Endocrinology-Hormones

Methylprednisolone (NSC-19987, Medrol) acetate is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation.

Monomethyl fumarate, an active metabolite of Dimethyl fumarate (DMF), is a potent GPR109A agonist. Monomethyl fumarate has the potential for multiple neuroprotective pathways and other models of retinal disease.

SAR439859 is an orally available, nonsteroidal selective estrogen receptor degrader/downregulator (SERD).

TRC253, also known as JNJ63576253, is a potent and orally active androgen receptor antagonist.

TMP778 is a novel, potent, and selective RORγt inverse agonist.

ML 193 is a selective GPR55 antagonist (IC50 = 221 nM). Exhibits >27-, >145- and >145-fold selectivity for GPR55 over CB1, GPR35 and CB2, respectively. Inhibits ERK signaling in vitro.

Triptorelin is a synthetic gonadotropin-releasing hormone (GnRH) peptide agonist that binds to the GnRH receptor. It inhibits the growth of DU145, LNCaP, and PC3 prostate and OVCAR-3 ovarian cancer cells.

Cetrorelix diacetate (SB-075 diacetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM.

QCC-374 is prostanoid agonist potentially for the treatment of pulmonary arterial hypertension.

BAM(8-22), a proteolytically cleaved product of proenkephalin A, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1, and induces scratching in mice in an Mrgpr-dependent manner.

(D-Trp12,Tyr34)-pTH (7-34) amide (bovine) is a potent and competitive antagonist of parathyroid hormone (PTH), with a Ki of 69 nM in bovine renal cortical membrane. (D-Trp12,Tyr34)-pTH (7-34) amide (bovine) can be used for growth and development regulation.

ELA-21 (human) is an apelin receptor agonist with a pKi of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways.

(Glu2)-TRH, a metabolically stable analogue of Thyrotropin-releasing hormone (TRH), is a negative modulator for the cholinergic effect of TRH in the mouse brain. (Glu2)-TRH significantly attenuates TRH-induced hippocampal extracellular acetylcholine release. (Glu2)-TRH is not metabolized by thyroliberinase. (Glu2)-TRH manifests neuroprotective, antidepressant, anticonvulsant in the CNS.

Histrelin acetate, a GnRH analogue, is a GnRH Receptor agonist. Histrelin acetate increases serum luteinising hormone (LH), follicle stimulating hormone (FSH) and testosterone levels. Histrelin acetate can be used in the research of prostate cancer, endometriosis.

LHRH, the luteinizing hormone-releasing hormone, is a neuropeptide hypothalamic. LHRH regulates reproduction. LHRH can be used for the research of cancer.

SLU-PP-332 is a pan-Estrogen Receptor/ERR agonist with EC50 values of 98, 230 and 430 nM for ERRα, ERRβ and ERRγ, respectively. SLUPP-332 enhances mitochondrial function and cellular respiration in skeletal muscle cell lines. SLU-PP-332 has the potential to study metabolic diseases as well as improve muscle function.

Luxdegalutamide (ARV-766) is an orally active proteolysis-targeting chimera (PROTAC) designed to selectively degrade the androgen receptor (AR), including clinically relevant resistance-associated mutants such as T878A, H875Y, and L702H. By inducing AR ubiquitination and proteasomal degradation, Luxdegalutamide effectively suppresses AR signaling and exhibits potent antitumor activity. It is a promising therapeutic agent and research tool for studying castration-resistant prostate cancer (CRPC) and mechanisms of AR-driven oncogenesis.

ARD-2585 is an exceptionally potent, orally active PROTAC degrader of the androgen receptor (AR), designed to selectively and efficiently induce AR degradation for potential therapeutic applications.

Prednisolone hemisuccinate is a synthetic glucocorticoid derivative of cortisol, commonly used in the treatment of inflammatory and autoimmune disorders. It exerts anti-inflammatory and immunosuppressive effects by modulating gene expression through glucocorticoid receptor activation.

ALG-055009 is a selective thyroid hormone receptor β (THR-β) agonist with an EC50 of 0.063 μM. It effectively reduces total cholesterol levels in high-fat diet-induced rat models and is a promising compound for research related to metabolic dysfunction-associated fatty liver disease (MAFLD).

Pamoic acid disodium is a potent agonist of GPR35, with an EC50 of 79 nM. It induces GPR35 internalization and activates ERK1/2 signaling with EC50 values of 22 nM and 65 nM, respectively. Additionally, it effectively recruits β-arrestin2 to GPR35 and exhibits antinociceptive properties, supporting its potential in pain research.

ML192 is a selective antagonist of G protein-coupled receptor 55 (GPR55), effectively inhibiting GPR55-mediated signaling pathways. It blocks β-arrestin trafficking, suppresses ERK1/2 phosphorylation, and prevents PKCβII translocation, thereby interfering with downstream cellular responses. ML192 is a valuable tool for studying the physiological and pathological roles of GPR55 in processes such as inflammation, pain, cancer, and metabolic regulation.

Pamoic acid (Embonic acid) is a potent agonist of G protein-coupled receptor 35 (GPR35), with an EC₅₀ of 79 nM. Activation of GPR35 by pamoic acid is associated with both neuroprotective and anti-inflammatory effects, making it a valuable compound for research into neurological disorders and inflammatory diseases. Its pharmacological profile suggests potential therapeutic applications in conditions where GPR35-mediated signaling plays a regulatory role.

PROTAC AR/AR-V7 Degrader-1 (27c) is a PROTAC-based dual degrader targeting both full-length androgen receptor (AR) and its splice variant AR-V7, which is implicated in resistance to androgen deprivation therapies. It exhibits DC₅₀ values of 2.67 μM for AR and 2.64 μM for AR-V7, effectively promoting their proteasomal degradation. By eliminating both isoforms, compound 27c induces apoptosis in AR-driven cancer cells, making it a promising therapeutic candidate for castration-resistant prostate cancer (CRPC) and other AR/AR-V7–dependent malignancies.

ARD-1676 is an orally bioavailable PROTAC degrader of the androgen receptor (AR), composed of an AR-binding ligand and a cereblon-recruiting moiety. It effectively induces AR degradation both in vitro and in vivo, and demonstrates significant antitumor activity by inhibiting VCaP prostate cancer xenograft growth in mouse models. ARD-1676 represents a promising therapeutic strategy for targeting AR-driven malignancies.