P2X Receptor Antagonist

Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC₅₀ of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough.

Tricarbonyldichlororuthenium(II) dimer (CORM-2) is a CO-releasing molecule. Tricarbonyldichlororuthenium(II) dimer exhibits anti-inflammatory, antioxidant, and gastric mucosa-protective activities. Additionally, Tricarbonyldichlororuthenium(II) dimer has CO-independent functional effects on multiple potassium channels.

Sivopixant (S-600918) is a potent and selective P2X3 receptor antagonist (P2X3 IC₅₀=4.2 nM; P2X2/3 IC₅₀=1100 nM). Sivopixant shows strong analgesic effect.

Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an orally active antispastic agent with a vasodilator effect, used for the research of muscle stiffness and pain. Eperisone Hydrochloride is a potent and selectively P2X7 receptor antagonist, also shows antagonism for human P2X3. Eperisone Hydrochloride works by relaxing both skeletal muscles and vascularsmooth muscles, demonstrating a variety of effects such as reduction ofmyotonia, improvement of circulationand and suppression of the pain reflex.

PSB-10211 is a P2X2 receptor antagonist with an IC₅₀ of 0.086 μM against rat P2X2 receptors. PSB-10211 inhibits ATP-mediated currents of rat P2X2 receptors expressed in Xenopus oocytes. PSB-10211 can be used in studies related to pain and urinary incontinence.

P2X7 receptor antagonist-2 is a potent P2X7 receptor antagonist with a pIC₅₀ value of 6.5-7.5. P2X7 receptor antagonist-2 has efficacy of combating neuroinflammation.

Minodronic acid (YM-529) hydrate is an FPP synthase inhibitor with an IC₅₀ of 3 nM, and also an antagonist of P2X2/3 receptors with an IC₅₀ of 62.7 μM. Minodronic acid hydrate induces tumor cell apoptosis and inhibits cell growth. Minodronic acid hydrate also suppresses bone resorption. Minodronic acid hydrate can be used in research related to osteoporosis and cancer.

Eperisone (hydrochloride) (Standard) is the analytical standard of Eperisone (hydrochloride). This product is intended for research and analytical applications. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an orally active antispastic agent with a vasodilator effect, used for the research of muscle stiffness and pain. Eperisone Hydrochloride is a potent and selectively P2X7 receptor antagonist, also shows antagonism for human P2X3. Eperisone Hydrochloride works by relaxing both skeletal muscles and vascularsmooth muscles, demonstrating a variety of effects such as reduction ofmyotonia, improvement of circulationand and suppression of the pain reflex.

(Rac)-EVT-401 (HY-145466) is the racemate of EVT-401 (HY-178230). (Rac)-EVT-401 is a P2X7 receptor antagonist that can be used in research related to rheumatoid arthritis.

JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pK_i values of 9.1 and 7.9 for rat and human P2X7 channels, respectively.

AZ11645373 is a highly selective and potent antagonist at human but not rat P2X7 receptors，AZ11645373 inhibits ATP-evoked IL-1β release from lipopolysaccharide-activated THP-1 cells , with an IC₅₀ value of 90 nM.

(E/Z)-Sivopixant ((E/Z)-S-600918) is a potent P2X3 receptor antagonist with an IC₅₀ of 4 nM. (E/Z)-Sivopixant can be used for respiratory diseases research.

Ro 0437626 is a selective purinergic (P2X₁) receptor antagonist (IC₅₀ = 3 μM), but shows low affinity for P2X2, P2X3 and P2X2/3 receptors (IC₅₀ > 100 μM).

NF110 is a P2X₃ receptor antagonist (K_i = 36 nM) and inactive toward P2Y receptors stably expressed (IC₅₀s > 10 M). NF110 blocks alphabeta-methylene-ATP-induced currents (IC₅₀ = 527 nM) in rat dorsal root ganglia neurons.

AF-353 hydrochloride is a potent, selective and orally bioavailable P2X3/P2X2/3 receptor antagonist, with a pIC₅₀ of 8.0 for both human and rat P2X3, and with a pIC₅₀ of 7.3 for human P2X2/3.

MRS4596 is a potent and selective P2X4 receptor antagonist with an IC₅₀ value of 1.38 μM for human P2X4 receptor. MRS4596 has neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4596 can be used in research of ischemic stroke .

Iso-PPADS tetrasodium is a P2X-purinoceptor antagonist. Iso-PPADS tetrasodium inhibits P2X1 and P2X3 receptor with IC₅₀s of 43 nM and 84 nM. Iso-PPADS tetrasodium is protective against ventilator-induced brain injury (VIBI).

P2X3 antagonist 39 (compound 26a) is a selective P2X3 receptor antagonist with an IC₅₀ value of 54.9 nM. P2X3 antagonist 39 can be used in the study of neuropathic pain model.

JNJ-54166060 is a potent and selective P2X7 receptor antagonist, with IC₅₀s of 4/115/72 nM for human/rat/mouse P2X7 receptor, respectively.

MRS4719 is a potent P2X4 receptor antagonist with an IC₅₀ value of 0.503 μM for human P2X4 receptor. MRS4719 can reduce infarct volume and reduce brain atrophy, showing neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4719 also reduces ATP-induced [Ca²⁺]_i influx in primary human monocyte-derived macrophages. MRS4719 can be used to research ischemic stroke.