NF279 

NF279 is a selective P2X1 receptor antagonist and NTPDase inhibitor, with a P2X1 IC₅₀ value of 19 nM. NF279 suppresses GABA-evoked currents, reduces ATP-excited respiratory activity, alters hypoglossal nerve burst parameters, and blocks CXCR4, CCR5, CXCR3, and CXCR7-mediated calcium responses. NF279 arrests HIV-1 fusion downstream of CD4 binding, inhibits R5- and X4-tropic HIV-1 strains. NF279 can be used for the research of HIV-1 infection^{[1][2][3][4][5][6]}.

NF279 (1-100 μM; 10 min) potently inhibits human NTPDase1, NTPDase2, NTPDase3, and NTPDase8, with the highest potency against human NTPDase3 (IC₅₀ 0.6 μM) and the lowest potency against human NTPDase8 ATPase activity (IC₅₀ 36 μM)^[2].
NF279 (1-100 μM; 10 min) potently inhibits mouse NTPDase1, NTPDase2, NTPDase3, and NTPDase8, with the highest potency against mouse NTPDase2 (IC₅₀ 3.3 μM) and the lowest potency against mouse NTPDase1 ATPase activity (IC₅₀ 52 μM)^[2].
NF279 (20 µM) reduces GABA-activated currents in isolated primary rat hippocampal pyramidal neurons to a mean of 61.8% of control, with a reversible inhibitory effect^[3].
NF279 (3-300 nM; 10 s pre-incubation; 1-30 µM; simultaneous co-application) potently and reversibly inhibits rat P2X1 receptors expressed in Xenopus laevis oocytes, with an IC₅₀ of 19 nM following 10 s pre-incubation, and shows reduced potency (IC₅₀ 2.02 µM) when co-applied with ATP^[4].
NF279 (0.3-10 µM; 10 s pre-incubation; 10-300 µM; simultaneous co-application) reversibly inhibits rat P2X3 receptors expressed in Xenopus laevis oocytes, with an IC₅₀ of 1.62 µM following 10 s pre-incubation, and shows greatly reduced potency (IC₅₀ 85.5 µM) when co-applied with ATP^[4].
NF279 (1-10 µM; simultaneous co-application; post-activation application) acts as a reversible, competitive antagonist of rat P2X2 receptors expressed in Xenopus laevis oocytes, with an IC₅₀ of 0.76 µM and a K_B value of 0.36 µM derived from Schild analysis^[4].
NF279 shows very low potency against human P2X4 receptors expressed in Xenopus laevis oocytes, with less than 50% inhibition at 300 µM and an IC₅₀ greater than 300 µM^[4].
NF279 (10-50 μM; 90 min) dose-dependently inhibits X4-tropic, R5-tropic, and dual-tropic HIV-1 fusion with TZM-bl cells without affecting cell viability or VSV-G-mediated fusion, with greater potency against HXB2 Env-mediated fusion^[5].
NF279 (30 μM; 90 min) dose-dependently inhibits X4-tropic HIV-1 fusion with CEM-A cells without affecting cell viability, with lower potency than observed in TZM-bl cells^[5].
NF279 (30 μM; 90 min) potently inhibits X4-tropic and R5-tropic HIV-1 fusion with TZM-bl cells^[5].
NF279 (30 μM; 10 min preincubation) acts as a dual CXCR4/CCR5 antagonist by completely blocking chemokine-mediated calcium signaling in TZM-bl cells^[5].
NF279 (30 μM; 10 min preincubation) blocks gp120-mediated CXCR4 activation by inhibiting calcium signaling in TZM-bl cells^[5].
NF279 (30 μM; 10 min preincubation) acts as a partial CXCR4 antagonist and blocks CXCR3/CXCR7 signaling by inhibiting chemokine-mediated calcium flux in CEM-A cells^[5].
NF279 (0-50 μM; 90 min) inhibits R5-tropic HIV-1 fusion with both wild-type CCR5-expressing TZM-bl cells and CCR5^G163R mutant-expressing JGR.H11 cells, with greater potency against the mutant coreceptor (IC₅₀ = 4.5 μM for JGR.H11 cells, 13.3 μM for TZM-bl cells)^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1401.12

C₄₉H₃₀N₆Na₆O₂₃S₆

202983-32-2

Solid

White to off-white

O=C(NC1=CC=C(C=C1)C(NC2=CC=C(C=C2)C(NC3=CC=C(S(=O)(O[Na])=O)C4=CC(S(=O)(O[Na])=O)=CC(S(=O)(O[Na])=O)=C34)=O)=O)NC5=CC=C(C=C5)C(NC6=CC=C(C=C6)C(NC7=CC=C(S(=O)(O[Na])=O)C8=CC(S(=O)(O[Na])=O)=CC(S(=O)(O[Na])=O)=C78)=O)=O

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [1]. Ning S, et al. The effect of ATP and P2X receptor on respiration in the neunatal rat transverse medullary slice. IEEE Xplore. 2008 Jun 03;1054-1057.

  [2]. Munkonda MN, et al. Inhibition of human and mouse plasma membrane bound NTPDases by P2 receptor antagonists. Biochem Pharmacol. 2007;74(10):1524-1534.  [Content Brief]

  [3]. Storozhuk MV, et al. Several P2X receptor antagonists, including NF279 and PPADS suppress GABA responses in isolated hippocampal neurons. Pharmacologyonline. 2015 Jan;1:72-76.

  [4]. Rettinger J, et al. The suramin analogue NF279 is a novel and potent antagonist selective for the P2X(1) receptor. Neuropharmacology. 2000;39(11):2044-2053.  [Content Brief]

  [5]. Giroud C, et al. P2X1 Receptor Antagonists Inhibit HIV-1 Fusion by Blocking Virus-Coreceptor Interactions. J Virol. 2015;89(18):9368-9382.  [Content Brief]

  [6]. Klapperstück M, et al. Antagonism by the suramin analogue NF279 on human P2X(1) and P2X(7) receptors. Eur J Pharmacol. 2000;387(3):245-252.  [Content Brief]