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- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- 规格:
10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥880.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥800.0 |
| 规格: | 10 mg | 产品价格: | ¥1250.0 |
| 规格: | 25 mg | 产品价格: | ¥2800.0 |
| 规格: | 50 mg | 产品价格: | ¥4300.0 |
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PF-05085727
CAS No. : 1415637-72-7
MCE 国际站:PF-05085727
产品活性:PF-05085727 是一种强效的 cGMP 依赖性的 PDE2A (IC50=2 nM) 选择性和具有脑通透性的抑制剂。PF-05085727 对 PDE2A 的选择性是 PDE1 和 PDE3-11 的 4000 倍。
研究领域:Metabolic Enzyme/Protease
作用靶点:Phosphodiesterase (PDE)
In Vitro: PF-05085727 shows weak activity with IC50 of 162 μM to induce cell death in a cellular toxicity assay using transformed human liver endothelial (THLE) cells.
PF-05085727 (3 μM) shows a minimal inhibition of cytochrome P450 enzymes (CYPs), inhibits 1A2, 2C8, 2C9, 2D6 and 3A4 with percentage% of 16%, 18%, 7%, 4%, and 30%, respectively.
PF-05085727 (10 μM) inhibits PDE1B, PDE4B, PDE7B and PDE10A with IC50 values of 12.146 μM, 22,503 μM, 13.157 μM and 6.515 μM, respectively.
In Vivo: PF-05085727 (subcutaneous injection; 3.2 mg/kg/mice; 3 mg/kg/rat) gives a ratio of unbound brain (Cbu) to unbound plasma (Cpu) of ca. 0.27 and 0.37, respectively.
PF-05085727 in mice leads to an acute and exposure-dependent elevation in the accumulation of bulk levels of cGMP in cortex, striatum, and hippocampus as measured by enzyme-linked immunosorbent assay.
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