receptor-related

Deucravacitinib (BMS-986165) 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.

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

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.

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.

RWJ-51204 is a selective adenosine A2A receptor antagonist and a partial agonist of GABA(A) receptor (IC50: 0.2-2 nM). It has neuroprotective and movement-improving effects and can be used in research related to Parkinson's disease.

NO-prednisolone (NCX-1015) is a compound that effectively stimulates the production of IL-10 in vivo. It is a Prednisolone derivative that releases nitric oxide (NO).

YE 120 is a highly potent GPR35 agonist (EC50: 32.5 nM) with potential anti-inflammatory and anti-cancer activities, which can be used to study G protein-coupled receptor-related diseases.

Itasetron (U 98079A) is a 5-hydroxytryptamine 3-receptor antagonist used to prevent age-related memory deficits in rats.Itasetron's antiemetic activity in animal models of cancer chemotherapy and radiation therapy may be useful in the study of amnesia.

Cilansetron is an effective and selective 5-HT3 receptor antagonist that can be used for related diseases caused by colitis.

N-5984, a β3-adrenergic receptor agonist, is used potentially for the treatment of obesity, overactive bladder and type 2 diabetes.

ML-209 is an antagonist of retinoic acid receptor-related orphan receptor γt (RORγt; IC50= 1.1 μM in a reporter assay).1It inhibits RORγt-induced transcription in HEK293T cells expressing the human receptor (IC50= 300 nM). ML-209 inhibits RORγt-dependent differentiation of isolated na?ve cord blood human CD4+T cells into Th17 T helper cells.

TREM2 agonist-1 (I-246) is a triggering receptor expressed on myeloid cells-2 (TREM2) agonist with an EC50 ranging from 3.0 μM to 100 μM.

mTOR HDAC-IN-1 (Compound 50) is a dual inhibitor of mTOR and HDAC, with IC50 values of 0.49 nM and 0.91 nM, respectively, holding potential as an anti-cancer agent [1].

ONO-8713 is a selective prostaglandin E receptor subtype EP1 antagonist used to study diseases of the biblical system and metabolism-related diseases.

Nemazoline Free Base acts as an α1-adrenergic agonist and an α2-adrenergic antagonist, and may be used in the treatment of trace amine-associated receptor-related disorders.

IRAK inhibitor 2 (IRAK-IN-2) is a potent inhibitor of interleukin 1 receptor-associated kinase 4 (IRAK-4) for the study of inflammation-related diseases.

KSK68 is a potent dual sigma-1 and histamine H3 receptor antagonist with potential analgesic activity and high affinity for H3 receptors, sigma-1, sigma-2 receptors.KSK68 can be used in the study of pain related diseases.