GPCR/G-Protéine

COX-2-IN-6: Potent, selective COX-2 inhibitor; oral; IC50 0.84μM, Ki 69nM; blocks PGE2 synthesis; prevents colorectal cancer.

GRPR antagonist-2 blocks GRPR, kills some cancer cells, effective on HGC-27 (IC50: 0.77 μM) & Pan02 (IC50: 2.5 μM).

Fosrolapitant is an antagonist of the neurokinin 1 (NK1) receptor.

Nocloprost (SH 475) is a prostaglandin E2 (PGE2) analog, an EP1 and EP3 receptor agonist with local gastric protection and ulcer healing effects.

OX2R agonist 1 is an OX2R activator with an EC50 of less than 100 nM. It is utilized in research related to narcolepsy and cataplexy.

ONO-8809: Thromboxane A2 antagonist, reduces airway hyperresponse, macrophage accumulation, and MMP-9 in SHRSP brains.

RS 61756-007 is a selective thromboxane receptor (TP) agonist.

KF26777 is a potent and selective antagonist of adenosine A3 receptor.

LB-102 is an orally active inhibitor of dopamine D2, D3, and serotonin 5-HT7 receptors, utilized in the study of schizophrenia and other psychiatric disorders.

Pentacosafluorotridecanoic Acid (PFTrDA) is a perfluoroalkyl substance (PFAS) that exhibits various biological impacts across different species. In zebrafish embryos, exposure to PFTrDA induces yolk sac edema and increases mRNA expression of thyroid hormone synthesis genes, including tshβ, at concentrations of 0.1 and 0.3 mg/L. At a dosage of 10 mg/kg, PFTrDA reduces serum testosterone and luteinizing hormone levels, as well as palmitic acid, linoleic acid, and oleic acid levels in the testicular interstitial cells of late adolescent rats. In humans, maternal plasma levels of PFTrDA during pregnancy are positively correlated with the development of eczema in female infants (but not male infants), and PFTrDA levels are higher in the livers of cancerous humans compared to non-cancerous ones. Additionally, PFTrDA is found in marine mammals.

Taranabant: potent CB1 receptor inverse agonist; inhibits agonists with 0.13 nM Ki in vitro.

ASN-1377642 is an NK1 receptor antagonist with a Ki value of 251 nM. It demonstrates antitumor activity in breast cancer cells with high expression of NK1R-Tr.

Diosuxentan is an inhibitor of ETA and is utilized in research pertaining to cardiovascular, renal, and neuronal inflammatory diseases.

GnRH antagonist 2 is a GnRH receptor antagonist, useful for studying endocrine diseases.

12(S)-HEPE, made from EPA by 12-LO, is an anti-inflammatory ω-3 derivative affecting leukotriene formation.

9-Methyl-β-carboline is a cognitive enhancer with neuroprotective, neurorestorative, and anti-inflammatory properties. Its behavioral effects may be linked to hippocampal dopamine levels and the stimulation of dendritic and synaptic proliferation.

BAY 38-7271: potent neuroprotective, selective CB1/CB2 agonist, Ki of 1.85 nM (CB1) & 5.96 nM (CB2).

PF-07258669 is a selective melanocortin 4 receptor (MC4) antagonist used in the study of cachexia and loss of appetite.

AZD5462 is a potent orally available relaxin receptor RXFP1 agonist for the study of heart failure and cancer.

Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist.Cost-effective and quality-assured.