High affinity P2X3
receptor antagonist (Ki
values are 36, 82 and 4144 nM for P2X3
recombinant receptors respectively). Shows no activity at P2Y1
> 10 μ
M). Potently inhibits α
-meATP-evoked desensitizing currents in rat DRG neurons (IC50
= 527 nM). Shows antitumor activity against several tumor types.
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All Tocris products are intended for laboratory research use only.
Antitumour activity of suramin analogues in human tumour cell lines and primary cultures of tumour cells from patients.
Dhar et al.
Structure-activity relationships of analogues of NF449 confirm NF449 as the most potent and selective known P2X1 receptor antagonist.
Kassack et al.
The suramin analog 4,4',4'',4'''-(Carbonylbis(imino-5,1,3-benzenetriylbis (carbonylimino)))tetra-kis-benzenesulfonic acid (NF110) potently blocks P2X3 receptors: subtype selectivity is determined by location of sulfonic
Hausmann et al.