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Antagonists

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SML0004 (S)-(+)-Clopidogrel hydrogensulfate ≥98% (HPLC) (S)-(+)-Clopidogrel hydrogen sulfate is an antithrombotic antiplatelet agent. It specifically and irreversibly inhibits the Purinoceptor P2Y12 subtype which inhibits ADP-induced platelet aggregation. (S)-(+)-Clopidogrel hydrogen sulfate is the active isomer.
T4146 1,3,9-Trimethylxanthine ≥98% (HPLC), solid 1,3,9-Trimethylxanthine is an adenosine receptor antagonist.
P2278 1,3-Dimethyl-8-phenylxanthine crystalline Selective A1 adenosine receptor antagonist.
A022 1,3-Dipropyl-8-(p-sulfophenyl)xanthine powder Water soluble adenosine receptor antagonist with slight selectivity for A1 receptors.
D134 3,7-Dimethyl-1-propargylxanthine ≥98% (HPLC), powder Selective A2 adenosine receptor antagonist.
SML0450 5-BDBD ≥98% (HPLC) 5-BDBD is a specific inhibitor of P2X4. The compound inhibits P2X4 currents in CHO cells with an IC50 of 500 nM.
C197 8-(3-Chlorostyryl)caffeine ≥98% (HPLC), solid Selective A2A adenosine receptor antagonist.
A013 8-(p-Sulfophenyl)theophylline hydrate solid Polar adenosine receptor antagonist, which penetrates cells to a limited extent and is relatively soluble in water.
C102 8-Cyclopentyl-1,3-dimethylxanthine ≥98% (HPLC), powder Selective A1 adenosine receptor antagonist.
C101 8-Cyclopentyl-1,3-dipropylxanthine solid Selective A1 adenosine receptor antagonist.
A2979 A-317491 sodium salt hydrate ≥98% (HPLC), powder Novel P2X3 and P2X2/3 receptor antagonist
SML0617   A-804598 ≥98% (HPLC) A-804598 is a P2X7 selective, competitive antagonist. In competition assays, the IC50s for human, rat and mouse channels are 11, 10 and 9 nM, respectively.
SML0728   ANR-94 ≥98% (HPLC) ANR-94 is a potent antagonist of the adenosine A2A receptor (AA2AR). The Ki for human AA2AR is 46 nM. ANR-94 displays neuroprotective properties in rat models of Parkinson′s disease. ANR-94 reverses GABA-A receptor desensitization in oocyte and neuronal electrophysiological preparations.
BM0020 BMS-646786 ≥98% (HPLC) BMS-646786 is a potent and specific inhibitor of P2Y1 purinergic receptor that inhibits ADP-mediated platelet aggregation in human blood samples. BMS-646786 significantly reduces thrombus weight in a rat arterial thrombosis model with a limited effect on bleeding.
BM0027   BMS-870145 ≥98% (HPLC) BMS-870145 is an orally available, potent and selective P2Y1 purinergic receptor antagonist. BMS-870145 demonstrated similar antithrombotic efficacy with less bleeding compared with P2Y12 antagonist prasugrel in rabbits.
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.
B5311 Biperiden hydrochloride ≥98% (HPLC), powder Biperiden hydrochloride is antiparkinsonian; non-selective muscarinic receptor antagonist. It is used for the adjunctive treatment of all forms of Parkinson′s Disease (postencephalitic, idiopathic, and arteriosclerotic); also commonly used to improve parkinsonian signs and symptoms related to antipsychotic drug therapy. LD50 in rats 750 mg/kg; in dogs 340 mg/kg.
C199 CGS-15943 solid Highly potent, non-selective adenosine receptor antagonist.
PZ0124 CP-66713 ≥98% (HPLC) CP-66713 is an adenosine A2 receptor antagonist.
SML1902 ISAM-140 ≥98% (HPLC) New ISAM-140 is a potent and selective A2B adenosine receptor antagonist (A2BAR). ISAM-140 exhibits remarkable selectivity over A1, A2A, and A3 adenosine receptors.
SML0422 Istradefylline ≥98% (HPLC) Istradefylline (KW-6002) is a potent and selective adenosine A2A receptor selective antagonist which has been investigated for use in Parkinson′s Disease.
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.
SML1722 LUF5834 ≥98% (HPLC) LUF5834 is a potent A2A and A2B adenosine receptor partial agonist with an EC50 value of 12 nM and 45-fold selectivity over the adenosine A3 receptor.
M227 MRS 1191 solid MRS 1191 is putative A3 adenosine receptor antagonist, highly selective for human A3 receptor vs human A1 receptor. MRS 1067, MRS 1191 and MRS 1220 were found to be competitive in saturation binding studies using the agonist radioligand [125I]AB-MECA at cloned human brain A3 receptors expressed in HEK-293 cells. Antagonism was demonstrated in functional assays consisting of agonist-induced inhibition of adenylate cyclase and the stimulation of binding of [35S]guanosine 5′-O-(3-thiotriphosphate) ([35S]GTP-gamma-S) to the associated G-proteins. Activation of the human A3 receptor in A3R-CHO results in markedly impaired cell cycle progression, suggesting an important role for this adenosine receptor subtype in cell cycle regulation and cell growth. Activation of adenosine A3 receptors by Cl-IBMECA (100 nM) increased the magnitude of theta-burst induced LTP (from 1.2+/-0.6% in the control solution to 25.5+/-0.8% in the presence of Cl-IBMECA) and attenuated LTD (from 30.0+/-5.5% decrease in the control solution to 13.6+/-6.6% decrease in the presence of Cl-IBMECA). The selective adenosine A3 receptor antagonist, MRS 1191 (5-10 μM), prevented the effects of Cl-IBMECA. These findings indicate a functional role for adenosine A3 receptors in the modulation of synaptic plasticity.
M228 MRS 1220 solid MRS1220 is a putative A3 adenosine receptor antagonist. MRS 1220 was found to be competitive in saturation binding studies using the agonist radioligand 125I AB-MECA at cloned human brain A3 receptors expressed in HEK-293 cells. Antagonism was demonstrated in functional assays consisting of agonist-induced inhibition of adenylate cyclase and the stimulation of binding of 35S guanosine 5′-O-(3-thiotriphosphate (35S GTP-gamma-S) to the associated G-proteins. MRS 1220 and MRS 1191, with KB values of 1.7 and 92 nM, respectively, proved to be highly selective for human A3 receptor vs human A1 receptor-mediated effects on adenylate cyclase. In addition, MRS 1220 reversed the effect of A3 agonist-elicited inhibition of tumor necrosis factor-alpha formation in the human macrophage U-937 cell line, with an IC50 value of 0.3 μM.
M1809 MRS 1523 >98% (HPLC) Selective A3 adenosine receptor antagonist in the rat.
M6316 MRS 1754 hydrate ≥98% (HPLC), solid MRS 1754 hydrate is a potent A2B adenosine receptor antagonist.
M7684 MRS 2159 >98% (HPLC), solid P2X1 purinoceptor antagonist.
M3808 MRS 2179 ammonium salt hydrate ≥98% (HPLC) Competitive P2Y1 purinoceptor antagonist.
M5942 MRS 2395 ≥98% (HPLC), solid Antagonist for P2Y12 purinoceptor; inhibits ADP-induced aggregation in rat platelets and antagonizes ADP-induced inhibition of cAMP in rat and human platelets in the presence of PGE1 without affecting P2Y1 receptor-induced PLC activity in transfected astrocytoma cells.
M3568 MSX-3 hydrate ≥98% (HPLC), solid Selective A2A adenosine receptor antagonist prodrug.
N8652 NF 023 hydrate ≥98% (HPLC), solid NF 023 is a potent, selective P2X1 purinoceptor antagonist.
P0373 PSB 1115 potassium salt hydrate ≥95% (HPLC) PSB 1115 is a highly selective, water-soluble, human A2B adenosine receptor antagonist.
SML0212 PSB36 ≥98% (HPLC) Inhibition of A1 adenosine receptor by PSB36 modulates the spinal antinociception in animal models.
PSB36 is a very potent, selective antagonist of the adenosine A1 receptor. The compound selectivity (Ki) for human A1, A2A, A2B and A3 receptors is 0.7, 980, 187 and 2300 respectively. PSB36 is considerably more potent that DPCPX (EC50 0.012 nM vs 2.9 nM)
SML0331 Prasugrel ≥98% (HPLC) Prasugrel is a platelet inhibitor that reduces the aggregation of platelets by irreversible binding to P2Y12 receptors. Prasugrel interacts in an irreversible manner with the residues Cys97 and Cys175 of the human P2Y12-receptor.
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.
R3904 Reversine ≥98% (HPLC), solid Reversine was first described as a synthetic substituted purine with activity as a dedifferentiation agent; it was shown to induces differentiated lineage-committed cells to become multipotent mesenchymal stem cells (MSCs). Reversine has also been show to have activity as a potent, selective human A3 adenosine receptor antagonist (Ki value of 0.66 μM), as an ATP-competitive Aurora kinase inhibitor, and as a Mps1 kinase inhibitor. Additionally, studies have shown reversine to be an anti-cancer agent, inhibiting growth and inducing cell death in various cancer cell types.
S4568 SCH 58261 ≥98% (HPLC), solid A2A adenosine receptor antagonist.
SCH 58261 reduces the levels of TNF-α, Fas-L, Bax expression and activation of JNK-MAPK pathway. It has neuroprotective effects as it reduces demyelination of the neurons. SCH 58261 increases the concentration of secretion of dopamine and elicits locomotor sensitization, an attractive option in the possible treatment of Parkinson′s disease.
V5888 VUF 5574 Potent, selective, and competitive A3 adenosine receptor antagonist.
X103 Xanthine amine congener ≥96% (HPLC) Xanthine amine congener is a potent, nonselective adenosine receptor antagonist (A1 and A2B > A2A).
Z0153 ZM 241385 ≥98% (HPLC) ZM 241385 is a potent selective adenosine A2A antagonist. The A2A receptor plays a role in regulating myocardial oxygen consumption and coronary blood flow and is highly expressed in the brain, where it has important roles in the regulation of glutamate and dopamine release. ZM 241385 has neuroprotective effects and is being investigated for use in Parkinson′s and other neurodegenerative disorders.