β-ar

Compound 43, also known as β-AR antagonist 2, is an antagonist of β-AR with an IC50 of 0.17 μM. It inhibits the growth of mouse A549 xenograft tumors and demonstrates cardioprotective efficacy against DOX-induced heart failure in C57 mice [1].

AR-08 is a potent α2-adrenergic receptor agonist for the study of ADHD and attention deficit.

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.

PROTAC AR Degrader-9 (Compound c6) is a PROTAC-based degrader specifically targeting the androgen receptor. It effectively degrades the androgen receptor in human dermal papilla cells (HDPC) with a DC50 of 262.38 nM. Additionally, this compound enhances the expression of paracrine factors, such as TGF-β1 and β-catenin, thereby promoting hair regeneration in mouse models. [Pink: ligand for target protein AR ligand-38; Black: linker; Blue: ligand for E3 ligase Cereblon]

Azenosertib (ZN-c3) is an orally active, specific GPR119 agonist. Azenosertib (ZN-c3) stimulates cell proliferation and improves pancreatic β-cell function. [1]

AR-13324 analog mesylate, an inhibitor of Rho-kinase and the norepinephrine transporter, reduces intraocular pressure in normotensive monkey eyes.

AR-13324 M1 metabolite is a hydrolysis metabolite of AR-13324 mesylate.

AR-A 2 is a selective 5-HT1B receptor antagonist with high affinity to guinea pig cortex 5-HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki: 0.24 and 0.47 nM), exhibiting a 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki: 5 nM).

AR-C102222 hydrochloride is a competitive, orally active, and highly selective inducible nitric oxide synthase (iNOS) inhibitor (IC50: 37 nM). It has antinociception and anti-inflammatory activities.

AR453588 is an orally bioavailable anti-diabetic glucokinase activator (EC50: 42 nM) with anti-hyperglycemic activity.

AR453588 hydrochloride is an orally bioavailable anti-diabetic glucokinase activator (EC50: 42 nM) with anti-hyperglycemic activity.

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).

β3-AR agonist 2 is a potent and selective agonist of β3-adrenergic receptor (β3-AR with an EC50 of 8 nM).

ar-Turmerol is a useful organic compound for research related to life sciences and the catalog number is T126273.

(rel)-AR234960 is the active relative configuration of AR234960, a non-peptide agonist of MAS.

AR-9281 (APAU) is a potent and selective inhibitor of soluble epoxide hydrolase (s-EH) potentially for the treatment of hypertension and type 2 diabetes

AR-C155858 is an inhibitor of monocarboxylate transporter MCT1 and MCT2 (Kis: 2.3 nM and 10 nM).

AR-A014418 (GSK 3β inhibitor VIII) is an ATP-competitive, and selective GSK3β inhibitor.

AR ligand-30 serves as the target protein ligand for PROTAC Bavdegalutamide, utilized in prostate cancer research.

AR antagonist 9 is an orally active, selective androgen receptor (AR) antagonist that inhibits cancer by disrupting the formation of AR ligand-binding domain dimers, showing potential in overcoming drug resistance in prostate cancer (PCa). Its antagonistic activity against AR has an IC50 of 0.051 μM, comparable to Enzalutamide (IC50= 0.060 μM). This compound demonstrates superior inhibitory effects on ARF876L/T877A and ARW741C mutants compared to Enzalutamide. Additionally, AR antagonist 9 possesses favorable pharmacokinetic properties, with an oral bioavailability (F) of 66.24% in rats, and significantly inhibits tumor growth in LNCaP xenograft mouse models upon oral administration. AR antagonist 9 holds promise for research in overcoming PCa resistance.

AR ligand-32 is a ligand for target proteins, employed in the synthesis of PROTAC AR Degrader-7.

AR ligand-33 is a ligand for the androgen receptor (AR), and it can be used as a target protein ligand for the synthesis of PROTAC AR Degrader-8.

PROTAC AR Degrader-8 (Compound NP18) functions as a PROTAC degrader targeting the androgen receptor (AR) and effectively degrades AR-FL in both 22Rv1 and LNCaP cells with DC50 values of 0.018 μM and 0.14 μM, respectively. It also degrades AR-V7 in 22Rv1 cells with a DC50 of 0.026 μM. Additionally, PROTAC AR Degrader-8 inhibits the proliferation of 22Rv1 and LNCaP cancer cells, exhibiting IC50 values of 0.038 μM and 1.11 μM. It induces cell cycle arrest at the G2/M phase and triggers apoptosis in 22Rv1 cells (apoptosis). Demonstrating anticancer efficacy, PROTAC AR Degrader-8 shows activity in both mouse and zebrafish models. [Pink: ligand for target protein AR ligand-33; Black: linker; Blue: ligand for E3 ligase Cereblon]

AR ligand-38 is a ligand for the androgen receptor (androgen receptor) and can be utilized in the synthesis of PROTAC AR Degrader-9.