P2X Receptor Modulators

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A9736 A-438079 hydrochloride hydrate ≥98% (HPLC) A-438079 hydrochloride hydrate is a selective P2X7 purinoceptor antagonist in both human and rat with minimal activity at 75 different G-protein-coupled receptors, enzymes, transporters, and ion channels tested.
A2979 A-317491 sodium salt hydrate ≥98% (HPLC), powder A-317491 helps to decrease neuropathic and inflammatory pain by inhibiting the P2X3 receptor-mediated Ca2+ influx.
Novel P2X3 and P2X2/3 receptor antagonist
A7231 AZ11645373 ≥98% (HPLC), solid AZ11645373 is a selective and potent human P2X7 purinoceptor antagonist. KB values range from 5-20 nM for human P2X7 receptor inhibition. It is 500-fold less effective ats an inhibitor of rat P2X7 receptor responses.
B3756 8-Bromoadenosine 5′-triphosphate sodium salt ≥90% (HPLC) P2X purinoceptor agonist similar in reactivity to ATP.
SML1701 BX430 ≥98% (HPLC) BX430 is a selective noncompetitive allosteric antagonist of human P2X4 receptor channels. P2X4 receptors are highly expressed in the CNS, and have been studied as a therapeutic target for neuropathic pain and inflammation, and treatment of traumatic brain injury, cerebral ischemia, and spinal cord injury. BX430 is highly selective for human P2X4, with minimal activity towards other P2X subtypes, including P2X1–P2X3, P2X5, and P2X7. BX430 is also an antagonist of zebrafish P2X4 but has no effect on rat and mouse P2X4 receptors. BX430 has an IC50 value of 540 nM.
C1506 Cytidine 5′-triphosphate disodium salt ≥95% Cytidine 5′-triphosphate (CTP) prevents the action of aspartate carbamoyltransferase. This enzyme participates in pyrimidine biosynthesis. Like adenosine triphosphate (ATP), CTP serves as a molecule of high energy. It acts as a coenzyme in glycerophospholipid biosynthesis and protein glycosylation.
P2X4 purinergic receptor agonist.
SML1708 JNJ-47965567 ≥98% (HPLC) JNJ-47965567 is a potent P2X7 antagonist with high affinity for the rat receptor (pKi = 8.7). It is centrally available after systemic injection with a superior brain:plasma distribution compared to other available P2X7 antagonists. JNJ-47965567 was shown to suppress epileptic seizures in a mouse model of epilepsy. It appears to have a disease modifying effect since spontaneous seizure rates did not increase once treatment with JNJ-477965567 was stopped.
M6517 α,β-Methyleneadenosine 5′-triphosphate lithium salt ≥93% (HPLC), solid P2 purinoceptor agonist that is more potent than ATP at the P2X subtype.
M7510 β,γ-Methyleneadenosine 5′-triphosphate disodium salt ≥95%, solid Selective P2X purinoceptor agonist that is more potent than ATP, but less potent than α, β-methylene-L-adenosine 5′-triphosphate.
M7684 MRS 2159 >98% (HPLC), solid P2X1 purinoceptor antagonist.
N8652 NF 023 hydrate ≥98% (HPLC), solid NF 023 is a potent, selective P2X1 purinoceptor antagonist.
SML0753 PSB-12062 ≥98% (HPLC) PSB-12062 is a P2X4 receptor antagonist. P2X4 receptors are highly expressed in the CNS, and have been studied as a therapeutic target for neutopathic pain, and treatment of traumatic brain injury, cerebral ischemia, and spinal cord injury. PBS-12062 is a new P2X4-specific antagonist with equal potency against human, rat and mouse receptors (IC50s 1.38, 0.92 and 1.76 μM, respecitively). The compound does not display significant inhibition of human P2X1, P2X2, P2X3 or P2X7 at 10 μM.
P178 Pyridoxal phosphate-6-azo(benzene-2,4-disulfonic acid) tetrasodium salt hydrate solid, ≥98% (HPLC) Non-selective P2 purinoceptor antagonist which blocks responses at both pre- and post-junctional sites.