389142-38-5
Chemical Structure
NF449
- CAS No.: 389142-38-5
- Formula:C41H32N6O29S8
- Molecular Weight:1329.24
IUPAC Name: 4,4',4'',4'''-((5,5'-(carbonylbis(azanediyl))bis(isophthaloyl))tetrakis(azanediyl))tetrakis(benzene-1,3-disulfonic acid)
InChIKey: FXAIVMYRMNONEG-UHFFFAOYSA-N
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
Biological Activity: 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[1][2].
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NF449 | 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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References
- [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]
