Adenosine Receptor Agonist

Inosine-¹³C is the ¹³C labeled Inosine. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A₁ (A₁R) and A_2A (A_2AR) receptors.

A3AR agonist 1 (Compound 12) is an A3AR agonist (K_i: 25.8 nM). A3AR agonist 1 stimulates β-arrestin2 recruitment, with an EC₅₀ value of 5.17 nM. A3AR agonist 1 can be used for research of inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, etc.

CCPA (2-Chloro-N6-cyclopentyladenosine) hemihydrate a highly selective A1 adenosine receptors agonist with a K_i of 0.4 nM. CCPA hemihydrate inhibits adenylate cyclase with an IC₅₀ of 33 nM. CCPA hemihydrate exhibits anti-seizure and cardiacprotective activity. CCPA hemihydrate can be used for the research of seizure and myocardial infarction.

GW-493838 is a potent Adenosine A1 (A1AR) agonist. GW-493838 has the potential for the research of neuropathic pain.

MRS3558 is a potent and selective A3AR agonist, with K_i values of 0.6 nM for humans and 0.9 nM for rats, making it suitable for research in the fields of neuropathic pain and anesthesia.

BW-534U87 is an orally active adenosine A1 receptor agonist and competitive adenosine deaminase (ADA) inhibitor (K_i=7 μM). BW-534U87 elevates brain adenosine levels and suppresses epileptiform activity. BW-534U87 demonstrate anticonvulsant efficacy in animal seizure models. BW-534U87 is promising for research of epilepsy and adenosine-related neuropsychiatric disorders.

N6-Benzyl-5'-ethylcarboxamido adenosine is a selective A3 adenosine receptor agonist.

hA3AR agonist 1 is a potent human A₃ adenosine receptor (hA₃AR) agonist with a K_i value of 2.40 nM.

A3AR agonist 3 (Compound 15A) is a A3 adenosine receptor (A3AR) agonist, with K_i and EC₅₀ values of 2.27 and 0.20 nM for hA3 and cAMP, respectivelly. A3AR agonist 3 can be used for the research of neuroinflammation.

Adenosine monophosphate-¹³C₁₀,¹⁵N₅,d₁₂ (AMP-¹³C₁₀,¹⁵N₅,d₁₂) dilithium is ¹³C and ¹⁵N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction.

A3AR agonist 2 (Compound 19) a selective A3AR agonist (K_i: 22.1 nM). A3AR agonist 2 stimulates β-arrestin2 recruitment, with EC₅₀ value of 4.36 nM. A3AR agonist 2 can be used for research of inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, and other chronic conditions. A3AR agonist 2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

7-Methyladenosine perchlorate is a synthetic analog of adenosine with agonist activity at adenosine receptors. 7-Methyladenosine perchlorate is able to modulate cell signaling and is useful for studying adenosine-related biological processes. 7-Methyladenosine perchlorate can be used as a potential inhibitor in compound development.

CP-608039 is a potent and selective adenosine A3 receptor agonist. CP-608039 can be used for ischemic myocardial injury research.

A3AR agonist 4 is an A3 adenosine receptor (A3AR) agonist (K_i: 1.24 nM for hA3AR). A3AR agonist 4 inhibits cAMP production with an EC₅₀ of 0.17 nM. A3AR agonist 4 can be used for research of inflammation and pain.

(Rac)-Mirabegron-d₅ is a deuterium labeled (Rac)-Mirabegron. (Rac)-Mirabegron is the racemate of Mirabegron. Mirabegron is a selective β3-adrenoceptor agonist.

A3AR modulator 1 (MRS8054) is an orally active A3 adenosine receptor (A3AR) (Adenosine Receptor) positive allosteric modulator (PAM). A3AR modulator 1 greatly enhances Cl-IB-MECA-stimulated [³⁵S]GTPγS binding E_max.

MRS7469 is a highly selective A1 adenosine receptor (A1AR) agonist with over 2000-fold selectivity over other adenosine receptor subtypes. MRS7469 stably binds to the orthosteric binding site of A1AR, and exhibits extremely high affinity for both humans and mice (e.g., human pK_i is 8.67, mouse pK_i is 9.43). By activating central A1AR, MRS7469 significantly induces hypothermia, motor inhibition and psychomotor dysfunction, and can be widely used in research related to depression and other relevant fields.

AMP-579 is an adenosine receptor agonist that primarily targets adenosine A1 and A2_A receptors (with K_i values of 1.7 and 4.5 nM for the A1 receptor in rat brain and adipocytes, and a K_i value of 56 nM for the A2_A receptor in rat brain). AMP-579 inhibits lipolysis, restores insulin-dependent glucose transport, and reduces heart rate through the activation of A1 receptors, while it induces vasodilation, particularly in coronary arteries, through the activation of A2_A receptors (with an IC₅₀ of 0.3 μM in porcine coronary arterial rings). AMP 579 shows potential for application in cardioprotection and the treatment of acute myocardial infarction.

MRS5663 (Compound 3a) is an A3AR agonist, with an EC₅₀ of 5.62 nM for β-arrestin2 recruitment assay. MRS5663 has a cytoprotective effect on skeletal muscle ischemia-reperfusion injury/claudication model.

LASSBio-1359 is an adenosine A2A receptor agonist with vasodilatory and anti-inflammatory activities.