SML1100
Varespladib
≥98% (HPLC), Secretory phospholipase A2 inhibitor, powder
别名:
2-[[3-（2-氨基-2-氧代乙酰基）-2-乙基-1-（苯甲基）-1H-吲哚-4-基]氧基]-乙酸, A-001, LY-315920, LY315920
产品名称
Varespladib, ≥98% (HPLC)
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 10 mg/mL, clear
储存温度
−20°C
SMILES字符串
[Na+].[n]2(c3c(c(ccc3)OCC(=O)[O-])c(c2CC)C(=O)C(=O)N)Cc1ccccc1
InChI
1S/C21H20N2O5.Na/c1-2-14-19(20(26)21(22)27)18-15(9-6-10-16(18)28-12-17(24)25)23(14)11-13-7-4-3-5-8-13;/h3-10H,2,11-12H2,1H3,(H2,22,27)(H,24,25);/q;+1/p-1
InChI key
XZZUHXILQXLTGV-UHFFFAOYSA-M
应用
伐瑞拉迪作为分泌型磷脂酶A2(sPLA2)抑制剂的应用实例：
- 检测其对神经鞘氨醇半乳糖苷(psychosine)诱导的人星形胶质细胞毒性的作用
- 检测其对黑蛇(P. colletti)蛇毒的中和作用
- 检测其联用蛇毒金属蛋白酶(SVMP)抑制剂Marimastat，对抗蝰蛇毒伤的保护作用
生化/生理作用
伐瑞拉迪(Varespladib)是抗蝰蛇和眼镜蛇毒液的有效解毒药，主要用于蛇咬伤治疗。根据体外结构研究，它可作用于磷脂酶A2(PLA2)样毒素的疏水性通道。它可阻断sPLA2相关的炎症级联反应。
伐瑞拉迪是一种有效且选择性的分泌型磷脂酶 A2（sPLA2）抑制剂。
伐瑞拉迪是一种有效且选择性的分泌型磷脂酶 A2（sPLA2）抑制剂。 化合物伐瑞拉迪在低 nM 浓度下抑制人和小鼠 sPLA2 IIA、V 和 X 组酶。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Laura-Oana Albulescu et al.
Nature communications, 11(1), 6094-6094 (2020-12-17)
Snakebite is a medical emergency causing high mortality and morbidity in rural tropical communities that typically experience delayed access to unaffordable therapeutics. Viperid snakes are responsible for the majority of envenomings, but extensive interspecific variation in venom composition dictates that
Christina N Zdenek et al.
Toxicology letters, 330, 176-184 (2020-05-23)
Venoms from Pseudechis species (Australian black snakes) within the Elapidae family are rich in anticoagulant PLA2 toxins, with the exception of one species (P. porphyriacus) that possesses procoagulant mutated forms of the clotting enzyme Factor Xa. Previously the mechanism of
Guilherme H M Salvador et al.
Scientific reports, 9(1), 17203-17203 (2019-11-22)
The World Health Organization recently listed snakebite envenoming as a Neglected Tropical Disease, proposing strategies to significantly reduce the global burden of this complex pathology by 2030. In this context, effective adjuvant treatments to complement conventional antivenom therapy based on
Cedric Misslin et al.
PloS one, 12(11), e0187217-e0187217 (2017-11-03)
Krabbe disease is a fatal rare inherited lipid storage disorder affecting 1:100,000 births. This illness is caused by mutations in the galc gene encoding for the enzyme galactosylceramidase (GALC). Dysfunction of GALC has been linked to the toxic build-up of
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