NF 449 CAS: 389142-38-5
MF: C41H24N6O29S8•8Na
MW: 1505.09
A selective G-protein antagonist.

NF 449 (CAS 389142-38-5)

NF 449 | CAS 389142-38-5 is rated 5.0 out of 5 by 1.
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Synonym: 4,4',4'',4'''-[Carbonylbis(imino-5,1,3-be nzenetriyl-bis(carbonylimino))]tetrakis-1,3-benzen edisulfonic acid octasodium salt
Application: A selective G-protein antagonist
CAS Number: 389142-38-5
Purity: ≥95%
Molecular Weight: 1505.09
Molecular Formula: C41H24N6O29S88Na
* Refer to Certificate of Analysis for lot specific data (including water content).
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NF 449 is a selective Gsα-subunit G-protein antagonist which reduces the association rate of guanosine 5'-[γ-thio]triphosphate ([35S]GTP[γS]) binding to Gα s -s (Gs&alpha-s) and inhibits the stimulation of adenylyl cyclase activity in S49 cyc- membranes. In addition, NF 449 interferes with binding between the Adenosine A1-R (A1-adenosine receptor) and its cognate G proteins (Gi/Go). Alternate studies suggest that NF449 inhibits a wide array of P2 receptors such as P2X3, P2Y1, and P2Y2, while showing the highest selectivity towards P2X1. Furthermore, NF449 can disrupt the coupling of β-AR (β-adrenergic receptors).


References

1. Hohenegger, M., et al. 1998. Proc. Natl. Acad. Sci. U.S.A. 95: 346-351. PMID: 9419378
2. Braun, K., et al. 2001. Naunyn Schmiedebergs Arch. Pharmacol. 364: 285-290. PMID: 11521173
3. Kassack, M.U., et al. 2004. Eur J Med Chem. 39: 345-357. PMID: 15072843

Physical State :
Solid
Solubility :
Soluble in water (100 mg/ml) with gentle warming.
Storage :
Store at 4° C
IC50 :
rP2X1: IC50 = 0.28 nM; rP2X1+5: IC50 = 0.69 nM; rP2X2+3: IC50 = 120 nM; GTPγS binding to Gsα-s-subunit: IC50 = 140 nM; Coupling of β-adrenergic receptors to Gs: EC5050 = 7.9 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
5310945
EC Number :
MFCD03791135
SMILES :
[Na]OOOSc1ccc(NC(=O)c2cc(NC(=O)Nc3cc(cc(c3)C(=O)Nc3ccc(cc3S(=O)(=O)O[Na])S(=O)(=O)O[Na])C(=O)Nc3ccc(SOOO[Na])cc3SOOO[Na])cc(c2)C(=O)Nc2ccc(cc2S(=O)(=O)O[Na])S(=O)(=O)O[Na])c(SOOO[Na])c1

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NF 449  Product Citations

See how others have used NF 449. Click on the entry to view the PubMed entry .

Citations 1 to 5 of 5 total

PMID: # 30731136  Höllerhage, M. et al. 2019. Neuropharmacology. 149: 13-26.

PMID: # 28611772  Villagra-Blanco, R.|Silva, LMR.|Muñoz-Caro, T.|Yang, Z.|Li, J.|Gärtner, U.|Taubert, A.|Zhang, X.|Hermosilla, C.| et al. 2017. Front Immunol. 8: 606.

PMID: # 24641330  Chi, Y. et al. 2014. British journal of pharmacology. 171: 3448-62.

PMID: # 22276108  Rasmuson, A. et al. 2012. PloS one. 7: e29331.

PMID: # 23022524  Kumar, DP. et al. 2012. Biochemical and biophysical research communications. 427: 600-5.

Citations 1 to 5 of 5 total
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Rated 5 out of 5 by from Kassack et al Kassack et al. (PubMed ID 15072843) showed that NF449 is a potent and selective P2X(1) antagonist. -SCBT Publication Review
Date published: 2015-04-27
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