1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. NF449 octasodium

NF449 octasodium 

Cat. No.: HY-112461A
Handling Instructions

NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a G-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs.

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NF449 octasodium Chemical Structure

NF449 octasodium Chemical Structure

CAS No. : 627034-85-9

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Description

NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a G-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs[1][2].

In Vitro

NF449 suppressed the rate of GTP[γS] binding to rGsα-s while barely affecting binding to rGiα-1 (IC50=140 nM), inhibits stimulation of adenylyl cyclase activity in S49 cyc− membranes (deficient in endogenous Gsα) by exogenously added Gsα-s, and blocks the coupling of β-adrenergic receptors to Gs (EC50=7.9 μM)[2].

In Vivo

At a dose of 10 mg/kg, NF449 inhibits the ex vivo aggregation triggered by 5 g/ml collagen in WT mouse platelets without affecting that induced by 5 μM ADP. At a higher dose (50 mg/kg), NF449 inhibits ex vivo platelet aggregation in response to not only 10 g/ml collagen but also 5 M ADP, indicating nonselective inhibition of the P2Y1 and/or P2Y12 receptor[3].

Molecular Weight

1505.09

Formula

C₄₁H₂₄N₆Na₈O₂₉S₈

CAS No.

627034-85-9

SMILES

O=C(NC1=CC(C(NC2=CC=C(S(=O)(O[Na])=O)C=C2S(=O)(O[Na])=O)=O)=CC(C(NC3=CC=C(S(=O)(O[Na])=O)C=C3S(=O)(O[Na])=O)=O)=C1)NC4=CC(C(NC5=CC=C(S(=O)(O[Na])=O)C=C5S(=O)(O[Na])=O)=O)=CC(C(NC6=CC=C(S(=O)(O[Na])=O)C=C6S(=O)(O[Na])=O)=O)=C4

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Keywords:

NF449 octasodiumP2X ReceptorP2XRsGTPselectiveadenylylcyclaseGsantithromboticaggregationplateletInhibitorinhibitorinhibit

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NF449 octasodium
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