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Product details

名称

APY0201

分子类型

小分子

英文名称

APY0201

货号

A646803-5mg

包装规格

5mg

浓度

≥98%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

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

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。

CAS号

1232221-74-7

分子式

C23H23N7O

分子量

413.5 g/mol

PubChem编号

56927660

Isomeric SMILES

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

IIUPAC Name

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

INCHI

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+

InChi Key

RFZQYGBLRIKROZ-PCLIKHOPSA-N

Smiles

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

PubChem CID

56927660

MeSH Entry Terms

APY0201

溶解性

DMSO : ≥ 35 mg/mL (84.65 mM)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

413.196 Da

单同位素质量Monoisotopic Mass

413.196 Da

拓扑极表面积Topological Polar Surface Area

79.900 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

592.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

3.300

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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