receptor-related

S18-000003 is an effective orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t inhibitor (IC50: 29 nM). S18-000003 inhibits IL-17 production.

Mps1-IN-1 is a potent, selective, and ATP-competitive inhibitor of Mps1 kinase (IC50: 367 nM).

Mps1-IN-1 dihydrochloride, a potent ATP-competitive inhibitor of Mps1 kinase, exhibits an IC50 of 367 nM. It effectively inhibits the activity of Mps1 mitotic kinase and disrupts spindle assembly checkpoint (SAC) function, thereby reducing the viability of both cancerous and 'normal' cells.

The compound 4A7C-301-Nurr1 agonist is a specific agonist for the nuclear receptor-related 1 (Nurr1). By binding to the Nurr1 ligand-binding domain with an IC50 value of 48.22 nM, it enhances the transcriptional activity of both Nurr1-LBD and the full-length Nurr1, as demonstrated in reporter assays using SK-N-BE(2)C human neuroblastoma cells, with EC50 values of 6.53 and 50-70 µM, respectively. Additionally, administration of 4A7C-301-Nurr1 agonist at a dosage of 5 mg/kg per day has been shown to mitigate dopaminergic cell death in the striatum and substantia nigra pars compacta and ameliorate motor and olfactory deficits in mouse models of Parkinson's disease, circumventing the induction of dyskinesia-like behaviors. These models were induced either by the neurotoxin MPTP or by overexpression of α-synuclein.

A2B receptor antagonist 1 is a small molecule antagonist and an A2B adenosine receptor antagonist with potent antagonistic activity, and can be used for research on adenosine receptor-related diseases.

48740 RP (RP 55779, (Rac)-RP-55778) belongs to synthetic compounds and is a platelet-activating factor (PAF) receptor antagonist with anti-inflammatory activity. This compound can be used in inflammation-related research, exerting its pharmacological effects through inhibition of the PAF/PAFR signaling pathway.

Oxidopamine hydrobromide (6-OHDA hydrobromide) is a widely used neurotoxin and an antagonist of the neurotransmitter dopamine. It selectively destroys dopaminergic neurons, promotes COX-2 activation, induces PGE2 synthesis, and stimulates the secretion of the pro-inflammatory cytokine IL-1β. It is commonly used to establish animal models of Parkinson’s disease (PD).

5-HT2 antagonist 1 is a small molecule antagonist functioning as a 5-HT2B receptor antagonist (IC50 = 33.4 nM), with oral bioactivity and weak inhibition of α1 receptors, employed in research on hepatocellular carcinoma and related diseases.

ZT 52656A hydrochloride belongs to synthetic small molecule compounds and is a highly selective kappa opioid receptor (KOR) agonist with good receptor selectivity and potential peripheral action characteristics. This compound effectively prevents or significantly alleviates ocular pain through KOR activation, and can be used in pain-related mechanism research.

Deucravacitinib is a highly selective, orally bioavailable, allosteric TYK2 inhibitor for the treatment of autoimmune diseases. It blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain, inhibiting IL-12/23 and type I IFN pathways. It selectively binds to the TYK2 pseudokinase (JH2) domain with an IC50 of 1.0 nM.

Meclinertant (SR 48692) is a small-molecule compound and a neurotensin receptor-1 (NTSR1) antagonist with good selectivity and cell permeability. This compound can be used to study neurotensin signaling pathways and related neurological diseases, and serves as a potential diagnostic and therapeutic probe targeting NTSR1-positive tumors.

Rimegepant (BMS 927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki value of 0.027 nM.

GW3965 hydrochloride (GW3965 HCl) belongs to synthetic small molecules and is a liver X receptor (LXR) agonist (hLXRα EC50 = 190 nM; hLXRβ EC50 = 30 nM) with subtype selectivity, cell permeability, and oral activity. This compound is used in research related to metabolism, inflammation, and neuropathic pain.

Pancreatic Polypeptide, rat acetate is a natural product and an NPY receptor agonist with high affinity for NPYR4 and receptor selectivity, commonly used in experimental models studying energy balance, feeding behavior, and related metabolic diseases.

Resatorvid (TAK-242), a selective Toll-like receptor 4 (TLR4) inhibitor, binds directly to Cys747 to prevent TLR4-TIRAP interaction, thereby blocking downstream signaling. Resatorvid exhibits antitumor, anti-inflammatory, and neuroprotective activities.

Cyclodrine hydrochloride is a dual cholinergic muscarinic receptor (mAChR) and nicotinic receptor (nAChR) antagonist that can be used in the study of neurologically related diseases.

Elubrixin (SB-656933) inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation. Elubrixin is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist.

ERRα antagonist-1 (ERR+/- antagonist-1) is a high-affinity, selective antagonist of the estrogen-related receptor α (ERRα). It effectively prevents the interaction of ERRα with both Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, displaying IC50 values of 170 nM and 180 nM, respectively. Notably, ERRα antagonist-1 does not interfere with the interactions involving ERRβ or ERRγ and the PGC-1α and PGC-1β coactivators. Furthermore, it does not affect the interaction between either ERα or ERβ and PGC-1α or SRC-1.

CCK-A receptor inhibitor 1 is a potent cholecystokinin A (CCK-A) receptor inhibitor (IC50: 340 nM) and can be used to study digestive system-related diseases.

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

Sulamserod (RS 100302) is a potent 5-HT4 receptor antagonist with antiarrhythmic activity for the study of atrial fibrillation and cardiovascular related diseases.

(±)-WS75624B is a potent ECE inhibitor (IC50:0.03 μg/mL), a serotonin receptor agonist.This compound is unstable in powder form and other related salt forms are recommended.

AZD-0284 is an inverse agonist of the nuclear receptor RORγ. In development for the treatment of plaque psoriasis vulgaris and respiratory tract disorders[1].

MK-0773 FA (MK-0773 FA (606101-58-0 Free base)) is a selective androgen receptor modulator with an IC50 value of 6.6 nM for AR, which can be used for the prevention and treatment of cancer-related muscle wasting.