NF449

Name: NF449
Brand: TargetMol
SKU: T210023
Rating: 4.5 (1 reviews)

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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

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Catalog No. T210023Cas No. 389142-38-5

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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 Weight	1329.24
Formula	C₄₁H₃₂N₆O₂₉S₈
Cas No.	389142-38-5

Storage & Solubility Information

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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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DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

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mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

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