Chemical Structure : TPN171
CAS No.: 1229018-87-4
货号: PC-49288Not For Human Use, Lab Use Only.
TPN171 (TPN-171) is a highly potent, selective phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 0.62 nM, 32-fold selectivity over PDE6.
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TPN171 (TPN-171) is a highly potent, selective phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 0.62 nM, 32-fold selectivity over PDE6.
TPN171 shows an excellent selectivity over PDE2, 3, 4, 7, 8, 9, and 10 (>16,129-fold), and 1610-fold selectivity over PDE11, which is much more selective than tadalafil (9-fold).
TPN171 (20 mg/kg) demonstrated antihypertensive effect in an acute model of hypertension in spontaneously hypertensive rats (SHR), rapidly and remarkably decreases the blood pressure.
TPN171 also shows the efficacy in pulmonary arterial hypertension (PAH) model comparable to that of sildenafil or bosentan, and its dose (1 mg/kg) is much lower than that of sildenafil (25 mg/kg) or bosentan (100 mg/kg).
分子量 | 441.576 | |
分子式 | C24H35N5O3 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
N-(3-(5,6-Diethyl-4(3H)-pyrimidone-2-yl)-4-n-propoxyphenyl)-2-(4-methylpiperazin-1-yl)acetamide |
1. Zhen Wang, et al. J Med Chem. 2019 May 23;62(10):4979-4990.
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