Varespladib (LY315920)|172732-68-2|(伐瑞拉迪; LY315920)-陌孚医药/Medlife

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Varespladib (LY315920) (Synonyms: 伐瑞拉迪; LY315920)

目录号: PC12508 纯度: ≥98%

CAS No. :172732-68-2

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中文名称

Varespladib (LY315920)

中文别名

[[3-(氨基氧代乙酰基)-2-乙基-1-(苯基甲基)-1H-吲哚-4-基]氧基]乙酸;D-对甲砜基苯丝氨酸乙酯;伐瑞拉迪;伐瑞拉地

英文名称

Varespladib (LY315920)

英文别名

LY315920;Varespladib (LY315920);2-[[3-(2-Amino-2-oxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]Acetic Acid;LY-315920;LY315920(Varespladib);N-(3,4-dimethoxyphenyl)-6,7-dimethoxyquinazolin-4-amine;Varespladib;2-[[3-(2-Amino-2-oxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]-acetic acid;A-001;[[3-(Aminooxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]acetic acid;LY-333013;2-(1-benzyl-2-ethyl-3-oxamoylindol-4-yl)oxyacetic acid;2-(3-(2-amino-2-oxoacetyl)-1-benzyl-2-ethyl-1H-indol-4-yloxy)acetic acid

Cas No.

172732-68-2

分子式

C₂₁N₂O₅H₂₀

分子量

380.39

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Varespladib (LY315920) is a potent and selective group IIA, secretory phospholipase A₂ (sPLA₂) inhibitor with an IC₅₀ of 9 nM. Varespladib exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC₅₀s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively.

性状

Solid

IC50 & Target[1][2]

sPLA2

9 nM (IC₅₀)

体外研究(In Vitro)

Varespladib (10 μM; 24 and 48 hours; HCjE cells) treatment results in complete inhibition of the RA-induced increase in MUC16 protein detected in cell lysates at both time points.
Varespladib (10 μM; 24 and 48 hours; HCjE cells) treatment significantly inhibits RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	HCjE cells
Concentration:	10 μM
Incubation Time:	24 hours and 48 hours
Result:	Significantly inhibited the RA-induced MUC16 protein expression at both time points.

RT-PCR

Cell Line:	HCjE cells
Concentration:	10 μM
Incubation Time:	24 hours and 48 hours
Result:	Significantly inhibited RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours.

体内研究(In Vivo)

Varespladib treatment inhibits human sPLA₂-induced release of thromboxane A₂ (TXA₂) from isolated guinea pig lung bronchoalveolar lavage cells with an IC₅₀ of 0.79 μM. And the ED₅₀ for Varespladib is 16.1 mg/kg.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Hartley guinea pigs (300-500 g)
Dosage:	3 mg/kg, 10 mg/kg, and 30 mg/kg
Administration:	Intravenous injection (Pharmacokinetic study)
Result:	Consistent inhibition of sPLA₂ activity in BAL fluid was observed. Reduced the human sPLA₂-induced generation of TXA₂ on BAL cells from guinea pigs.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

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. 1 [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (262.89 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6289 mL	13.1444 mL	26.2888 mL
5 mM	0.5258 mL	2.6289 mL	5.2578 mL
10 mM	0.2629 mL	1.3144 mL	2.6289 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制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

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.5 mg/mL (6.57 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.57 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 17% Polyethylene glycol 12-hydroxystearate in saline
Solubility: 1.5 mg/mL (3.94 mM); Suspended solution; Need ultrasonic

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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