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Merck
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Key Documents

5.08957

Sigma-Aldrich

PDE5 Inhibitor, Cpd7a

别名:

PDE5 Inhibitor, Cpd7a

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About This Item

经验公式(希尔记法):
C22H20ClN3O2
分子量:
393.87
分類程式碼代碼:
12352200
NACRES:
NA.77

化驗

≥98% (HPLC)

品質等級

形狀

solid

效力

270 pM IC50

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
protect from light

顏色

cream

溶解度

DMSO: 100 mg/mL

儲存溫度

2-8°C

一般說明

A cell-permeable, brain permeant, quinoline-based compound that acts as a highly potent and selective inhibitor of phosphodiesterase 5 (PDEV; IC50 = 270 pM). Exhibits over 10,000 fold greater selectivity over various other phosphodiestrases and trivial activity against PDE VI (IC50 = 339 nM). Shown to increase cGMP levels in mouse hippocampus and attenuates long term potentiation and memory defects in mice with elevated levels of oligomeric Aβ42. It is rapidly absorbed with peak plasma concentration observed at 30 min. Displays desirable pharmacokinetic properties with plasma t1/2 = 1.33 h and brain t1/2 = 1.04 h.
A cell-permeable, brain permeant, quinoline-based compound that acts as a highly potent and selective inhibitor of phosphodiesterase 5 (PDEV; IC50 = 270 pM). Exhibits over 10,000 fold greater selectivity over various other phosphodiestrases and trivial activity against PDE VI (IC50 = 339 nM). Shown to increase cGMP levels in mouse hippocampus and attenuates long term potentiation and memory defects in mice with elevated levels of oligomeric Aβ42. It is rapidly absorbed with peak plasma concentration observed at 30 min. Displays desirable pharmacokinetic properties with plasma t1/2 = 1.33 h and brain t1/2 = 1.04 h.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

生化/生理作用

Primary Target
PDE5
Reversible: yes

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他說明

Fiorito, J., et al. 2013. Eur. J. Med. Chem.60, 285.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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