Endocrinología / Hormonas

Neuropeptide AF (93-110), Human is an endogenous antiopioid peptide.

Antiproliferative agent-51 (Compound 18h) inhibits estrogen receptor α (ERα)-mediated transcription with an IC50 of 1.6 nM. It also suppresses the proliferation of cancer cells ZR-75, with an IC50 of 0.031 μM, and exhibits antitumor activity in mouse models.

3-Cl-Pyridine-amide-acrylaldehyde-piperazine serves as a synthetic intermediate for LO-4-25. LO-4-25 is a ligand for the androgen receptor (AR) DNA binding domain and is linked to a truncated fumaramide handle via a connector. In 22Rv1 cells, LO-4-25 demonstrates potent degradation of both AR and AR-V7.

Chymase is a proteolytic enzyme predominantly found in mast cells (MC), fibroblasts, and vascular endothelial cells. It is released into the extracellular matrix in response to inflammatory signals, tissue damage, and cellular stress. Chymase also plays a role in the generation of angiotensin II (Ang II), making it significant for cardiovascular disease research.

Termitomycamide B, a fatty acid from T. titanicus, protects Neuro2a cells from ER stress-induced death at 0.1 μg/ml.

Antihypertensive agent 2 (Compound 4g) exhibits effective antagonistic activities against angiotensin II receptor 1 and reduces blood pressure with equal or

Potent μ opioid antagonist, IC50 3.5 nM, 1200x selectivity over δ and somatostatin, brain-penetrant, active in vivo.

β-Chlornaltrexamine dihydrochloride (β-CNA dihydrochloride) is an effective long-term antagonist of opioid receptors. It efficiently blocks the inhibition of dopamine release mediated by κ opioid receptor agonists. This compound is useful in the research of pain perception mechanisms.

Ota-vasotocin is a ligand utilized in quantitative receptor autoradiography for oxytocin receptors.

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.

R4K1 is a cell-permeable stapled peptide that binds with high affinity to estrogen receptor (ER) α, inhibiting its interaction with coactivators. It penetrates breast cancer cells, regulating gene transcription and suppressing cell proliferation. R4K1 is applicable for tumor research.

SL910102 is a nonpeptide angiotensin antagonist of the AT1 receptor.

TRV055: Gq-biased AT1R ligand, stimulates Gq signaling, aids Gq-biased agonist development.

TLB 150 Benzoate (RAD150) is a modulator of the androgen receptor with an IC50 value of 0.13 μM.

[Asp5]-Oxytocin is the first 5-position neurohypophyseal hormone analogue possessing significant biological activity.

ERα/ERβ antagonist-1 (Compound 10) functions as a partial antagonist of both ERα and ERβ. It reduces the activity of ERα and ERβ in HepG2 liver cells in a dose-dependent manner.

β-Naltrexamine dihydrochloride is an orally administered, irreversible opioid receptor antagonist. Its derivatives exhibit optimised subtype selectivity and can be used for pain research.

Morphiceptin is a synthetic tetrapeptide with morphinelike activities, highly specific for morphine receptors, but not for enkephalin receptors.

Potent μ-receptor antagonist, Ki=0.96nM, ineffective at δ (>10,000nM). Alters behavior in vivo, boosts K+ currents in rat neurons in vitro, μ-independent.

4,4'-(Cyclohexylidenemethylene)diphenol (Compound 2) is a symmetrical cyclic non-steroidal estrogen. It exhibits high binding affinity to estrogen receptors ERα and ERβ.