Adenosine A2A receptor (A2AR) Antagonist
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Derenofylline
0 ImagesSynonyms: SLV 320Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats.
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PSB36
0 ImagesPSB36 is a highly selective A1 adenosine receptor antagonist, with a Ki of 0.12 nM and a Kd of 0.7 nM. Systemic administration of PSB36 reduces formalin- and Carrageenan (HY-125474)-induced edema in mice and decreases pain-related behaviors, with no local paw activity. PSB36 prolongs the APD90 of rat and human atria, produces a frequency-dependent prolongation of rat atrial ERP, increases the diastolic threshold of rat atria, and shortens the duration of atrial fibrillation episodes. PSB36 can be used in research related to inflammatory pain, inflammatory hyperalgesia, edema and atrial fibrillation.
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INCB106385
0 ImagesCat. No.: HY-184213CAS No.: 2408260-34-2INCB106385 is an orally active A2A/A2B adenosine receptor antagonist, with an IC50 value of 4.4 nM for cAMP inhibition at the A2A adenosine receptor and an IC50 value of 6.4 nM for cAMP inhibition at the A2B adenosine receptor. INCB106385 inhibits the pCREB signaling pathway in immune cells, blocks adenosine-mediated immunosuppression in the tumor microenvironment, and induces tumor regression. INCB106385 exhibits efficacy as a monotherapy or in combination with anti-PD-1 antibodies in colon cancer models. INCB106385 can be used for the research of colon cancer.
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(E)-8-(3-Chlorostyryl)caffeine
0 ImagesSynonyms: (E)-CSC(E)-8-(3-Chlorostyryl)caffeine is a selective adenosine A2A receptor antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM by a pathway that is independent of its actions on the A2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research.
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ANR94
0 ImagesANR94 is a potent and selective adenosine A2A receptor (AA2AR) antagonist with an Ki of 46 nM for hAA2AR. ANR94 has the potential for the research of Parkinson's disease.
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M1069
0 ImagesM1069 is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity.
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MRS1334
0 ImagesMRS1334 is a potent and selective human adenosine A3 receptor antagonist with Kis of 2.69 nM, >100 nM, >100 nM for hA3, rA1, rA2A, respectively. MRS1334 blocks the protective effect of Cl-IB-MECA leading to significant bradycardia and elevated ST segment. MRS1334 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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A1AR antagonist 6
0 ImagesA1AR antagonist 6 (compound 15) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 6.38 and a pKi of 7.13.
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Adenosine receptor antagonist 2
0 ImagesAdenosine receptor antagonist 2 is an orally active A2a/A2b adenosine receptor antagonist with IC50s of 1 nM and 3 nM, respectively. Adenosine receptor antagonist 2 has anti-tumor activity.
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DMPX
0 ImagesSynonyms: 3,7-Dimethyl-1-propargylxanthineDMPX (3,7-Dimethyl-1-propargylxanthine) is a selective A2A adenosine receptor (A2A AR) antagonist that crosses the blood-brain barrier, with a Ki of 11 μM for rat A2 adenosine receptor and a Ki of 45 μM for rat A1 adenosine receptor. By blocking A2A receptors in specific brain regions, DMPX protects dopaminergic and GABAergic neurons from mitochondrial dysfunction. DMPX is applicable to research related to depression, Parkinson's disease and Huntington's disease.
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A2AAR antagonist 2
0 ImagesCat. No.: HY-N12422Purity: 99.40%3′-Methoxyfurano[4″,5″:3,4]chalcone (compound 2) is a selective A2AAR antagonist (IC50=33.5 nM) with high affinity. 3′-Methoxyfurano[4″,5″:3,4]chalcone is also a natural product obtained from the bark of Allium cepa L. 3′-Methoxyfurano[4″,5″:3,4]chalcone can promote T cell activation and can be used in cancer immunity research.
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MSX3
0 ImagesCat. No.: HY-102086CAS No.: 261717-23-1MSX3 is an orally active, selective A2a adenosine receptor antagonist and a prodrug of MSX2 (HY-117184). MSX3 reduces hyperphosphorylation of Tau at specific epitopes in mice without altering total Tau levels, Tau fragments, or Tau aggregation in these animals. MSX3 enhances spatial memory. MSX3 regulates effort-related decision-making behaviors. MSX3 reverses D2 antagonist-induced suppression of lever pressing, increased Chow feed intake, reduced selection of high-barrier arms, and prolonged response latency, and also slightly attenuates effects induced by D1 antagonists. MSX3 can be used in the research of Tauopathies (Alzheimer's disease-related), depression, and Parkinsonism.
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A1AR antagonist 5
0 ImagesCat. No.: HY-147544CAS No.: 1030509-01-3A1AR antagonist 5 (compound 20) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 5.83 and a pKi of 6.11.
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ST 1535
0 ImagesST 1535 is a potent and orally active A2A adenosine receptor antagonist. ST 1535 shows antiparkinsonian activity and antitremorigenic effects. ST 1535 has the potential for the research of Parkinson’s disease.
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A1AR antagonist 4
0 ImagesCat. No.: HY-147543CAS No.: 1031993-35-7A1AR antagonist 4 (compound 22) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 5.51 and a pKi of 6.29.
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LAS38096
0 ImagesCat. No.: HY-111295CAS No.: 851371-22-7LAS38096 is a potent, selective, and efficacious A2B Adenosine Receptor antagonist, with a Ki of 17 nM.
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