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TPN171

Chemical Structure : TPN171

CAS No.: 1229018-87-4

TPN171 (TPN-171)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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).

Physicochemical Properties

M.Wt 441.576
Formula C24H35N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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