NF449
Based on 7 publication(s) in Google Scholar
NF449 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 is a Gsα-selective G Protein antagonist. NF449 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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- CAS No.: 389142-38-5
- Formule: C41H32N6O29S8
- Masse moléculaire:1329.24
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) NF449
More- Cell Host Microbe. 2025 Sep 30:S1931-3128(25)00375-0. [Abstract]
- Proc Natl Acad Sci U S A. 2024 Oct 29;121(44):e2318767121. [Abstract]
- EMBO J. 2025 Sep 1. [Abstract]
- J Agric Food Chem. 2026 Apr 22;74(15):12132-12144. [Abstract]
- Vet Parasitol. 2026 May:344:110769. [Abstract]
- Vet Parasitol. 2022 Dec:312:109841. [Abstract]
- bioRxiv. 2026 Jun 3.
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Bio/Physico-chemical Assay
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Activité biologique
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p2x1 Receptor |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 389142-38-5
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Masse moléculaire 1329.24
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Formule C41H32N6O29S8
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SMILES
O=C(NC1=CC(C(NC2=CC=C(S(=O)(O)=O)C=C2S(=O)(O)=O)=O)=CC(C(NC3=CC=C(S(=O)(O)=O)C=C3S(=O)(O)=O)=O)=C1)NC4=CC(C(NC5=CC=C(S(=O)(O)=O)C=C5S(=O)(O)=O)=O)=CC(C(NC6=CC=C(S(=O)(O)=O)C=C6S(=O)(O)=O)=O)=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (7)
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Journal Impact Factor
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Most Recent
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Cell Host Microbe
Immunometabolic reprogramming of macrophages by gut microbiota-derived cadaverine controls colon inflammation. [Abstract]2025 Sep 30:S1931-3128(25)00375-0. PMID: 41033313 -
Proc Natl Acad Sci U S A
The pyruvate-GPR31 axis promotes transepithelial dendrite formation in human intestinal dendritic cells. [Abstract]2024 Oct 29;121(44):e2318767121. PMID: 39432783
NF449 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2024 Oct 29;121(44):e2318767121. [Abstract]
NF449 octasodium (10 μM; 30 min), a Gsα-subunit-selective G-protein antagonist，canceled PA-induced dendrite protrusion of iPSC-derived cDC1s.
NF449 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2024 Oct 29;121(44):e2318767121. [Abstract]
NF449 octasodium (10 μM; 30 min), a Gsα antagonist, abolished the significant increase in the percentage of OVA+ cells displaying antigen uptake among GPR31-expressing iPSC-derived cDC1s during PA stimulation.
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EMBO J
GNAS/PKA signaling promotes aberrant osteochondral differentiation of Gli1+ tendon sheath progenitors. [Abstract]2025 Sep 1. PMID: 40890486 -
J Agric Food Chem
Preventive Effect of Caffeic Acid Phenethyl Ester, an Active Component of Propolis, against TNF-α-Induced Endothelial Dysfunction through the β2-Adrenoceptor-Mediated eNOS/NO Signal Pathway. [Abstract]2026 Apr 22;74(15):12132-12144. PMID: 41957988 -
Vet Parasitol
2026 May:344:110769. PMID: 41967379 -
Vet Parasitol
Giardia duodenalis trophozoites triggered bovine neutrophil extracellular traps formation dependent on P2X1 receptor and PAD4 in vitro. [Abstract]2022 Dec:312:109841. PMID: 36427458
NF449 purchased from MedChemExpress. Usage Cited in: Vet Parasitol. 2022 Dec:312:109841. [Abstract]
The purinergic P2X1 receptor's inhibitor NF449 octasodium (10 mM; 30 min) sharply declined Giardia duodenalis trophozoites-triggered NET formation.
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Pureté et documentation
Références
[1]. Rettinger J, et al. Profiling at recombinant homomeric and heteromeric rat P2X receptors identifies the suramin analogue NF449 as a highly potent P2X1 receptor antagonist. Neuropharmacology. 2005;48(3):461-468. [Content Brief]
[2]. Hohenegger M, et al. Gsalpha-selective G protein antagonists. Proc Natl Acad Sci U S A. 1998;95(1):346-351. [Content Brief]
[3]. Hechler B, et al. Inhibition of platelet functions and thrombosis through selective or nonselective inhibition of the platelet P2 receptors with increasing doses of NF449 [4,4',4'',4'''-(carbonylbis(imino-5,1,3-benzenetriylbis-(carbonylimino)))tetrakis-benzene-1,3-disulfonic acid octasodium salt]. J Pharmacol Exp Ther. 2005;314(1):232-243. [Content Brief]
Calculators
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NF449 Related Classifications
HY-112461 Related Classifications
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