roundabout, axon guidance receptor, homolog 4

Protease-Activated Receptor-4 diTFA,2454 is the proteinase-activated receptor-4 (PAR4)agonist

RXFP1 receptor agonist-4 (Example 268) is an agonist for the RXFP1 receptor, demonstrated to suppress cAMP production in HEK293 cells that stably express the human RXFP1 receptor, exhibiting an effective concentration (EC50) of 4.9 nM [1].

Compound 14a (P2X7 receptor antagonist-4) is a P2X7R antagonist with IC50 values of 64.7 nM in humans and 10.1 nM in mice. It inhibits the activation of the NLRP3 inflammasome, which subsequently reduces the expression of caspase-1, gasdermin D, IL-1β, and IL-18 in the kidneys of mice with sepsis-induced damage [1].

TGR5 Receptor Agonist 4, a selective agonist for the Bile Acid Receptor (TGR5), exhibits potent activity with an EC50 of 2 nM for human TGR5 (hTGR5) and 3 nM for mouse TGR5 (mTGR5). It is notably involved in mediating hypoglycemic and weight loss effects [1].

GLP-1 receptor agonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist , has an EC50 of 64.5 nM. GLP-1 receptor agonist 4 can be used in the research for treatment of diabetes.

APJ Receptor Agonist 4 is a potent, orally active apelin receptor (APJ) agonist, demonstrating an EC50 of 0.06 nM and a Ki of 0.07 nM. It exhibits excellent pharmacokinetic profiles in rodent heart failure (HF) models and has shown an acceptable safety profile in preclinical toxicology studies. This compound effectively improves cardiac function, making it valuable for research into HF disease.

Adenosine receptor antagonist 4 is an adenosine receptor antagonist.

Estrogen Receptor Antagonist 4 is a potent inhibitor of the estrogen receptor (ER), crucial for regulating cell growth, differentiation, and apoptosis. This compound holds promise for cancer research[1].

Protease-Activated Receptor-4 is the proteinase-activated receptor-4 (PAR4) agonist, with Antiplatelet Therapy

NMDA receptor antagonist 4 (IIc) is an uncompetitive, voltage-dependent, orally active NMDAR blocker, with an IC 50 of 1.93 μM. NMDA receptor antagonist 4 shows a positive predicted blood-brain-barrier (BBB) permeability, and can be used in Alzheimer's disease research[1].

GABAA receptor agent 4 (compound 1e) is a potent antagonist of γ-GABAAR with Ki of 0.18 µM. GABAA receptor agent 4 has immunomodulatory potential which was shown to efficiently rescue the inhibition of T cell proliferation [1].

Orexin receptor antagonist 4 is potent and selective orexin 2 receptor (OX2R) antagonist. Orexin receptor antagonist 4 shows IC50 of 4.27 nM and 295 nM for OX2R and OX1R, respectively.

AMPA Receptor Modulator-4, a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (BTD), serves as an orally active positive allosteric modulator of the AMPA receptors (AMPAR PAMs). This compound is capable of crossing the blood-brain barrier and has been found to enhance cognitive performance and working memory in mice [1].

Mu opioid receptor antagonist 4 (compound 31) is a potent and selective mu opioid receptor (MOR) antagonist that permeates the blood-brain barrier (Ki: 0.38 nM, EC50: 0.38 nM). Mu opioid receptor antagonist 2 can be used to study opioid use disorder (OUD).

NMDA receptor modulator 4 (Compound 169) can be used for the research of neurological disorder that is a potent modulator of NMDA receptor [1].

EP4 receptor antagonist 4 is an agonist of EP4 receptor (human pEC 50 = 6.3) [1].

Androgen receptor antagonist 4 (Compound AT2) has anticancer activities. Androgen receptor antagonist 4 potently antagonizes the activity of AR transcriptional, inhibits downstream target gene of AR, and blocks the DHT-induced nuclear translocation of AR. Androgen receptor antagonist 4 is an antagonist of androgen receptor (AR) (IC 50 = 0.15 μM) [1].

EP2 receptor agonist 4 selectively activates the EP2 receptor with an efficacy concentration (EC50) of 43 nM [1].

Sigma-1 receptor antagonist 4 (Compound 32) is a potent σ1R antagonist that significantly enhances morphine's analgesic effects and reverses morphine-induced analgesic tolerance, potentially preventing morphine tolerance [1].