APY0201

COA

级别和纯度:

≥98%

CAS编号: 1232221-74-7
分子式: C₂₃H₂₃N₇O
分子量: 413.5
PubChem编号: 56927660

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货号 (SKU)	包装规格	是否现货
A646803-1mg	1mg	期货
A646803-2mg	2mg	期货
A646803-5mg	5mg	期货
A646803-10mg	10mg	期货
A646803-50mg	50mg	期货
A646803-100mg	100mg	期货

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Immunology/Inflammation (1938) Interleukin Related (132) PI3K/Akt/mTOR (764) PIKfyve (9)

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基本描述

规格或纯度	≥98%
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。
储存温度	-20°C储存
运输条件	超低温冰袋运输
作用类型	抑制剂
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
纯度	≥98%

关联靶点（人）

PIKFYVE Tchem 1-phosphatidylinositol 3-phosphate 5-kinase (270 活性数据)

点击查看靶蛋白信息： PIKFYVE

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

关联靶点（其它种属）

Hdac6 Histone deacetylase 6 (222 活性数据)

点击查看靶蛋白信息： Hdac6

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

Murine hepatitis virus (113 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

rep Replicase polyprotein 1ab (378 活性数据)

点击查看靶蛋白信息： rep

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

SARS-CoV-2 (38078 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

作用机制

作用机制	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	参考文献

名称和识别符

分子类型	小分子
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
Isomeric SMILES	CC1=CC(=CC=C1)/C=N/NC2=NC3=CC(=NN3C(=C2)N4CCOCC4)C5=CC=NC=C5
PubChem CID	56927660
MeSH Entry Terms	APY0201
分子量	413.5

化学和物理性质

溶解性	DMSO : ≥ 35 mg/mL (84.65 mM)
分子量	413.500 g/mol
XLogP3	3.300
氢键供体数Hydrogen Bond Donor Count	1
氢键受体数Hydrogen Bond Acceptor Count	7
可旋转键计数Rotatable Bond Count	5
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	31
形式电荷Formal Charge	0
复杂度Complexity	592.000
同位素原子数Isotope Atom Count	0
定义的原子立体中心计数Defined Atom Stereocenter Count	0
未定义的原子立体中心计数Undefined Atom Stereocenter Count	0
定义的键立体中心计数Defined Bond Stereocenter Count	1
未定义的键立体中心计数Undefined Bond Stereocenter Count	0
所有立体化学键的总数The total count of all stereochemical bonds	1
共价键合单元计数Covalently-Bonded Unit Count	1

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