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1415637-72-7

中文名稱 PF-05085727
英文名稱 PF-05085727
CAS 1415637-72-7
分子式 C20H18F3N7
分子量 413.4
MOL 文件 1415637-72-7.mol
1415637-72-7 結(jié)構(gòu)式 1415637-72-7 結(jié)構(gòu)式

基本信息

中文別名
4-(氮雜環(huán)丁烷-1-基)-1-甲基-3-(1-甲基-5-(4-(三氟甲基)苯基)-1H-吡唑-4-基)-1H-吡唑并[3,4-D]嘧啶
英文別名
PF-05085727
PF-05085727 >=98% (HPLC)
4-(AZETIDIN-1-YL)-1-METHYL-3-(1-METHYL-5-(4-(TRIFLUOROMETHYL)PHENYL)-1H-PYRAZOL-4-YL)-1H-PYRAZOLO[3,4-D]PYRIMIDINE
1H-Pyrazolo[3,4-d]pyrimidine, 4-(1-azetidinyl)-1-methyl-3-[1-methyl-5-[4-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl]-

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度DMSO : 62.5 mg/mL (151.19 mM; Need ultrasonic)
形態(tài)Solid
顏色White to yellow
PF-05085727價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-102050PF-05085727
PF-05085727
1415637-72-75mg800元
2024/11/08HY-102050PF-05085727
PF-05085727
1415637-72-710mM * 1mLin DMSO880元
2024/11/08HY-102050PF-05085727
PF-05085727
1415637-72-710mg1250元

常見問題列表

生物活性
PF-05085727 是一種強(qiáng)效的 cGMP 依賴性的 PDE2A (IC50=2 nM) 選擇性和具有腦通透性的抑制劑。PF-05085727 對 PDE2A 的選擇性是 PDE1 和 PDE3-11 的 4000 倍。
靶點(diǎn)

PDE2A

2 nM (IC 50 )

體外研究

PF-05085727 shows weak activity with IC 50 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 IC 50 values of 12.146 μM, 22,503 μM, 13.157 μM and 6.515 μM, respectively.

體內(nèi)研究

PF-05085727 (subcutaneous injection; 3.2 mg/kg/mice; 3 mg/kg/rat) gives a ratio of unbound brain (C bu ) to unbound plasma (C pu ) 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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