10 nM – 1 µM.

A-740003 is a potent and selective competitive antagonist of P2X7 receptors with IC₅₀ values of 18 nM, 44 nM and 0.68 µM for rat, human and mouse receptors, respectively. A-740003 reduces neuropathic pain and tumor growth in vivo^1,2.

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).

-20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.

1-100 nM.

A-804598 is a potent and selective, competitive and high-affinity antagonist of the purinergic P2X7 receptor, with IC₅₀ values of around 10 nM for mouse, rat, and human receptors^1-3.

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).

Store at -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.

1-50 nM.

A-839977 is a potent and selective antagonist of P2X7 receptors, shown to inhibit BzATP-induced Ca²⁺ responses at human, rat and mouse P2X7 receptors with IC₅₀ values of 20 nM, 42 nM and 150 nM, respectively. A-839977 produces significant anti-nociception and anti-hyperalgesia (ED₅₀ = 40-100μmol/kg) in animal models of inflammatory pain¹.

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).

-20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.

1-100 nM.

AACBA hydrochloride is a potent and selective antagonist of P2X7 receptors, shown to inhibit human and rat P2X7 receptors with IC₅₀ values of 18 nM and 29 nM, respectively. Active in vivo on acute models of pain and inflammation¹.

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Soluble up to 200 mM in water. Centrifuge all products before handling (10000 x g 5 min).

Store at -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.

1-100 nM.

AZ 10606120 dihydrochloride is a potent and selective non-competitive antagonist of P2X7 receptors, acting as a negative allosteric modulator shown to inhibit human P2X7 receptors with pIC₅₀ of 8.1-8.9^1-3. It also inhibits growth and neoangiogenesis of P2X7-expressing tumors in mice⁴.

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Soluble up to 100 mM in DMSO and up to 20 mM in water. Centrifuge all products before handling (10000 x g 5 min).

Store at -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.

0.1-5 µM.

AZ11645373 is a potent and selective antagonist of human P2X7 purinergic receptors (K_B = 5-20 nM), significantly less active on rat receptors, and inactive on other P2X receptor subtypes¹.

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at +4°C.

Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).

-20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.

1-100 nM.

AZD-9056 is a potent and selective, orally bioavailable antagonist of the purinergic P2X7 receptor, shown to inhibit YoPro1 uptake in HEK–hP2X7 cells with IC₅₀ of 11.2 nM¹. AZD-9056 shows pain-relieving and anti-inflammatory effects in vivo².

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).

-20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.

1-10 µM.

CAY10593 (VU0155069) is an antagonist of purinergic P2X7 receptors, shown to inhibit ATP-induced ethidium⁺ uptake in RPMI 8226 cells with IC₅₀ of 2 µM¹. It is also a potent and selective inhibitor of phospholipase D1 (IC₅₀ of 46 and 933 nM for PLD1 and PLD2, respectively)².

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).

-20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.

0.1-10 µM.

GW 791343 hydrochloride is a species-specific allosteric modulator of the purinergic P2X7 receptors, acting as a negative modulator of human P2X7 (pIC₅₀ = 6.9 - 7.2), and as a positive modulator of rat P2X7^1,2.

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Soluble up to 100 mM in DMSO and in water. Centrifuge all products before handling (10000 x g 5 min).

-20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.

20 nM – 1 µM.

JNJ-47965567 is a potent and highly selective antagonist of purinergic P2X7 receptors, shown to inhibit BzATP-induced Ca²⁺ responses at human, rat and mouse P2X7 receptors with pIC₅₀ values of 8.3, 7.2 and 7.5, respectively. JNJ-47965567 is centrally permeable and active in vivo¹.

Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).

-20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.

10 nM – 1 µM.

JNJ-54166060 is a novel, potent and selective antagonist of purinergic P2X7 receptors, with IC₅₀ of 4 nM on human receptors. Orally bioavailable, with an ED₅₀ of 2.3 mg/kg and a brain/plasma ratio of close to 3 in rats¹.

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).

-20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.

20 nM – 20 µM.

KN-62 is a potent non-competitive antagonist of the purinergic P2X7 receptors, shown to inhibit Bz-ATP-induced currents in HEK–hP2X7 cells with IC₅₀ of 25 nM. KN-62 is also a selective, cell permeable inhibitor of Ca2+/calmodulin-dependent kinase type II, with IC50 of approximately 1 µM¹.

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).

-20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.

5-50 µM.

ZINC58368839 is a novel antagonist of purinergic P2X7 receptors, shown to inhibit BzATP-induced Ca²⁺ responses in HEK–hP2X7 cells with IC₅₀ of 4.8 µM¹.

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).

-20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.