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.

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.

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 125487 sulfamate is a 5-HT4 receptor antagonist.

5-HT1B/1D receptor antagonist

platelet fibrinogen receptor glycoprotein IIb/IIIa (GpIIb/IIIa) antagonist

GR 46611 is a selective 5-HT1B and 5-HT1D receptor agonist and can be used in studies about the treatment of epilepsy.

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 100679 is an antagonist of NK2 receptor.

GR 83895 is an antagonist of prototype fibrinogen receptor.

GR 128107 is an antagonist of melatonin receptor.

GR 196429, a melatonin receptor agonist, exhibits selectivity for the MT1 subtype. This compound not only promotes sleep and alters circadian rhythms but also stimulates melatonin release in mice.

GR 218,231 is a selective antagonist of D3 dopamine receptor.

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