androgen receptor antagonist 5

Androgen receptor antagonist 5 is a potent antagonist of the androgen receptor (AR) (IC50: 6.17 μM). Androgen receptor antagonist 5 inhibited the proliferation of prostate cancer cells LNCaP and showed antitumor effect in LNCaP xenograft mice model, which can be used to study prostate cancer.

ID11916 is an orally active compound functioning as both an androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. It disrupts androgen binding to AR, impedes nuclear translocation, and blocks androgen-dependent transcriptional activity of AR, while simultaneously elevating intracellular cGMP levels by inhibiting PKG activation. Moreover, ID11916 exhibits potent anticancer effects in prostate cancer cell lines VCaP and 22Rv1, as well as in AR-positive breast cancer cell line SK-BR-3.

AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension when administered prior to induction or after establishment of hypertension.2 1.Cárdenas, S., Colombero, C., Panelo, L., et al.GPR75 receptor mediates 20-HETE-signaling and metastatic features of androgen-insensitive prostate cancer cellsBiochim. Biophys. Acta Mol. Cell Biol. Lipids1865(2)158573(2020) 2.Sedláková, L., Kikerlová, S., Husková, Z., et al.20-Hydroxyeicosatetraenoic acid antagonist attenuates the development of malignant hypertension and reverses it once established: a study in Cyp1a1-Ren-2 transgenic ratsBiosci. Rep.38(5)BSR20171496(2018)

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ～6 μM and a selective PPAR-gamma modulator.

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].

Compound 30a, known as AR Antagonist 5, is a selective androgen receptor (AR) antagonist that demonstrates an IC 50 value of 134.8 nM. It exhibits favorable pharmacokinetic properties, characterized by high skin exposure and low plasma exposure [1].

EPI-001 (Standard) is the standard substance of EPI-001, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ～6 μM and a selective PPAR-gamma modulator.