Catalog No.
Product Name
Application
Product Information
Citations
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GPR40 activator
GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1. -
GPR88 receptor agonist
(1R,2R)-2-PCCA hydrochloride is a diastereomer of 2-PCCA, and acts as a potent GPR88 receptor agonist, with an EC50 of 3 nM in cell-free assay, and 603 nM in cell assay. -
SARD ligand
(R)-UT-155 (compound 11) is a selective androgen receptor degrader (SARD) ligand. Less active than the S-isomer. -
estrogen receptor (ERα) antagonist
AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD). -
thyroid hormone receptor agonist
Eprotirome is a liver-selective thyroid hormone receptor agonist. -
GPR40 agonist
AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. -
progesterone receptor agonist
Nomegestrol acetate is a potent, highly selective progestogen, which is characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors. -
oestrogen receptor antagonist
Enclomiphene citrate is a potent and orally active oestrogen receptor antagonist, with antioestrogenic property. -
D prostanoid receptor 2 antagonist
Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. -
direct renin inhibitor
Aliskiren D6 Hydrochloride (CGP 60536 D6 Hydrochloride) is is deuterium labeled Aliskiren, which is a direct renin inhibitor with IC50 of 1.5 nM. -
glucocorticoid receptor agonist
Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist. -
estrogen receptor (ER) inhibitor
WAY-169916 is a pathway-selective inhibitor of estrogen receptor (ER) that acts by inhibiting NF-kB transcriptional activity. -
antiestrogenic properties
FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus. -
cell permeable TgPrxII inhibitor
Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII). -
ERRα agonist
Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist. -
5α-reductase inhibitor
Finasteride Carboxaldehyde is a metabolite of Finasteride in human bile (M2 metabolite) that can be used for proteomics research. -
Antiandrogenic agent
4'-Methoxyresveratrol (4'-O-Methylresveratrol) is a polyphenol derived from Dipterocarpaceae, with antiandrogenic, antifungal and anti-inflammatory activities. -
synthetic glucocorticoid receptor agonist
Methylprednisolone (NSC-19987, Medrol) acetate is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. -
GPR109A agonist
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. -
Estrogen receptor degrader
SAR439859 is an orally available, nonsteroidal selective estrogen receptor degrader/downregulator (SERD). -
Androgen receptor antagonist
TRC253, also known as JNJ63576253, is a potent and orally active androgen receptor antagonist. -
GnRH peptide agonist
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. -
GnRH receptor antagonist
Cetrorelix diacetate (SB-075 diacetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM. - (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.
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GnRH Receptor agonist
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. -
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.
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PROTAC
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. - 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.
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THR-β agonist
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). -
GPR35 agonist
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. -
GPR55 antagonist
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. -
GPR35 agonist
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
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. -
PROTAC AR degrader
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.
