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NF449

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Catalog No. T210023Cas No. 389142-38-5

NF449 is a potent antagonist of the P2X1 receptor, displaying IC50 values of 0.28 nM, 0.69 nM, and 120 nM for rP2X1, rP2X1+5, and P2X2+3, respectively. It acts selectively against Gsα G proteins (G Protein). NF449 inhibits the binding rate of GTP[γS] to Gsα-s, suppresses the stimulation of adenylate cyclase activity, and blocks the coupling of β-adrenergic receptors with Gs.

NF449

NF449

😃Good
Catalog No. T210023Cas No. 389142-38-5
NF449 is a potent antagonist of the P2X1 receptor, displaying IC50 values of 0.28 nM, 0.69 nM, and 120 nM for rP2X1, rP2X1+5, and P2X2+3, respectively. It acts selectively against Gsα G proteins (G Protein). NF449 inhibits the binding rate of GTP[γS] to Gsα-s, suppresses the stimulation of adenylate cyclase activity, and blocks the coupling of β-adrenergic receptors with Gs.
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
NF449 is a potent antagonist of the P2X1 receptor, displaying IC50 values of 0.28 nM, 0.69 nM, and 120 nM for rP2X1, rP2X1+5, and P2X2+3, respectively. It acts selectively against Gsα G proteins (G Protein). NF449 inhibits the binding rate of GTP[γS] to Gsα-s, suppresses the stimulation of adenylate cyclase activity, and blocks the coupling of β-adrenergic receptors with Gs.
In vitro
NF449 hinders the binding rate of GTP[γS] to rGsα-s while having minimal effect on rGiα-1 binding (IC 50 = 140 nM). It suppresses the stimulation of adenylate cyclase activity in S49 cyc- membranes (lacking endogenous Gsα) through exogenously added Gsα-s and obstructs the coupling of β-adrenergic receptors with Gs (EC 50 = 7.9 μM).
In vivo
At a dosage of 10 mg/kg, NF449 inhibits platelet aggregation triggered by 5 g/mL collagen in WT mice without affecting aggregation induced by 5 μM ADP. At a higher dose (50 mg/kg), NF449 inhibits ex vivo platelet aggregation in response to both 10 g/mL collagen and 5 μM ADP, indicating non-selective inhibition of P2Y1 and/or P2Y12 receptors.
Chemical Properties
Molecular Weight1329.24
FormulaC41H32N6O29S8
Cas No.389142-38-5
SmilesO=C(NC=1C=C(C=C(C1)C(=O)NC2=CC=C(C=C2S(=O)(=O)O)S(=O)(=O)O)C(=O)NC3=CC=C(C=C3S(=O)(=O)O)S(=O)(=O)O)NC=4C=C(C=C(C4)C(=O)NC5=CC=C(C=C5S(=O)(=O)O)S(=O)(=O)O)C(=O)NC6=CC=C(C=C6S(=O)(=O)O)S(=O)(=O)O
Storage & Solubility Information
StoragePowder: -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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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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
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