ahr antagonist 2

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

A2B receptor antagonist 2 hydrochloride is an antagonist of adenosine receptor A2B (Ki = 2.30 μM for rA1, 6.8 μM for rA2A, 3.44 μM for hA2B).

AMPA receptor antagonist-2 is an AMPA receptor antagonist.

CRTh2 antagonist 2 is a selective and potent CRTH2 antagonist, IC50≤10 nM. CRTh2 antagonist 2 can be used to study the direction of androgenic alopecia.

TLR7/8/9 antagonist 2 is an orally active and highly bioavailable vTLR7/8/9 antagonist. TLR7/8/9 antagonist 2 inhibits HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC50s of 0.011 μM, 0.029 μM and 0,052 μM, respectively. TLR7/8/9 antagonist 2 can be used to study auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis.

Sigma-1 receptor antagonist 2 is a potent and selective antagonist of sigma 1 receptor (σ1 R) (σ1 and σ2 receptor with Kis of 3.88 and 1288 nM , respectively).

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

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

MrgprX2 antagonist-2 is a potent antagonist of MrgprX2. It holds potential for investigating skin inflammatory disorders.

CB1 antagonist 2 (AM4113) is caimabinoid 1 (CB1) antagonist which inhibits CB1 in vivo with an IC50 of 25.5 nM.

Compound 39, also known as CB2 receptor antagonist 2, is a potent CB2 antagonist exhibiting an IC50 of 0.33 μM. It engages in strong interactions with residues L17, W6.48, V6.51, and C7.42 [1].

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].

OT-R antagonist 2 is a nonpeptide low molecular weight antagonist of OT-R .

GPVI antagonist 2 (Compound 1) is a potential Glycoprotein VI (GPVI) antagonist, able to act on collagen (IC50: 0.35 μM), CRP (IC50: 0.80 μM), convulxin (IC50: 195.2 μM), thrombin (IC50. 81.38 μM). GPVI antagonist 2 is a promising anti-platelet agent.

ET Receptor Antagonist 2 (Compound 16j) is an orally active ET receptor antagonist with an IC50 of 0.22 nM, suitable for pulmonary arterial hypertension (PAH) research. It has been shown to mitigate monocrotaline-induced PAH in a rat model [1].

NOD1/2 Antagonist-1 is a potent dual inhibitor of nucleotide-binding oligomerization domain-like receptors 1 and 2 (NOD1/2), displaying inhibitory concentrations (IC50) of 1.13 μM for NOD1 and 0.77 μM for NOD2. It exhibits an acceptable half-life (T1/2) of 67.6 minutes. Additionally, NOD1/2 Antagonist-1 enhances the antitumor efficiency of Paclitaxel (PTX).

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

Protease-Activated Receptor-1 Antagonist 2 is an orally active antagonist of protease-activated receptor-1 (PAR-1), demonstrating significant potency with an IC 50 of 7 nM. It exhibits favorable pharmacokinetic characteristics, making it valuable in cardiovascular disease (CVD) research, including studies on atherosclerosis and restenosis [1].

Compound A-26, also known as FXR antagonist 2, is a diarylamide derivative that functions as a moderate FXR antagonist. It is utilized in researching hyperlipidemia and type 2 diabetes [1].

AT1R antagonist 2 is a potent AT1R selective ligand with good AT1R affinity (Ki: 26 nM).

EP2 receptor antagonist-2 (CID891729) is a compound that not only serves as an antagonist to the EP2 receptor, blocking its activation by PGE2, but also reduces lactate dehydrogenase (LDH) release triggered by N-methyl-D-aspartate (NMDA).

NMDA receptor antagonist 2 is a highly potent and orally active NR2B subtype-selective antagonist of the N-methyl-D-aspartate (NMDA) receptor. It exhibits remarkable binding affinities, with an IC50 of 1.0 nM and a Ki value of 0.88 nM. This compound finds valuable application in scientific investigations focusing on neuropathic pain and Parkinson’s disease.

CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunotherapy with an IC 50 value of 95 nM.

The compound is an a1/a3 adenosine receptor antagonist, which helps to treat (neurological) inflammatory diseases.

GRPR antagonist-2 is a potent antagonist of the gastrin-releasing peptide receptor (GRPR) and exhibits anticancer effects by being cytotoxic to certain cancer cells (able to act on HGC-27 cells (IC50: 0.77 μM) and Pan02 cells (IC50: 2.5 μM)).

Calcium Channel antagonist 2 is a calcium channel antagonist (IC50=5-20 μM) that can be used to study diseases due to Ca2+ channels like pain and diabetes.

ERRα antagonist-2 (Compound 11) is a potential Reverse agonist of ERR α (estrogen receptor related receptor α) (IC50=0.80 μ M). ERRα antagonist-2 can inhibit the migration and invasion of ER-negative MDA-MB-231 cells. ERRα antiagonist-2 inhibits the growth of breast cancer in vivo.

Compound 121, a D3R/MOR antagonist with K i values of 361 nM and 85.2 nM for D3R and MOR respectively, has the potential for analgesic effects through MOR partial agonism and may reduce opioid-misuse liability through D3R antagonism [1].

SSTR5 antagonist 2 is a highly potent, oral active and selective antagonist of somatostatin (receptor) subtype 5 (SSTR5),with potential to treat type 2 diabetes mellitus (T2DM).

GnRH antagonist 2 (formula I) is a potent GnRH receptor antagonist with valuable applications in endometriosis research[1].

A1AR antagonist 2 (compound 18h) is a potent antagonist of the A1 adenosine receptor (AR). A1AR antagonist 2 has Ki values of 1.49, 10.2, and 50.1 nM for hA 1, hA 2A, and hA 2B, respectively [1].

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 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.

SSTR5 antagonist 2 hydrochloride is a potent, orally active, selective growth hormone inhibitory hormone (receptor) subtype 5 (SSTR5) antagonist that has shown potential for investigation in type 2 diabetes.

LPA5 antagonist 2 (compound 65) is a highly water-soluble LPA5 antagonist that significantly reduces nociception.LPA5 antagonist 2 can be used to study inflammatory and neuropathic pain.

A3AR antagonist 2 is a potent antagonist of the human A3 adenosine receptor, exhibiting a Ki value of 4.54 nM.

Galectin-3, a β-galactoside-specific carbohydrate recognition protein (lectin), facilitates the migration of B-cell precursor acute lymphoblastic leukemia (BCP-ALL) cells and demonstrates resistance to pharmaceutical interventions.

CCK-B Receptor Antagonist 2 is a potent and orally active antagonist of Gastrin/CCK-B (IC50: 0.43 nM). It also inhibits gastrin/CCK-A activity (IC50: 1.82 μM).

RXR antagonist 2 is a potent antagonist of RXR (Ki: 0.391 μM, Kd: 0.281 μM). RXR antagonist 2 has shown research potential for RXR-related diseases.

GPR34 receptor antagonist 2 (Tyrosine, N-[(2E)-3-(4'-chloro[1,1'-biphenyl]-4-yl)-1-oxo-2-propen-1-yl]-O-(phenylmethyl)-) is an anti-inflammatory agent.

CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively.

Mu opioid receptor antagonist 2 (compound 25) is a potent and selective mu opioid receptor (MOR) antagonist that permeates the blood-brain barrier (Ki: 0.37 nM, EC50: 0.44 nM). Mu opioid receptor antagonist 2 can be used to study opioid use disorder (OUD).

CCR8 antagonist 2 is a potent antagonist of CCR8 that inhibits the activity of CCR8 (C-C Motif chemokine receptor 8), which is predominantly expressed on Treg and Th2 cells, and not on Th1 cells. CCR8 antagonist 2 can be used for the treatment of CCR8-mediated diseases (e.g. cancer and/or neuropathic pain).

Y2-Antagonist-2 is a novel, selective, soluble non-peptidic NPY Y2 receptor antagonist with enhanced CNS exposure.

AhR agonist 2 (Compound 12a) is a highly potent agonist of the aryl hydrocarbon receptor (AhR), exhibiting an EC50 value of 0.03 nM. This compound rapidly induces nuclear enrichment of AhR and initiates transcription of downstream genes, thereby promoting skin barrier repair. AhR agonist 2 shows promising potential for psoriasis research [1].

AR antagonist 2 (compound 58) is a potent inhibitor of the androgen receptor (AR) (IC50: 0.95 μM).

LXR antagonist 2 (compound 10rr) is a potent LXR (liver X receptor) inverse agonist, acting on LXRβ (IC50: 0.36 μM) and LXRα (IC50: 2.25 μM). LXR antagonist 2 is an adipogenesis inhibitor that downregulates LXR target genes SREBP-1c, ACC, FAS and SCD-1. LXR antagonist 2 exhibits hypolipidemic activity in Triton WR-1339-induced hyperlipidemic mice.

GPR84 Antagonist 2, a potent and selective GPR84 antagonist (IC 50 = 8.95 nM), demonstrates oral activity and significantly enhances potency in calcium mobilization assays. It effectively inhibits neutrophil and macrophage chemotaxis following GPR84 activation, highlighting its research potential for ulcerative colitis.

LPA2 antagonist 2 is ＞480-fold more selective than LPA3 (IC50 of 13.85 μM).LPA2 antagonist 2 is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM.