| 中文名称 |
Varespladib methyl
|
| 英文名称 |
Varespladib methyl
|
| 英文别名 |
Acetic acid,[[3-(aminooxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]-, methylester;(3-AMINOOXALYL-1-BENZYL-2-ETHYL-1H-INDOL-4-YLOXY)-ACETIC ACID METHYL ESTER;A-002;LY333013;S-3013;Varespladib methyl
|
| Cas No. |
172733-08-3
|
| 分子式 |
C22H22N2O5
|
| 分子量 |
394.42
|
| 包装储存 |
-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
|
| 详情描述 |
Varespladib methyl (A-002; LY333013) 是一种选择性的磷脂酶 A2 (PLA2) 抑制剂。
|
| 产品详情 |
Varespladib methyl (A-002; LY333013) 是一种选择性的磷脂酶 A2 (PLA2) 抑制剂。
|
| 生物活性 |
Varespladib methyl (A-002; LY333013) is a selective inhibitor of group II secretory phospholipase A2 (PLA2).
|
| 性状 |
Solid
|
| IC50 & Target[1][2] |
phospholipase A2 (PLA2)
|
| 体外研究(In Vitro) |
Varespladib methyl (LY333013) is an orally-administered methyl ester pro-drug that is metabolized to LY315920. Varespladib and its orally bioavailable prodrug, Varespladib methyl (methyl-Varespladib) shows high-level secretory PLA2 (sPLA2) inhibition at nanomolar and picomolar concentrations against 28 medically important snake venoms from six continents. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
|
| 储存方式 |
-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
|
| ClinicalTrial |
|
| 参考文献 |
[1]. Bradley JD, et al. A randomized, double-blinded, placebo-controlled clinical trial of LY333013, a selective inhibitor of group II secretory phospholipase A2, in the treatment of rheumatoid arthritis. J Rheumatol. 2005 Mar;32(3):417-23.[2]. Lewin M, et al. Varespladib (LY315920) Appears to Be a Potent, Broad-Spectrum, Inhibitor of Snake Venom Phospholipase A2 and a Possible Pre-Referral Treatment for Envenomation. Toxins (Basel). 2016 Aug 25;8(9). pii: E248.
|
| 溶解度数据 |
In Vitro: DMSO : 100 mg/mL (253.54 mM; Need ultrasonic)配制储备液
|
[1]. Bradley JD, et al. A randomized, double-blinded, placebo-controlled clinical trial of LY333013, a selective inhibitor of group II secretory phospholipase A2, in the treatment of rheumatoid arthritis. J Rheumatol. 2005 Mar;32(3):417-23.[2]. Lewin M, et al. Varespladib (LY315920) Appears to Be a Potent, Broad-Spectrum, Inhibitor of Snake Venom Phospholipase A2 and a Possible Pre-Referral Treatment for Envenomation. Toxins (Basel). 2016 Aug 25;8(9). pii: E248.
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。