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TPN171

Name: TPN171
Brand: TargetMol
SKU: T13193
Price: 133 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T13193Cas No. 1229018-87-4

TPN171 is potent PDE5 inhibitor with subnanomolar potency for PDE5 and good selectivity over PDE6, which has the potential for the treatment of pulmonary arterial hypertension (PAH). TPN171 was proven to exert a longer lasting effect than sildenafil in animal models, providing a foundation for a once-daily oral administration for its clinical use.

TPN171

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Purity: 99.83%

Catalog No. T13193Cas No. 1229018-87-4

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$133	In Stock	In Stock
5 mg	$337	In Stock	In Stock
10 mg	$487	In Stock	In Stock
25 mg	$738	In Stock	In Stock
50 mg	$981	In Stock	In Stock
100 mg	$1,350	In Stock	In Stock
500 mg	$2,710	-	In Stock
1 mL x 10 mM (in DMSO)	$370	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.83%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

TPN171 AI Summary

TPN171 is a potent inhibitor of human phosphodiesterase 5A1 (PDE5A1) with an IC50 value of 0.62 nM. It exhibits good metabolic stability, retaining 91.0% of its presence in human liver microsomes. The compound demonstrates a binding affinity to the PDE5A1 catalytic domain with a dissociation constant (Kd) of 82.0 nM and characterized thermodynamic binding parameters (deltaG, deltaH, -TdeltaS). It shows high selectivity for PDE5A1 over other phosphodiesterase isoforms (PDE1, PDE2A1, PDE3, PDE4, PDE6C, PDE7, PDE8A1, PDE9A2, PDE10A, PDE11A4), with selectivity ratios exceeding 16,000 for most isoforms. Pharmacokinetic studies in Sprague-Dawley rats and Beagle dogs reveal key properties such as Tmax, Cmax, AUC, MRT, half-life, clearance, volume of distribution, and oral bioavailability, supporting its potential for therapeutic development. In phase 1 clinical trials involving humans, the terminal half-life of TPN171 was found to be 10.9 hours, further indicating its viability as a therapeutic agent..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	TPN171 is potent PDE5 inhibitor with subnanomolar potency for PDE5 and good selectivity over PDE6, which has the potential for the treatment of pulmonary arterial hypertension (PAH). TPN171 was proven to exert a longer lasting effect than sildenafil in animal models, providing a foundation for a once-daily oral administration for its clinical use.
Targets&IC50	PDE5:0.62 nM

Chemical Properties

Molecular Weight	441.57
Formula	C₂₄H₃₅N₅O₃
Cas No.	1229018-87-4
Smiles	CCCOc1ccc(NC(=O)CN2CCN(C)CC2)cc1-c1nc(CC)c(CC)c(=O)[nH]1
Relative Density.	1.20 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (113.23 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.26 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2646 mL	11.3232 mL	22.6465 mL	113.2323 mL
5 mM	0.4529 mL	2.2646 mL	4.5293 mL	22.6465 mL
10 mM	0.2265 mL	1.1323 mL	2.2646 mL	11.3232 mL
20 mM	0.1132 mL	0.5662 mL	1.1323 mL	5.6616 mL
50 mM	0.0453 mL	0.2265 mL	0.4529 mL	2.2646 mL
100 mM	0.0226 mL	0.1132 mL	0.2265 mL	1.1323 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc