gr

OP-3633 is an effective and selective steroidal glucocorticoid receptor (GR) antagonist (IC50: 29 nM). OP-3633 shows low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism. It also has an inhibition of GR transcriptional activity.

NXT629 is a selective and highly efficient PPAR-α antagonist with anticancer activity. It inhibits PPARδ, PPARγ, Erβ, GR, and TRβ and can be used in research on ovarian cancer and melanoma.

Exicorilant is a selective and oral active glucocorticoid receptor (GR) antagonist (Ki: 7 nM) and it also has the potential to overcome adiposity, glucose intolerance, and dyslipidemia.

GR-95168 ((+)-C-BVDU) is an antiviral compound for the study of herpes simplex virus infections type 1 and type 2.

GR 103691, a potent and selective dopamine D3 receptor antagonist (Ki: 0.4 nM), exhibits more than 100-fold selectivity for human dopamine D3 receptors over human D4 and D1 sites.

GR 113808 is a selective 5-HT4 receptor antagonist that inhibits 5-HT1B, 5-HT2A, 5-HT2C, and 5-HT3 receptors, and attenuates dopamine release.

GR148672X is an inhibitor of triacyglycerol hydrolase (TGH) (IC50: 4 nM).

GR-14-3-3 stabilizer-1 (compound 10) is a molecular glue stabilizer designed for the creation of a molecular adhesive that targets glucocorticoid receptors (GR), thereby inhibiting the interaction between GR and 14-3-3 proteins.

GR-28 is an inhibitor of the small C-terminal domain phosphatase 1 (SCP1). It suppresses the transcriptional activity of the repressor element 1-silencing transcription factor (REST) and inhibits the proliferation of glioblastoma cells, with IC50 values of 2.9 and 10.1 µM for cell lines A172 and T98G, respectively.

GR 55562 is a selective 5-HT1B receptor antagonist. It can be used for research into neurological disorders.

GR 125487 sulfamate is a 5-HT4 receptor antagonist.

5-HT1B/1D receptor antagonist

GR 144053 trihydrochloride is a potent and selective GPIIb/IIIa receptor antagonist (IC50 = 20 nM). It inhibits fibrinogen-mediated platelet aggregation, used for thrombosis and antiplatelet drug discovery research.

GR 55562 dihydrochloride is a selective serotonin 5-HT 1B antagonist with weak antagonistic activity against 5-HT 1D, and can be used for research on neurological diseases.

GR 89696 fumarate is a highly selective κ2 opioid receptor agonist (IC50 = 0.04nM) with anti-pruritchy, anti-injury and neuroprotective effects.

Potent and selective tachykinin NK2 receptor antagonist

GR 94800 acetate is a potent and selective neurokinin 2(NK-2) antagonist.

GR 122222X is an inhibitor of topoisomerase II.

GR-125487 is a 5-HT4R partial agonist. It also has favorable ADME properties and good in vivo efficacy.

GR203040 inhibits cyclophosphamide-induced damage in the rat and ferret bladder. GR-203040 is a selective NK1 receptor antagonist.

GR 83895 is an antagonist of prototype fibrinogen receptor.

GR 128107 is an antagonist of melatonin receptor.

GR-55562 dihydrobromide is a antagonist of 5-HT1B/5-HT1D serotonin receptor.

GR-112000 is a peptide-based tachykinin NK2 receptor antagonist.