| Bioactivity | NF023 hexasodium is a selective and competitive P2X1 receptor antagonist, with IC50 values of 0.21 μM, 28.9 μM, > 50 μM and > 100 μM for human P2X1, P2X3, P2X2, and P2X4-mediated responses respectively[1][2][3][4]. |
| Invitro | NF023 is selective for recombinant Gi alpha-1 and recombinant Go alpha (EC50 value of approximately 300 nM)[2].NF023 inhibits P2X1 receptors in a voltage-insensitive manner. NF023 (5 and 30 μM) causes a shift of the concentration-response curve to the right without affecting the maximal response to ATP (KB=1.190.2 μM)[4]. |
| In Vivo | NF023 (100 µmol/kg i.v.) antagonizes vasopressor responses to α,β-mATP but not to noradrenaline In pithed rats[3]. |
| Name | NF023 hexasodium |
| CAS | 104869-31-0 |
| Formula | C35H20N4Na6O21S6 |
| Molar Mass | 1162.88 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. F Soto, et al. Antagonistic Properties of the Suramin Analogue NF023 at Heterologously Expressed P2X Receptors. Neuropharmacology. 1999 Jan;38(1):141-9. [2]. M Freissmuth, et al. Suramin Analogues as Subtype-Selective G Protein Inhibitors. Mol Pharmacol. 1996 Apr;49(4):602-11. [3]. G Lambrecht, et al. Agonists and Antagonists Acting at P2X Receptors: Selectivity Profiles and Functional Implications. Naunyn Schmiedebergs Arch Pharmacol. 2000 Nov;362(4-5):340-50. [4]. M Silva-Ramos, et al. Activation of Prejunctional P2x2/3 Heterotrimers by ATP Enhances the Cholinergic Tone in Obstructed Human Urinary Bladders. J Pharmacol Exp Ther. 2020 Jan;372(1):63-72. |
NF023 hexasodium
CAS: 104869-31-0 F: C35H20N4Na6O21S6 W: 1162.88
NF023 hexasodium is a selective and competitive P2X1 receptor antagonist, with IC50 values of 0.21 μM, 28.9 μM, > 50
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