APY0201

CAS: 1232221-74-7 货号: A654749 分子式: C23H23N7O 分子量: 413.5 PubChem CID: 56927660
有货
级别和纯度: Moligand™ ? Moligand™ —— 阿拉丁的配体和生物活性小分子系列。适用于需要明确小分子工具的受体、通路和结合研究。 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
A654749-1ml
期货 Stock Image
¥1,299.90
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概述


APY0201 is a potent PIKfyve inhibitor, which inhibits the conversion of PtdIns3P to PtdIns(3,5)P 2 in the presence of in the presence of [ 33 P]ATP with an IC 50 of 5.2 nM. APY0201 also inhibits IL-12/IL-23 production.

In Vitro

APY0201 works differently from anti-IL-12/23 antibodies and acts by inhibiting production of these proinflammatory cytokines with characteristic selectivity over other cytokines, including tumor necrosis factor-alpha (TNF-α). In stimulated thioglycollate-induced mouse peritoneal exudate cells (TG-PEC), APY0201 strongly inhibits IL-12p70 and IL-12p40 production, with IC 50 s of 8.4 and 16 nM, respectively. APY0201 also inhibits IL-12p40 at 99 nM in human PBMC. APY0201 shows significant selectivity for the production of IL-12p70 and IL-12p40 over TNF-α, and this selectivity is maintained across species. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Oral APY0201 at a 30 mg/kg dose shows significant reduction of IL-12p70 production (78% inhibition relative to that of the vehicle control), which implys that the inhibitory potential of APY0201 against IL-12 is confirmed in the animal experiment . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:PIKfyve 5.2 nM (IC 50 ) IL-12 IL-23

规格

规格或纯度
Moligand™, 10mM in DMSO
英文名称
APY0201
生化机理
APY0201 是一种强效的 PIKfyve 抑制剂,它能抑制 PtdIns3P 向 PtdIns(3,5)P 2 的转化,在 [ 33 P]ATP 存在的情况下,IC 50 为 5.2 nM。APY0201 还能抑制 IL-12/IL-23 的产生。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC1=CC(=CC=C1)/C=N/NC2=NC3=CC(=NN3C(=C2)N4CCOCC4)C5=CC=NC=C5
PubChem CID
MeSH Entry Terms
APY0201
分子量
413.5

高级数据

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