ar antagonist-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].

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].

5-HT6/5-HT2AR antagonist-1 is a potent dual antagonist for the 5-HT6 and 5-HT2A receptors, demonstrating high efficacy with K_i values of 11 nM and 39 nM, respectively [1].

GluN2B-NMDAR Antagonist-1, an orally active compound, functions as a GluN2B-NMDAR antagonist with neuroprotective properties. It is applicable in the research of ischemic injury [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 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].

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.

A3AR antagonist 1 is a potent and selective human A3adenosine receptor (AR) antagonist (Ki: 4.63) and has no affinity for the rat A3AR.

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].

AR antagonist 10 (Compound Y5) is a potent, orally active androgen receptor (AR) antagonist with an IC50 value of 0.04 μM. It demonstrates a dual mechanism of action: antagonizing AR by disrupting AR dimerization and inducing AR degradation through the ubiquitin-proteasome pathway. This compound shows excellent activity against various resistant AR mutants and effectively inhibits the growth of LNCaP xenograft tumors. AR antagonist 10 is applicable for research in resistant prostate cancer.

AR antagonist 14 serves as a ligand for the target protein in PROTAC applications. It can be coupled with VH 101-amide-piperidine-Pip-alkyne to synthesize the PROTAC degrader [ARD-69].

AR antagonist 11 (Compound c2) is a selective androgen receptor antagonist with an IC50 of 0.019 μM. It is also effective against the ARF877L/T878A mutant (IC50: 1.03 μM). Additionally, AR antagonist 11 inhibits LNCaP cell proliferation and decreases PSA protein expression (IC50: 0.54 μM). This compound is applicable in prostate cancer (PCa) research.

AR antagonist 13 (compound 19) is an androgen receptor (AR) antagonist that inhibits prostate cancer cell growth, achieving an inhibition rate of over 71.5% at a concentration of 10 μM.

AR antagonist 15 is an orally active androgen receptor (AR) antagonist with an IC50 of 97 nM for ART787A. It impairs AR nuclear translocation, hinders AR homodimerization, and inhibits AR-regulated gene transcription by competitively binding to the ligand-binding pocket. AR antagonist 15 significantly reduces prostate-specific antigen (PSA) levels and induces apoptosis by decreasing the expression of apoptosis-related proteins. This compound is useful for prostate cancer research.

AR antagonist 12 (compound 20i) is an orally active androgen receptor antagonist, demonstrating IC50 values of 119.3 μM for wt-AR and 98.2 μM for AR-F877L. It induces a dose- and time-dependent reduction in the protein levels of AR, AR-v7, and PSA. AR antagonist 12 exhibits anticancer activity, making it useful in the study of Enzalutamide-resistant prostate cancer.

NMDAR antagonist 1 is an orally active, NR2B-selective NMDAR antagonist.

A2AAR antagonist 1 (compound 21a) is a potent A2AAR (adenosine A2A receptor) antagonist with high ligand efficiency and a Ki value of 20 nM. It is applicable in neurodegenerative disease research [1].

(Rac)-NMDAR antagonist 1 is a racemate of NMDAR antagonist 1, a potent, orally active, NR2B-selective NMDAR antagonist.

A2AR-antagonist-1 (compound 38), an orally active adenosine A2A receptor antagonist with an IC50 value of 29 nM, demonstrates anti-tumor properties and stability in mouse liver microsomes (t1/2 = 86.1 min). Additionally, it activates T cells by inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and promoting expression of effector molecules (GZMB, IFNG, and IL-2) [1].

Compound 4a, also known as hA2AAR antagonist 1, is a highly selective hA2AAR antagonist with a Ki value of 5 nM. It is useful in the field of immuno-oncology research.

β2AR antagonist 1 (Cmpd-15PA) acts as an antagonist to the β2 adrenergic receptor (β2AR). This compound binds to the intracellular surface of β2AR.

Androgen receptor antagonist 1 is an orally available full antagonist of the androgen receptor (AR), with an IC50 value of 59 nM, demonstrating high potency against AR signaling. Androgen receptor antagonist 1 can further be employed in the synthesis of PROTAC AR degraders, which induce targeted protein degradation, achieving 24% and 47% AR protein reduction in LNCaP cells at concentrations of 1 μM and 10 μM, respectively, thereby offering significant utility in prostate cancer research.

UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively), and has anti-prostate cancer efficacy.

DMPX (3,7-Dimethyl-1-propargylxanthine) is a caffeine-like compound capable of crossing the blood-brain barrier. It serves as an A2-selective adenosine receptor (AR) antagonist, effectively and selectively blocking the hypothermia and behavioral inhibition induced by A2 adenosine receptor agonists, such as NECA. DMPX is utilized in research on diseases like Parkinson's disease.