1. Signaling Pathways
  2. GPCR/G Protein
  3. Adenosine Receptor

Adenosine Receptor

P1 receptor

Adenosine receptors (ARs) comprise a group of G protein-coupled receptors (GPCR) which mediate the physiological actions of adenosine. To date, four AR subtypes have been cloned and identified in different tissues. These receptors have distinct localization, signal transduction pathways and different means of regulation upon exposure to agonists. A key property of some of Adenosine receptors is their ability to serve as sensors of cellular oxidative stress, which is transmitted by transcription factors, such as NF-κB, to regulate the expression of ARs. The importance of Adenosine receptors in the regulation of normal and pathological processes such as sleep, the development of cancers and in protection against hearing loss will be examined.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-185758
    LUF5437
    Antagonist
    LUF5437 is a potent and selective adenosine A1 receptor antagonist with a rat Ki of 7.3 nM. LUF5437 can be used for research on cardiovascular and neurological diseases.
    LUF5437
  • HY-118455
    MRS1097
    Antagonist
    MRS1097 is a potent antagonist of adenosine hA3 receptor, with the Ki of 100 nM.
    MRS1097
  • HY-115494
    Neladenoson dalanate hydrochloride
    Agonist
    Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) hydrochloride is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate hydrochloride has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases.
    Neladenoson dalanate hydrochloride
  • HY-156983
    MRS 5980
    MRS 5980 is an A3AR agonist with a Ki value of 0.7 nM. MRS 5980 has oral activity.
    MRS 5980
  • HY-155772
    LUF7690
    LUF7690 (Compound 9) is a clickable and covalent affinity-based probe (AfBP) that targets the human A3AR (hA3AR). LUF7690 can be used in the detection and characterization of the hA3AR in different types of granulocytes, among other cell types.
    LUF7690
  • HY-144672
    A2A receptor antagonist 2
    Antagonist
    A2A receptor antagonist 2 (Compound 57) is a potent, highly selective adenosine A2A receptor (A2AR) antagonist with an IC50 of 8.3 nM.
    A2A receptor antagonist 2
  • HY-159889
    hA3AR agonist 2
    Agonist
    hA3AR agonist 2 (compound 1h) is an A3AR agonist, with a Ki of 3.5 nM.
    hA3AR agonist 2
  • HY-170948
    A2AR modulator-1
    Modulator
    A2AR modulator-1 (Compound 45) is a selective negative allosteric adenosine A2a receptor (A2aR) modulator with an IC50 value of 9 nM. A2AR modulator-1 reduces the affinity of endogenous adenosine for the receptor and inhibits cAMP signaling pathway activation. A2AR modulator-1 potently restores pCREB phosphorylation in CD4+ T cells, reversing immunosuppression in the tumor microenvironment, and shows potential to suppress tumor growth and metastasis in triple-negative breast cancer models.
    A2AR modulator-1
  • HY-171467
    MRS7799
    Antagonist
    MRS7799 is a selective A 3 Adenosine Receptor antagonist agsinst human, mouse, and rat A3AR with Kds of 0.55, 3.74 and 2.80 nM, respectively. MRS7799 can be used in the study of neurodegeneration, cancer, ischemia of the heart and brain, autoimmune inflammatory diseases.
    MRS7799
  • HY-W782193
    Sulcatone-d5
    Sulcatone-d5 (6-Methyl-5-hepten-2-one-d5) is the deuterium labeled Sulcatone (HY-W010435). Sulcatone (6-Methyl-5-hepten-2-one) is a plant-derived volatile organic compound with activities such as insecticidal, antifungal, and blood pressure-lowering effects. Sulcatone also serves as an insect pheromone and an endogenous metabolite, which can be found in feces. Changes in Sulcatone levels can be used for the auxiliary diagnosis of ulcerative colitis.
    Sulcatone-d<sub>5</sub>
  • HY-175195
    Adenosine receptor antagonist 6
    Antagonist
    Adenosine receptor antagonist 6 is an orally active and selective A2A adenosine receptor (A2AAR) antagonist, with a Ki of 19.18 nM. Adenosine receptor antagonist 6 inhibits 5’-N-ethylcarboxamide adenosine (NECA) (HY-103173)-mediated cAMP production (IC50 = 0.089 μM) and immunosuppression, while promoting IL-2 and IFN-γ secretion. Adenosine receptor antagonist 6 abolishes the immunosuppressive effects of adenosine on T-cell activation and cytokine release. Adenosine receptor antagonist 6 inhibits tumor growth in a CT26/MC38 xenograft model. Adenosine receptor antagonist 6 can be used for the study of colon cancer.
    Adenosine receptor antagonist 6
  • HY-A0168A
    Regadenoson hydrate
    Agonist
    Regadenoson hydrate (NSC 169186) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson hydrate also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS.
    Regadenoson hydrate
  • HY-146457
    A3AR antagonist 1
    Antagonist
    A3AR antagonist 1 (compound 17) is a potent and selective human A3 adenosine receptor (AR) antagonist, with an Ki of 4.63 nM. A3AR antagonist 1 shows no affinity for the rat A3 AR even at high concentrations.
    A3AR antagonist 1
  • HY-182432
    A3AR antagonist-7
    Antagonist
    A3AR antagonist-7 is a conjugable human A3 adenosine receptor (A3AR) antagonist with a Ki value of 31.8 nM. A3AR antagonist-7 is applicable to the research of melanoma, breast cancer and colorectal cancer.
    A3AR antagonist-7
  • HY-B0549S
    Flavoxate-d5
    Ligand
    Flavoxate-d5 is deuterium labeled Flavoxate. Flavoxate hydrochloride (Rec-7-0040; DW61) is an orally active L-type Ca2+ channel inhibitor and antispasmodic. Flavoxate hydrochloride inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba2+ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate hydrochloride induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate hydrochloride effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate hydrochloride can be used in research on overactive bladder and related voiding dysfunctions.
    Flavoxate-d<sub>5</sub>
  • HY-105410
    OT-7100
    OT-7100 is an orally active analgesic agent. OT-7100 inhibits hyperalgesia possibly by enhancing adenosinergic neurotransmission in the dorsal horn. OT-7100 can be used for the researches of inflammation, neurological and metabolic disease such as diabetes2].
    OT-7100
  • HY-106180
    DTI 0009
    Agonist
    DTI 0009 is a selective adenosine A1 receptor agonist used to reduce heart rate in patients with atrial fibrillation and to treat arrhythmias.
    DTI 0009
  • HY-12099
    A3AR antagonist 2
    Antagonist
    A3AR antagonist 2 (compound 18) is a potent Human A3 adenosine receptor antagonist with an Ki value of 4.54 nM.
    A3AR antagonist 2
  • HY-158057
    A2AR/A2BR antagonist 1
    Antagonist
    A2AR/A2BR antagonist 1 (compound 7ai) has a dual antagonistic effect on A2AR/A2BR, with the IC50 values of 11.2 nM and 6.4 nM for A2AR and A2BR, respectively. A2AR/A2BR antagonist 1 promotes T cell-mediated cancer cell death.
    A2AR/A2BR antagonist 1
  • HY-W011012R
    Adenosine 5'-monophosphate disodium (Standard)
    Adenosine 5'-monophosphate (disodium) (Standard) is the analytical standard of Adenosine 5'-monophosphate (disodium). This product is intended for research and analytical applications. Adenosine 5'-monophosphate disodium is an orally active purine nucleotide, and participates in ATP metabolism. Adenosine 5'-monophosphate disodium is also a ligand for adenosine 2B receptor. Adenosine 5'-monophosphate disodium can activate AMPK in skeletal muscle, and ameliorates insulin resistance and impaired glucose metabolism. Adenosine 5'-monophosphate disodium can be used for research of diabetes.
    Adenosine 5'-monophosphate disodium (Standard)
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