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Adenosines/P2 Nucleotide Receptor - Antagonists

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A2979 A-317491 sodium salt hydrate ≥98% (HPLC), powder Novel P2X3 and P2X2/3 receptor antagonist
 
C199 CGS-15943 solid Highly potent, non-selective adenosine receptor antagonist.
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora2b(29316)
C197 8-(3-Chlorostyryl)caffeine ≥98% (HPLC), solid Selective A2A adenosine receptor antagonist.
human ... ADORA2A(135)
mouse ... Maob(109731)
rat ... Adora1(29290), Adora2a(25369)
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.
 
PZ0124 CP-66713 ≥98% (HPLC) CP-66713 is an adenosine A2 receptor antagonist.
 
C102 8-Cyclopentyl-1,3-dimethylxanthine ≥98% (HPLC), powder Selective A1 adenosine receptor antagonist.
human ... ADORA1(134)
C101 8-Cyclopentyl-1,3-dipropylxanthine solid Selective A1 adenosine receptor antagonist.
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora2b(29316), Adora3(25370)
P2278 1,3-Dimethyl-8-phenylxanthine crystalline Selective A1 adenosine receptor antagonist.
human ... ADORA1(134), ADORA2B(136), ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora2b(29316)
D134 3,7-Dimethyl-1-propargylxanthine ≥98% (HPLC), powder Selective A2 adenosine receptor antagonist.
human ... ADORA2A(135), ADORA2B(136)
rat ... Adora1(29290), Adora2a(25369)
A022 1,3-Dipropyl-8-(p-sulfophenyl)xanthine powder Water soluble adenosine receptor antagonist with slight selectivity for A1 receptors.
human ... ADORA1(134), ADORA2B(136), ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora3(25370)
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.
human ... ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora3(25370)
M1809 MRS 1523 >98% (HPLC) Selective A3 adenosine receptor antagonist in the rat.
human ... ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora3(25370)
M6316 MRS 1754 hydrate ≥98% (HPLC), solid MRS 1754 hydrate is a potent A2B adenosine receptor antagonist.
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora2b(29316)
M7684 MRS 2159 >98% (HPLC), solid P2X1 purinoceptor antagonist.
human ... P2RX1(5023)
M3808 MRS 2179 ammonium salt hydrate ≥98% (HPLC) Competitive P2Y1 purinoceptor antagonist.
human ... P2RY1(5028)
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.
human ... P2RX1(5023), P2RY1(5028), P2RY11(5032), P2RY2(5029)
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)
 
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.
human ... LPAR4(2846), LTB4R(1241), P2RX1(5023), P2RY1(5028), P2RY10(27334), P2RY11(5032), P2RY12(64805), P2RY13(53829), P2RY14(9934), P2RY2(5029), P2RY4(5030), P2RY5(10161), P2RY6(5031), P2RY8(286530)
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.
 
A013 8-(p-Sulfophenyl)theophylline hydrate solid Polar adenosine receptor antagonist, which penetrates cells to a limited extent and is relatively soluble in water.
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140)
rat ... Adora1(29290), Adora2a(25369)
V5888 VUF 5574 Potent, selective, and competitive A3 adenosine receptor antagonist.
human ... ADORA3(140)
X103 Xanthine amine congener ≥96% (HPLC) Xanthine amine congener is a potent, nonselective adenosine receptor antagonist (A1 and A2B > A2A).
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora2b(29316), Adora3(25370)
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.