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A2A/2B R Inhibitors

" in MedChemExpress (MCE) Product Catalog:

3094

Inhibitors & Agonists

3

Screening Libraries

44

Fluorescent Dye

53

Biochemical Assay Reagents

294

Peptides

1

MCE Kits

131

Inhibitory Antibodies

268

Natural
Products

912

Recombinant Proteins

242

Isotope-Labeled Compounds

188

Antibodies

52

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P1108A

    CFTR Others
    Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B TFA antagonizes CRF2-mediated inhibition of gastric emptying [2] .
    Astressin <em>2B</em> TFA
  • HY-102024

    CPI-444 analog

    Adenosine Receptor Neurological Disease Cancer
    A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Ki values of 4 and 264 nM, respectively .
    <em>A2</em>A receptor antagonist 1
  • HY-148076

    Adenosine Receptor Cancer
    A2A receptor antagonist 3 (Example 92) is an adenosine A2a receptor antagonist with a Ki of 0.4 nM. A2A receptor antagonist 3 also binds to A2b, A1 and A3 receptor with Kis of 37, 107 and 1467 nM, respectively .
    <em>A2</em>A receptor antagonist 3
  • HY-P1108

    CFTR Others
    Astressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B antagonizes CRF2-mediated inhibition of gastric emptying [2] .
    Astressin <em>2B</em>
  • HY-144672

    Adenosine Receptor Inflammation/Immunology Cancer
    A2A receptor antagonist 2 (Compound 57) is a potent, highly selective adenosine A2A receptor (A2AR) antagonist with an IC50 of 8.3 nM .
    <em>A2</em>A receptor antagonist <em>2</em>
  • HY-145894

    Others Others
    NaPi2b-IN-2 (compound 5) is a potent inhibitor of sodium-dependent transport protein 2b (SLC34A2, NaPi2b), with an IC50 of 38 nM for human NaPi2b. NaPi2b-IN-2 can be used for the research of hyperphosphatemia .
    NaPi<em>2b</em>-IN-<em>2</em>
  • HY-P99348

    Ropeginterferon alfa-2B-njft; PEG-proline-interferon alpha-2B

    Apoptosis Cancer
    Ropeginterferon alfa-2b (Ropeginterferon alfa-2b-njft) is a monopegylated IFN-α that can be used for the research of myeloproliferative neoplasms .
    Ropeginterferon alfa-<em>2b</em>
  • HY-145897

    iGluR Neurological Disease
    NMDA-IN-2 (compound 6b), a Procaine derivative, is a NMDA receptor 2B subtype inhibitor .
    NMDA-IN-<em>2</em>
  • HY-P99497

    Integrin HCV Infection
    Cepeginterferon alfa-2b is a pegylated interferon. And Cepeginterferon alfa-2b has PEG with molecular weight of 20 kDa as a pegylated base. Cepeginterferon alfa-2b can be used for research of various diseases, such as hepatitis C virus (HCV), polycythemia vera (PV) and essential thrombocythemia (ET) [2].
    Cepeginterferon alfa-<em>2b</em>
  • HY-P99735

    IFNAR Infection
    Mipeginterferon alfa-2b is an interferon alpha-2b (IFNA2b) analogue, with an average number of 5 substituted among 11 amino groups (one N-terminal and 10 lysine N6). Mipeginterferon alfa-2b has the relative molecular mass of 40 kDa .
    Mipeginterferon alfa-<em>2b</em>
  • HY-P5695

    Bacterial Infection
    GP-2B is an antimicrobial peptide. GP-2B shows antibacterial activity against Gram-positive strain (MIC: 8-128 μg/mL for S. aureus and Enterococcus faecalis) .
    GP-<em>2B</em>
  • HY-P1114

    GSK-3 Neurological Disease
    2B-(SP) is a eIF2B-based substrate for glycogen synthase kinase-3 (GSK-3). 2B-(SP) is readily phosphorylated by both the α and β isoforms of GSK-3 .
    <em>2B</em>-(SP)
  • HY-145706

    Adenosine Receptor Neurological Disease
    A2A/A1 AR antagonist-1 (compound 1a) is dual potent A2A/A1 AR antagonist with Kis of 5.58 and 24.2 nM, respectively. A2A/A1 AR antagonist-1 has the potential for the research of ischemic stroke .
    <em>A2</em>A/A1 AR antagonist-1
  • HY-P1114A

    GSK-3 Cancer
    2B-(SP) TFA is a eIF2B-based substrate for glycogen synthase kinase-3 (GSK-3). 2B-(SP) TFA is readily phosphorylated by both the α and β isoforms of GSK-3 .
    <em>2B</em>-(SP) (TFA)
  • HY-116463C

    Sigma Receptor Neurological Disease
    (2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders .
    (<em>2</em><em>R</em>,3<em>R</em>)-E1<em>R</em>
  • HY-103169
    SCH442416
    1 Publications Verification

    Adenosine Receptor Neurological Disease
    SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR), with Kis of 0.048 and 0.5 nM for human and rat A2AR respectively. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). SCH442416 can be used for imaging of adenosine A2A receptors in rat and primate brain [2].
    SCH442416
  • HY-161418

    Adenosine Receptor Neurological Disease
    1-NBX is a potent and selective A1R ligand. 1-NBX exhibits significantly improved A1R affinity with with a Ki of 2.6 nM and lower affinity for the A2A receptor with a Ki of 164 nM. [ 18F]1-NBX acts as a promising candidate for further preclinical evaluation as potential PET tracer for A1R imaging .
    1-NBX
  • HY-120941

    Adenosine Receptor Cardiovascular Disease Inflammation/Immunology
    LASSBio-1359 is an adenosine A2A receptor agonist with vasodilatory and anti-inflammatory activities .
    LASSBio-1359
  • HY-137442
    Inupadenant
    1 Publications Verification

    EOS-850

    Adenosine Receptor Cancer
    Inupadenant is an orally active, highly selective A2A receptor antagonist. Inupadenant is not brain-penetrant. Inupadenant has potent anti-tumor activity .
    Inupadenant
  • HY-142957

    Others Others
    NaPi2b-IN-1 is a potent and orally active inhibitor of sodium-dependent phosphate transport protein 2b (NaPi2b) with an IC50 of 64 nM. NaPi2b is primarily expressed in the small intestine, lungs, and testes and plays an important role in phosphate homeostasis. NaPi2b-IN-1 has the potential for the research of hyperphosphatemia .
    NaPi<em>2b</em>-IN-1
  • HY-146429

    Others Metabolic Disease
    NaPi2b-IN-3 (compound 5) is a potent sodium-dependent transport protein 2b (SLC34A2, NaPi2b) inhibitor with IC50s of 71 nM and 28 nM for human NaPi2b and rat NaPi2b, respectively. NaPi2b-IN-3 can be used for researching hyperphosphatemia .
    NaPi<em>2b</em>-IN-3
  • HY-U00341

    Adenosine Receptor Neurological Disease
    ST4206 is a potent and orally active adenosine A2A receptor antagonist, with Kis of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively. ST4206 has the potential for Parkinson׳s disease research .
    ST4206
  • HY-117184

    Adenosine Receptor Neurological Disease
    MSX-2 is A2A adenosine receptor antagonist, with Ki of 5 nM in human that plays an important role in Parkinson's disease [2].
    MSX-<em>2</em>
  • HY-147541

    Adenosine Receptor Inflammation/Immunology
    A2A/A3 AR antagonist-1 (compound 23) is a dual A2A/A3 adenosine receptor (AR) fluorescent ligand, with Kis of 90 nM and 31.8 nM for hA2A AR and hA3 AR, respectively .
    <em>A2</em>A/A3 AR antagonist-1
  • HY-103164

    Adenosine Receptor Monoamine Oxidase Neurological Disease
    (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 .
    (E)-8-(3-Chlorostyryl)caffeine
  • HY-103162

    Adenosine Receptor Neurological Disease
    ANR94 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 [2].
    ANR94
  • HY-B2006

    Phosphatase Bacterial Infection
    Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC50 of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide .
    Fenvalerate
  • HY-101337

    RS 21361 free base

    Imiloxan is a potent and selective alpha 2B-adrenoceptor antagonist. Imiloxan has the potential for acute kidney injury research [2].
    Imiloxan
  • HY-101337A

    RS 21361

    Imiloxan hydrochloride is a potent and selective alpha 2B-adrenoceptor antagonist. Imiloxan hydrochloride has the potential for acute kidney injury research [2].
    Imiloxan hydrochloride
  • HY-N12250

    Others Cancer
    7-Deoxynarciclasine (compound 2b) can be isolated from Hymenocallis littoralis. 7-Deoxynarciclasine inhibits the cancer cell growth .
    7-Deoxynarciclasine
  • HY-10995
    Tozadenant
    2 Publications Verification

    SYN115

    Adenosine Receptor Neurological Disease
    Tozadenant is an adenosine A2A receptor antagonist, with Ki of 11.5 nM on human A2A and 6 nM on rhesus A2A.
    Tozadenant
  • HY-19533
    SCH 58261
    5+ Cited Publications

    Adenosine Receptor Cancer
    SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC50 of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively [2] .
    SCH 58261
  • HY-P99666

    IFNAR Infection
    Albinterferon alfa-2b is a type I interferon that activates novel genes and exerts potent antiviral and antiproliferative activity on target cells. Signaling by Albinterferon alfa-2b requires receptor-dependent activation of Stat1 and Stat2 to form a heterodimeric STAT that binds to the DNA-binding protein IRF-9 (p48) and forms ISGF-3 (IFN-stimulated gene factor 3). The driver genes are then further activated by ISGF-3 to achieve antiviral function .
    Interferon alfa
  • HY-106441A

    MK-0657; CERC-301

    iGluR Neurological Disease
    Rislenemdaz (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM, respectively.
    Rislenemdaz
  • HY-136233

    Adenosine Receptor Inflammation/Immunology
    PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research [2] .
    PSB 0777 ammonium
  • HY-136233A

    Adenosine Receptor Inflammation/Immunology
    PSB 0777 ammonium hydrate is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium hydrate has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium hydrate shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium hydrate has the potential for inflammatory bowel disease (IBS) research research [2] .
    PSB 0777 ammonium hydrate
  • HY-12294A
    PEAQX tetrasodium hydrate
    5 Publications Verification

    NVP-AAM077 tetrasodium hydrate

    iGluR Apoptosis Neurological Disease
    PEAQX (NVP-AAM077) tetrasodium hydrate is a potent, selective and orally active NMDA antagonist, with IC50 values of 270 nM and 29600 nM for hNMDAR 1A/2A and hNMDAR 1A/2B, respectively .
    PEAQX tetrasodium hydrate
  • HY-B2006S

    Phosphatase Bacterial Infection
    Fenvalerate-d5 is the deuterium labeled Fenvalerate. Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC50 of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide[1].
    Fenvalerate-d5
  • HY-15472

    5-HT Receptor Cardiovascular Disease
    PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.
    PRX-08066
  • HY-15472A

    5-HT Receptor Cardiovascular Disease
    PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.
    PRX-08066 maleate
  • HY-12294

    NVP-AAM077

    iGluR Neurological Disease
    PEAQX(NVP-AAM 077) is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/2B(29,600 nM).
    PEAQX
  • HY-160210

    Adrenergic Receptor Cardiovascular Disease
    BAY-6096 is a potent, selective, and highly water-soluble adrenergic receptor α2B antagonist with an IC50 of 14 nM. BAY-6096 can effectively reduceα 2B receptor agonist-induced rat vascular contraction .
    BAY-6096
  • HY-B0579
    Cyclosporin A
    95+ Cited Publications

    Cyclosporine A; Ciclosporin A; CsA

    Molecular Glues Phosphatase Complement System Antibiotic Inflammation/Immunology Cancer
    Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion .
    Cyclosporin A
  • HY-112840

    Adenosine Receptor Neurological Disease
    ST3932 is a metabolite of ST1535, acts as an antagonist of adenosine A2A receptor, with Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively.
    ST3932
  • HY-11100
    Asenapine maleate
    1 Publications Verification

    Org 5222 maleate

    5-HT Receptor Neurological Disease
    Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and D2 antagonist with Ki values of 0.03-4.0 nM, 1.3nM, respectively, and an antipsychotic.
    Asenapine maleate
  • HY-110279

    GPR68 Neurological Disease
    Ogerin is a selective GPR68 positive aliasing modulator (PAM) (pEC50=6.83) with a moderate antagonistic effect on A2A (Ki=220 nM). Ogerin inhibits the fear conditioning reflex in mice and also inhibits TGF-β-induced myofibroblast differentiation of fibroblasts from multiple organ systems. Ogerin can be used in the studies of fibrotic diseases and neurological disorders [2].
    Ogerin
  • HY-151145

    Glucosidase Metabolic Disease
    α-Glucosidase-IN-21 (Compound 2B) is a potent, orally active α-glucosidase inhibitor with an IC50 of 2.62 μM. α-Glucosidase-IN-21 shows anti-diabetic activity .
    α-Glucosidase-IN-21
  • HY-157262

    Others Infection
    Methyl isonicotinate-(CH2)2-COOH (hapten 2b) is a hapten that can be activated with NHS and DCC. Methyl isonicotinate-(CH2)2-COOH has more immunogenicity and hydrophobicity .
    Methyl isonicotinate-(CH<em>2</em>)<em>2</em>-COOH
  • HY-A0168S

    CVT-3146-d3

    Adenosine Receptor Cardiovascular Disease Cancer
    Regadenoson-d3 is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents[1][2][3].
    Regadenoson-d3
  • HY-101043

    Sigma Receptor iGluR Neurological Disease
    4-PPBP maleate is a potent σ 1 receptor ligand and agonist. 4-PPBP maleate is a non-competitive, selective NR1a/2B NMDA receptors (expressed in Xenopus oocytes) antagonist. 4-PPBP maleate provides neuroprotection [2] .
    4-PPBP maleate