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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-TPN171
TPN171

Chemical Structure : TPN171

CAS No.: 1229018-87-4

TPN171 (TPN-171)

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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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).

物理化学性质&存储条件

分子量 441.576
分子式 C24H35N5O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(3-(5,6-Diethyl-4(3H)-pyrimidone-2-yl)-4-n-propoxyphenyl)-2-(4-methylpiperazin-1-yl)acetamide

参考文献

1. Zhen Wang, et al. J Med Chem. 2019 May 23;62(10):4979-4990.

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