪 参考文献 | Varespladib/伐瑞拉迪 实验方案 | Varespladib/伐瑞拉迪 技术信息

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