APY0201

小分子

APY0201

A646803-5mg

5mg

≥98%

-20°C储存

超低温冰袋运输

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

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。

1232221-74-7

C23H23N7O

413.5 g/mol

56927660

CC1=CC(=CC=C1)/C=N/NC2=NC3=CC(=NN3C(=C2)N4CCOCC4)C5=CC=NC=C5

N-[(E)-(3-methylphenyl)methylideneamino]-7-morpholin-4-yl-2-pyridin-4-ylpyrazolo[1,5-a]pyrimidin-5-amine

1S/C23H23N7O/c1-17-3-2-4-18(13-17)16-25-27-21-15-23(29-9-11-31-12-10-29)30-22(26-21)14-20(28-30)19-5-7-24-8-6-19/h2-8,13-16H,9-12H2,1H3,(H,26,27)/b25-16+

RFZQYGBLRIKROZ-PCLIKHOPSA-N

CC1=CC(=CC=C1)C=NNC2=NC3=CC(=NN3C(=C2)N4CCOCC4)C5=CC=NC=C5

56927660

APY0201

DMSO : ≥ 35 mg/mL (84.65 mM)

1

7

5

413.196 Da

413.196 Da

79.900 Ų

31

0

592.000

0

1

3.300