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PL-3994

Name: PL-3994
Brand: TargetMol
SKU: T81444
Rating: 4.5 (1 reviews)

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Catalog No. T81444Cas No. 952295-80-6

PL-3994, a natriuretic peptide receptor-A (NPR-A) agonist resistant to neutral endopeptidase, functions as a bronchodilator, eliciting a concentration-dependent relaxation of pre-contracted guinea-pig trachea, evidenced by an IC50 of 42.7 nM [1].

PL-3994

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Catalog No. T81444Cas No. 952295-80-6

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
5 mg	Inquiry	Inquiry	Inquiry
50 mg	Inquiry	Inquiry	Inquiry

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

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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Product Introduction

Bioactivity

Description	PL-3994, a natriuretic peptide receptor-A (NPR-A) agonist resistant to neutral endopeptidase, functions as a bronchodilator, eliciting a concentration-dependent relaxation of pre-contracted guinea-pig trachea, evidenced by an IC50 of 42.7 nM [1].
In vitro	PL-3994 exhibits high binding affinity to recombinant NPR-As in human, canine, and rat models, with inhibition constants (K i) of 1 nM, 41 nM, and 10 nM, respectively.
In vivo	Intratracheal administration of PL-3994 at doses ranging from 1 to 1000 mg/kg (i.t.; single dose) elicits a dose-dependent attenuation of bronchoconstriction triggered by aerosolized methacholine; this occurs without markedly impacting cardiovascular parameters [1]. Notably, PL-3994 exhibits substantial resistance to human neutral endopeptidase (hNEP) degradation, maintaining 92% integrity after 2 hours, in contrast to the swift metabolism of natural counterparts, ANP and CNP, which display less than or equal to 1% remaining after 2 hours [1].

Chemical Properties

Molecular Weight	1875.19
Formula	C₈₂H₁₂₇N₂₇O₂₀S₂
Cas No.	952295-80-6
Smiles	C([C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H]2NC(=O)[C@H](CO)NC(=O)[C@]([C@H](CC)C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](CCCC)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC4=CN=CN4)NC(=O)[C@@H](NC(CCCCCC)=O)CSSC2)[H])(=O)N5[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C(N)=O)C5
Sequence	(Hept-cyclo(Cys-His-Phe-D-Ala-Gly-Arg-D-nle-Asp-Arg-Ile-Ser-Cys)-Tyr-(Arg mimetic)-NH2)
Sequence Short	Hept-cyclo(CHFAGRDRISC)-Y-(Arg mimetic)

Storage & Solubility Information

Storage

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

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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