Endocrinology/Hormones

NPFF1-R antagonist 1 (compound 8b) is a piperidine analog and an effective neuropeptide FF (NPFF) receptor antagonist. It exhibits 15-fold selectivity for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively.

VinclozolinM2-2204 is an androgen receptor AUTOTAC degrader with a DC50 of 200 nM in LNCaP prostate cancer cells. It induces the formation of AR+LC3+ autophagic membranes and is applicable for cancer research.

DP50 is a bifunctional compound containing both an opioid receptor agonist (MOP) and a neuropeptide FF receptor (NPFFR) antagonist. It can be utilized in studies related to analgesia.

PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist that activates the G protein signaling pathway with an EC50 of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). Additionally, PIPE-3297 promotes myelination and has anti-inflammatory properties.

OX04528 is an orally active and potent GPR84 biased agonist.OX04528 inhibits cAMP signaling and may be useful in cancer research.

CTOP acetate is a somatostatin analogue and a μ-opioid receptor antagonist.

(1S,2R)-2-PCCA is a novel and potent small molecule GPR88 receptor agonist with an EC50 value of 3 nM in the non-cellular system and 603 nM in the cellular

Awl 60 is a substance P (6-11) non-competitive antagonist.

GLL 398 is an orally active and selective degrader of estrogen receptor with an IC50 of 1.14 nM. GLL 398 blocks tumor growth in xenograft breast cancer models.

BMS-903452: potent GPR119 agonist, EC50 = 14 nM, treats rodent diabetes, no P450 inhibition, safe for liver cells.

Piperidylthiambutene hydrochloride is an opioid compound that exhibits analgesic effects in animal models.

Nociceptin (1-13), amide is a potent ORL1 (OP4) receptor agonist with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain

Alunacedase alfa (APN-01) is an angiotensin-converting enzyme 2 with antiviral activity.

non-peptide δ1 opioid receptor agonist

Ethamoxytriphetol is a non-steroidal estrogen antagonist.

Bradykinin potentiator-5 is a peptide inflammatory mediator, causes blood vessels to dilate (enlarge), and therefore causes blood pressure to fall.

DBPR116 is a prodrug of BPRMU191 that can penetrate the blood-brain barrier. It significantly enhances the delivery efficiency of drugs targeting the central nervous system. When combined with the antagonist Naltrexone, DBPR116 demonstrates superior safety and analgesic effects compared to morphine in various in vivo pharmacological studies, including thermal pain models, cancer pain models, constipation, sedation, psychological dependence, heart rate, and respiratory frequency. As a strategy for peripheral administration, DBPR116 effectively alleviates pain while reducing adverse effects, showing promise as a safer opioid analgesic.

PU-WS13 hydrobromide is a GRP94 inhibitor with anti-inflammatory activity and inhibits the proliferation of M2-like macrophages in mouse TNBC tumors.