1232221-74-7
1232221-74-7 structure
- Name: APY0201
- Chemical Name: N-(3-methylbenzylidene)-N'-(7-morpholin-2-pyridin-4-yl-pyrazolo[1,5-a]pyrimidin-5-yl)hydrazine
- CAS Number: 1232221-74-7
- Molecular Formula: C23H23N7O
- Molecular Weight: 413.47500
- Catalog: Signaling Pathways Immunology/Inflammation Interleukin Related
- Create Date: 2016-07-02 13:59:45
- Modify Date: 2024-01-07 08:38:11
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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.
| Name | N-(3-methylbenzylidene)-N'-(7-morpholin-2-pyridin-4-yl-pyrazolo[1,5-a]pyrimidin-5-yl)hydrazine |
|---|---|
| Synonyms |
N-(3-methyl-benzylidene)-N'-(7-morpholin-4-yl-2-pyridin-4-yl-pyrazolo[1,5-a]pyrimidin-5-yl)-hydrazine
N-(3-methyl-benzylidene)-N'-(7-morpholin-4-yl-2-pyridin-4-yl-pyrazolo[1,5-a]pyrimidin-5-yl)hydrazine APY0201 (E)-4-(5-(2-(3-methylbenzylidene)hydrazinyl)-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)morpholine |
| Description | 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. |
|---|---|
| Related Catalog | |
| Target |
PIKfyve:5.2 nM (IC50) IL-12 IL-23 |
| 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 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[1]. |
| 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[1]. |
| Cell Assay | Mouse TG-PEC or human PBMC are incubated with APY0201 (1, 10, 100, 1000 and 104 nM) in the presence of 100 ng/mL mouse or human IFN-γ and 0.05%w/v Staphylococcus aureus Cowan I strain (SAC)[1]. |
| Animal Admin | Mice[1] Female BALB/c mice (n=3) are used. Blood samples (systemic) or from the portal vein (portal) under anesthesia. After 30 min, mice are anesthetized with diethyl ether, and blood samples are collected by cardiacpuncture. Blood is collected in tubes containing 0.5 M-EDTA solution (pH 8.0). |
| References |
| Molecular Formula | C23H23N7O |
|---|---|
| Molecular Weight | 413.47500 |
| Exact Mass | 413.19600 |
| PSA | 79.94000 |
| LogP | 3.52030 |
| Appearance | light yellow solid |
| Storage condition | -20℃ |