ar antagonist 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].

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

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].

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].

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].

A1/A3 AR Antagonist 3 is a dual A1R/A3R antagonist that demonstrates high affinity within the low-micromolar to nanomolar range, and is potentially useful in the research of chronic heart diseases [1].

C5aR1 antagonist 1 (compound 7e) is an orally active C5a receptor antagonist. It demonstrates efficacy in both DISCO and migration assays, with IC50 values of 38 nM and 17 nM, respectively. This compound is useful for research in both acute and chronic inflammatory diseases.

A2AR/A2BR antagonist 1 (compound 7ai) acts as a dual antagonist to A2AR and A2BR with IC50 values of 11.2 nM and 6.4 nM, respectively. Additionally, A2AR/A2BR antagonist 1 enhances T cell-mediated cancer cell death.

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 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 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].

The compound is an A1/A3 adenosine receptor antagonist that aids in the treatment of (neurological) inflammatory diseases.

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.

C5aR1 antagonist peptide, a biologically active linear peptide originating from the C-terminus of the chemokine complement fragment 5 anaphylatoxin (C5a), inhibits C5a binding and activity at human and rat C5a receptors. Overexpression of C5a is linked to various immunoinflammatory diseases, including arthritis, Alzheimer's disease, cystic fibrosis, and systemic lupus erythematosus.

C5aR1 antagonist 2 (Compound 6a), an orally active antagonist of C5a receptor 1 (C5aR1), effectively inhibits increases in neutrophil counts induced by C5a. This compound demonstrates potency in both DISCO and migration assays, with IC50 values of 21 and 3 nM, respectively. It is utilized in the study of acute and chronic inflammatory 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.