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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 389142-38-5
- 分子式: C41H32N6O29S8
- 分子量:1329.24
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 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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P2X Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
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p2x1 Receptor |
体外実験
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. .
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 389142-38-5
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分子量 1329.24
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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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純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
NF449 関連分類
HY-112461 関連分類
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