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- 详细信息
- 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.
- 英文名:
PF-999
- 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/100 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: | ¥1400.0 |
| 规格: | 25 mg | 产品价格: | ¥2900.0 |
| 规格: | 50 mg | 产品价格: | ¥4900.0 |
| 规格: | 100 mg | 产品价格: | ¥8800.0 |
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PF-05180999
CAS No. : 1394033-54-5
MCE 国际站:PF-05180999
产品活性:PF-05180999 (PF-999) 是一种磷酸二酯酶 2A (PDE2A) 抑制剂,IC50 值为 1.6 nM。
研究领域:Metabolic Enzyme/Protease
作用靶点:Phosphodiesterase (PDE)
In Vitro: PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM. PF-05180999 binds to the rat, dog and monkey PDE2A, with Kis of 4.2, 8.4, and 5.5 nM and IC50s of 2.6, 5.2, and 3.4 nM, respectively. PF-05180999 shows weak activity against PDE, with IC50s of 2.03 μM (PDE10A1), 26.969 μM (PDE7B), 50.09 μM (PDE11A4), and >56.25 μM (PDE1B1, PDE3A1, PDE4D3, PDE5A1, PDE6 (bovine), PDE8B, PDE9A1), respectively. PF-05180999 is also a weak inducer of CYP3A4, and with no direct inhibition of human recombinant cytochrome P450 (CYP) enzymes (1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A) and no induction of CYP1A2.
In Vivo: PF-05180999 (Compound 30; 0.032-0.32 mg/kg mg/kg, s.c.) dramatically reduces the working memory errors produced by ketamine in a working memory radial arm maze (RAM) model in rats. PF-05180999 causes acute and exposure-dependent elevation in the accumulation of cGMP bulk levels in the cortex, striatum, and hippocampus, but with no changes in cAMP and the associated downstream phospho-cAMP response element-binding protein (p-CREB) in mice.
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