Lalistat 1 是一种有效的、选择性的、竞争性的溶酶体酸性脂肪酶抑制剂，其 IC50 为 68 nM。Lalistat 1 是流感病毒的免疫球蛋白 A1 蛋白酶 (IgA1P) 的抑制剂，对其他丝氨酸水解酶，如胰蛋白酶或内酰胺酶等影响较小。Lalistat 1 可用于 C 型尼曼氏病 (NPC) 的相关研究。
| 生物活性 |
Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease. |
|---|---|
| 体外研究 |
Lalistat 1 (0-100 μM) shows activity against different non-typeable H. influenzae (NTHi) IgAP variants from clinical isolates in Elisa assay. It shows a dose-dependent inhibition of IgA1P B1 and B2, but at higher inhibitor concentrations, consistent with the higher expression levels of these variants. Nearly complete inhibition of IgA1P B1 and B2 is observed at 50 μM, with complete inhibition at 100 μM. |
| 分子式 |
C12N4O3SH18
|
| 分子量 |
298.36
|
| CAS号 |
501104-16-1
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
| 储存方式 |
-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
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