货号	规格	价格	上海	北京	珠海	重庆	武汉
S82490-2mg	≥98%	￥600.00 S82490-2mg ￥600.00 3-5天	0 货期：3-5天	-	-	-	-
S82490-5mg	≥98%	￥990.00 S82490-5mg ￥990.00 3-5天	0 货期：3-5天	-	-	-	-
S82490-10mg	≥98%	￥1700.00 S82490-10mg ￥1700.00 3-5天	0 货期：3-5天	-	-	-	-
S82490-50mg	≥98%	￥4420.00 S82490-50mg ￥4420.00 3-5天	0 货期：3-5天	-	-	-	-
S82490-100mg	≥98%	￥7070.00 S82490-100mg ￥7070.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

APY0201 is a potent PIKfyve inhibitor, which inhibits the conversion of PtdIns3P to PtdIns(3,5)P2 in the presence of in the presence of [33P]ATP with an IC50 of 5.2 nM. APY0201 also inhibits IL-12/IL-23 production.

靶点：

IL-12;IL-23;PIKfyve:5.2 nM (IC50);PI3K; Interleukin

体外研究：

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 IC50s 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

体内研究：

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

参考文献：

1. Hayakawa N, et al. Structure-activity relationship study, target identification, and pharmacological characterization of a small molecular IL-12/23 inhibitor, APY0201. Bioorg Med Chem. 2014 Jun 1;22(11):3021-9.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.419 ml	12.093 ml	24.185 ml
5 mM	0.484 ml	2.419 ml	4.837 ml
10 mM	0.242 ml	1.209 ml	2.419 ml
50 mM	0.048 ml	0.242 ml	0.484 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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