阿吡莫德
货号:
IA3370
品牌:
Jinpan
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产品简介
有效期 | 2年 |
描述 | 是 IL-12/IL-23 的有效抑制剂。 |
别名 | 阿匹莫德;STA-5326 |
英文名称 | Apilimod |
CAS | 541550-19-0 |
分子式 | C23H26N6O2 |
分子量 | 418.49 |
储存条件 | -20℃ |
纯度 | ≥98% |
外观(性状) | Powder |
单位 | 瓶 |
生物活性 | Apilimod (STA-5326) 是一种有效的细胞因子 interleukin-12 (IL-12) 和 interleukin-23 (IL-23) 的口服抑制剂,具有治疗某些自身免疫和炎性疾病的潜力。Apilimod (STA-5326) 可抑制IL-12,在IFN-γ/SAC刺激的人PBMC细胞、人单核细胞和小鼠PBMC细胞中,对应的IC50值分别为1 nM、1 nM和2 nM。Apilimod (STA-5326) 也是一种具有细胞通透性的小分子化合物,抑制PIKfyve,IC50为14 nM。[1-2] |
In Vitro | Apilimod selectively inhibits TLR-induced cytokine expression. It selectively inhibits the production of IL12p40, whereas it has little effect on IL8 production in THP-1 cells[1]. Apilimod inhibits not only PtdIns(3,5)P2 but also PtdIns5P synthesis and that the cytoplasmic vacuolization triggered by the inhibitor is precluded or reversed by BafA1 through a mechanism associated, in part, with reduction in both PtdIns3P levels and EEA1 membrane recruitment.[2] |
SMILES | CC1=CC=CC(/C=N/NC2=CC(N3CCOCC3)=NC(OCCC4=CC=CC=N4)=N2)=C1 |
靶点 | Interleukin Related |
动物实验 | HeLa cells are metabolically labeled with [3H]inositol for 72 hr and treated with two doses of apilimod or the inactive analog API09 for 120 min. Lipids are extracted, deacetylated, and analyzed by HPLC.[1] |
数据来源文献 | [1] Cai X, et al. Chem Biol. 2013, 20(7):912-21. [2] Diego Sbrissa, et al. PLoS One. 2018, 13(9): e0204532. |
规格 | 2mg 5mg |