| CAS NO: | 1232221-74-7 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 413.48 |
|---|---|
| Formula | C23H23N7O |
| CAS No. | 1232221-74-7 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: ≥ 35 mg/mL |
| Water: <1 mg/mL | |
| Ethanol: N/A | |
| Other info | Chemical Name: (E)-4-(5-(2-(3-methylbenzylidene)hydrazinyl)-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)morpholine InChi Key: RFZQYGBLRIKROZ-PCLIKHOPSA-N InChi Code: 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+ SMILES Code: CC1=CC(/C=N/NC2=NC3=CC(C4=CC=NC=C4)=NN3C(N5CCOCC5)=C2)=CC=C1 |
| Synonyms | APY0201; APY-0201; APY 0201. |
| In Vitro | In vitro activity: APY0201 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.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). 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). |
|---|---|
| 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 |
| Animal model | |
| Formulation & Dosage | 30 mg/kg |
| References | Bioorg Med Chem. 2014 Jun 1;22(11):3021-9. |
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