a1ar

A1AR antagonist 1 (compound 18g) is a potent A1 adenosine receptor (AR) antagonist with Ki values of 2.08, 6.91, and 31.2 nM for hA1, hA2A, and hA2B, respectively [1].

AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.

A1AR antagonist 3 (compound 13) is a selective adenylate 1 (A1) receptor antagonist with an affinity for human A1 (Ki: 9.69 nM) and rat A1 (Ki: 0.529 nM). It is suitable for research on neurological diseases.

A1AR antagonist 5 (compound 20) is a potent and selective inhibitor of the A1 adenosine receptor (A1AR) with a pKi of 6.11 and a pIC50 of 5.83 [1].

A1AR antagonist 2 (compound 18h) is a potent antagonist of the A1 adenosine receptor (AR) with Ki values of 1.49, 10.2, and 50.1 nM for hA1, hA2A, and hA2B, respectively [1].

A1AR antagonist 6 (compound 15) is a potent and selective inhibitor of the A1 adenosine receptor (A1AR), exhibiting a pKi of 7.13 and a pIC50 of 6.38[1].

A1AR antagonist 4 (compound 22) is a potent and selective A1 adenosine receptor (A1AR) antagonist with a pIC50 value of 5.51 and a pKi value of 6.29 [1].

A2A A1 AR antagonist-1 (compound 1a) is a potent dual antagonist with Ki values of 5.58 nM and 24.2 nM for A2A and A1 AR, respectively, demonstrating potential for ischemic stroke research [1].

A1/A3 AR antagonist 1 (Compound 10) is a potent, dual adenosine 1 (A1) and adenosine 3 (A3) receptor antagonist that acts on human A1 (Ki: 37.6 nM), human A3 (Ki: 25.4 nM) and rat A1 (Ki: 1.47 nM). 1 Can be used to study renal failure, inflammatory lung disease and Alzheimer's disease.

Compound Cpd1, an α1b-AR antagonist 1, is a selective inhibitor of the α1B-AR receptor and can be utilized in research related to cardiovascular and central nervous system diseases [1].

PROTAC AR AR-V7 degrader-1 (27c) serves as a dual degrader targeting both AR and AR-V7, showcasing DC50 values of 2.67 and 2.64 μM for AR and AR-V7, respectively. It effectively induces apoptosis (Red: AR antagonist; Blue: E3 ligase ligand; Black: linker) [1].

AR AR-V7-IN-1 (Compound 20i) serves as an inhibitor of AR ARV7, demonstrating an IC 50 of 172.85 nM. It effectively inhibits cell growth in the LNCaP and 22RV1 cell lines, with IC 50 values of 4.87 μM and 2.07 μM, respectively. Additionally, it shows potent tumor growth inhibition in a 22RV1 xenograft study. AR AR-V7-IN-1 is useful in studies related to prostate cancer [1].

β3-AR agonist 1 is a highly selective, and orally available agonist of β3-adrenergic receptor (EC50: 18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold).

Ar-V7-IN-1 is a highly potent inhibitor specifically targeting Ar-V7, a splice variant of the androgen receptor exhibiting hormone-independent behavior, and shows promise for researching various indications, notably cancers such as prostate cancer[1].

PROTAC AR-V7 degrader-1 (Compound 6) is an orally bioavailable, potent, and selective degrader targeting the androgen receptor (AR) variant V7, achieving degradation with a DC50 of 0.32 µM by directing the VHL E3 ligase to the AR DNA-binding domain (DBD). It demonstrates efficacy in the 22Rv1 cell line expressing AR-V7, with an EC50 of 0.88 µM [1].

Compound 23, designated as A2A/A3 AR antagonist-1, is a dual fluorescent ligand targeting A2A and A3 adenosine receptors (AR), exhibiting dissociation constants (Ki) of 90 nM for hA2A AR and 31.8 nM for hA3 AR, respectively [1].

PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule from the protein-targeting chimeras (PROTACs) that selectively targets the N-terminal domain (AR-NTD) of the Androgen Receptor variant AR-V7. By antagonizing AR-NTD, it effectively degrades AR-V7 protein and induces apoptosis in prostate cancer (PC) cells, with degradation efficiencies of 62.2% (1 μM) and 71.1% (5 μM) in VCaP cells [1].

N6-(2-Phenylethyl)adenosine (N6-Phenethyladenosine) is an adenosine derivative and adenosine receptor agonist with Ki values of 11.8 nM for rat A1 receptors and 30.1 nM for human A1 receptors.

N6-Ethyladenosine, an adenosine derivative, acts as an agonist of Adenosine receptors (hA1AR and hA3AR) with Ki values of 4.9 nM and 4.7 nM, respectively.

CPFPX is a highly selective radioactive ligand for the A1 adenosine receptor (A1AR).

Adenosine receptor inhibitor 2 (compound 14b) is a potent inhibitor of AR (adenosine receptor), exhibiting dual affinity towards A1 A2A ARs with higher affinity for A1- than A2A AR, and Ki values of 52.2 nM for A1 AR and 167 nM for A2A AR.

VCP-746 is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling. VCP746 reduces hypertrophy in a rat neonatal cardiac myocyte model. VCP746 is a hybrid molecule consisting of an adenosine moiety linked to an adenosine A1 receptor (A1AR) allosteric modulator moiety. At the A1AR, VCP746 mediated cardioprotection in the absence of haemodynamic side effects such as bradycardia.

2'-MeCCPA is a potent and highly selective A1 adenosine receptor (A1AR) agonist with a K-value of 1.8 nM for AR. 2'-MeCCPA inhibits trichostatin-stimulated adenylate cyclase activity with an IC value of 13.1 nM, exhibits analgesic activity, and can be used in the study of HCV.

FSCPX is a potent and selective irreversible antagonist of the A1 adenosine receptor (A1AR), exhibiting low nanomolar binding potency. It can effectively decrease the interstitial adenosine level in the guinea pig atrium, thereby modifying the effect of [NBTI], a nucleoside transport inhibitor.

MIPS521 ({2-Amino-4-[3,5-bis(trifluoromethyl)phenyl]thiophen-3-yl}(4-chlorophenyl)methanone) is a positive allosteric modulator of the A1R.