ahr antagonist 5

AHR antagonist 5 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist(example 39; IC50 < 0.5 μΜ). It significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1.

AHR antagonist 5 free base is an orally active antagonist of AHR with IC50s of ~35-150 nM in human and rodent cell lines.

AHR antagonist 5 hemimaleate is a potent antagonist (IC50 < 0.5 μM) of the orally active aryl hydrocarbon receptor (AHR). aHR antagonist 5 hemimaleate in combination with the detection site inhibitor anti-PD-1 exhibited inhibitory effects on tumor growth.

Adenosine receptor A1 antagonist 5 acts as an adenosine antagonist, is an oxypurine, acts as an insecticide and pest control agent, and has an inhibitory effect on elevated blood pressure.

CCR2 antagonist 5 (JNJ-41443532) is a selective and orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM).JNJ-41443532 binds mCCR2 with a Ki of 9.6 µM, which can be used to study inflammatory diseases and diabetes. diseases and diabetes.

5-HT6/7 antagonist 1 is a dual 5-HT6/7/2A and D2 receptor antagonist for the study of dementia and Alzheimer's disease.

5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist. It binds to 5-HT3 receptors in rat brain cortical membranes (Ki: 0.25 nM).

5-HT2 antagonist 1 is a potent 5-HT2 receptor antagonist, has weak α1 adrenoceptor blocking activity.

5-HT2A antagonist 1 is a 5-HT2A antagonist. It may be useful in the treatment of gastrointestinal disorders circulatory disorders.

AHR antagonist 2 is an antagonist of the aryl hydrocarbon receptor. The IC50s for human AHR and mouse AHR are 0.885 and 2.03 nM, respectively.

AHR antagonist 4 is a potent aryl hydrocarbon receptor (AHR) antagonist(example 293; IC50: 82.2 nM).It has anti-cancer effects.

5-HT4 antagonist 1 is an antagonist of 5-HT4 (pKi = 9.6).

MrgprX2 antagonist-5, which acts as a potent antagonist of MrgprX2. It exhibits the ability to effectively inhibit the activity of MrgprX2, making it an ideal candidate for research related to inflammatory skin disorders.

Compound 29 is a 5-HT6R antagonist that acts by inhibiting the 5-HT6 receptor.

AHR antagonist 7 (compound 4j), a selective aryl hydrocarbon receptor (AhR) antagonist with high affinity, demonstrates a dissociation constant (K i) of 1.4 nM [1].

5-HT7R antagonist 1 (free base) is a G protein-biased antagonist for the 5-HT 7 R receptor, with a dissociation constant (K i) of 6.5 nM.

5-HT3 antagonist 2 is an antagonist of 5-HT3 receptor.

5-HT1A antagonist 1 (compound 6f) is a potent and selective 5-HT1Areceptor antagonist (Ki: 35 nM). 5-HT1A antagonist 1 can be used in the study of central nervous system disorders.

A1AR antagonist 5 (compound 20) is a potent and selective antagonist of A1 adenosine receptor (A1AR) with a pKi of 6.11 and a pIC 50 of 5.83 [1].

CXCR2 antagonist 5 (compound 25) is a potent CXCR2 antagonist. CXCR2 antagonist 5 shows potent CXCR2 binding affinity ( IC 50 =0.013 μM) and calcium mobilization ( IC 50 =0.1 μM) [ 1].

Estrogen receptor antagonist 5 is a potent antagonist of the Estrogen receptor. Estrogen receptor (Estrogen receptor) is a ligand-activated transcriptional regulatory protein that interacts with endogenous estrogens and mediates the induction of a variety of biological effects. estrogen receptor antagonist 5 has potential for metastatic disease studies.

5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound which is a 5-HT 3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT 3 agonist and 2-methyl-5-HT, and exhibits anti-depressant effect in mice [1].

5-HT2B antagonist-1 is an orally active 5-HT2B receptor antagonist with an IC 50 of 33.4 nM. It can be used in studies of diseases characterized by 5-HT2B receptor signaling, such as hepatocellular carcinoma, cardiovascular disease or gastrointestinal disease [1] [2].

5-HT7R antagonist 1 is a G protein-biased antagonist with Ki of 6.5 nM for 5-HT 7R.

NMDA receptor antagonist 5 (Compound 10e), a potent and non-toxic NMDA receptor antagonist, exhibits brain permeability. It is of significance in studying neurological disorders [1].

Sigma-1 receptor antagonist 5 (compound 12), a 4-pyridylpiperidine derivative, exhibits analgesic properties through its antagonistic action on sigma receptors (Ki=4.5 nM (σ1R), 10 nM (σ2R)) and the histamine H3 receptor (hH3R, Ki=7.7 nM, IC50=215 nM). It effectively attenuates Capsaicin-induced nociception and demonstrates significant antinociceptive effects in both nociceptive and neuropathic pain models [1].

5-HT6/5-HT2AR antagonist-1 is a powerful and effective compound that acts as a dual antagonist for both the 5-HT6 and 5-HT2A receptors. It exhibits high potency with K i values of 11 nM and 39 nM for the respective receptors [1].

Androgen receptor antagonist 5 is a potent antagonist of the androgen receptor (AR) (IC50: 6.17 μM). Androgen receptor antagonist 5 inhibited the proliferation of prostate cancer cells LNCaP and showed antitumor effect in LNCaP xenograft mice model, which can be used to study prostate cancer.

5-HT3 antagonist 1 is a potent and selective antagonist of 5-HT3 receptor.

Compound 8 (5-HT6R antagonist 1), a 5-HT6R antagonist (K i : 5 nM), not only demonstrates inhibition of platelet aggregation and excellent metabolic stability but also reverses MK-801-induced memory impairments in rats, suggesting its utility in Alzheimer's disease (AD) research [1].

CXCR4 antagonist 5 (compound 23), a potent CXCR4 antagonist, exhibits high inhibition efficacy against CXCR4 with an IC50 value of 8.8 nM. It effectively suppresses CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and hinders CXCR4/CXCL12-mediated chemotaxis. Moreover, Compound 23 demonstrates favorable physicochemical properties and in vitro safety profiles, exhibiting only marginal to moderate inhibition of CYP isozymes and hERG [1].

Mu opioid receptor antagonist 5 (compound NAP) is a selective mu opioid receptor (MOR) antagonist that crosses the blood-brain barrier (EC50: 1.14 nM, Ki: 0.37 nM). Mu opioid receptor antagonist 5 can be used to study opioid use disorder (OUD).

AHR-16303B oxalate is a novel antagonist of 5-HT2 receptors.

CHD-5 is a selective antagonist of the aryl hydrocarbon receptor (AhR).

Kynurenic acid, an active metabolite of tryptophan, is synthesized through a kynurenine intermediate by kynurenine aminotransferases (KATs). It acts as an antagonist of both NMDA and AMPA receptors, as well as α7 nicotinic acetylcholine receptors (nAChRs; EC50s = 235, 101, and 7 µM, respectively), and functions as an agonist for the aryl hydrocarbon receptor (AhR) and G protein-coupled receptor 35 (GPR35; EC50s = 1.4 and 39 µM, respectively). In a neonatal rat model of cerebral hypoxic-ischemia, induced by carotid artery ligation, administration of kynurenic acid at 300 mg/kg prevents weight loss in the lesioned hemisphere. Additionally, at concentrations of 1 and 5 mg/ml, it protects against neurodegeneration in the rhabdomere of the eye in an Htt93QtransgenicDrosophila model of Huntington's disease. Elevated levels of kynurenic acid in the cerebrospinal fluid have been observed in patients with schizophrenia.