ahr antagonist 4

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

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 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.

EP3 antagonist 4 is an EP3 antagonist that inhibits hEP with a Ki of 2 nM. EP3 antagonist 4 showed low in vivo clearance, high oral AUC and good bioavailability in complete PK studies in rats. EP3 antagonist 4 can be used to study diabetes and cellular dysfunction.

Calcium Channel antagonist 4 is a voltage-gated calcium channel inhibitor (IC50 : 5-20 μM).

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].

TRPV4 antagonist 4, a potent inhibitor of TRPV4 with an IC50 of 22.65 nM, effectively blocks TRPV4 current and demonstrates protective properties against acute lung injury [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].

Adenosine receptor antagonist 4 is an adenosine receptor antagonist.

CXCR2 antagonist 4 (compound 7) is a highly potent antagonist that inhibits CXCR2 with an IC50 value of 0.13 μM. It also effectively inhibits the cytosolic calcium increase induced by CXCL8, with an IC50 value of 27 μM. CXCR2 antagonist 4 shows promising potential for anticancer research [1].

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].

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].

CCR2 antagonist 4 hydrochloride is a specific CCR2 antagonist (IC50s: 180 nM for CCR2b). It potently inhibits MCP-1-induced chemotaxis (IC50: 24 nM).

MrgprX2 antagonist-4 and compound B-51 E117, is a potent MrgprX2 antagonist. It specifically targets and inhibits the MrgprX2 receptor, making it suitable for investigating various inflammatory skin disorders.

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.

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).

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

CCR2 antagonist 4 (Teijin compound 1) is a potent and specific antagonist of CCR2(IC50s of 180 nM), and potently inhibits MCP-1-induced chemotaxis(IC50 of 24 nM).

AHR agonist 4 (compound 24e), as an Aryl hydrocarbon receptor (AHR) agonist, modulates the immune equilibrium between Th17/22 and Treg cells. It is a lead compound under investigation for anti-psoriasis drugs and demonstrates efficacy in mitigating imiquimod (IMQ)-induced psoriasis-like skin lesions [1].

CCR4 Antagonist 4 (Compound 22) is a potent and selective antagonist of the CC chemokine receptor-4 (CCR4), displaying an IC50 value of 0.02 μM. It also inhibits MDC-mediated chemotaxis and Ca2+ mobilization, with IC50 values of 0.007 μM and 0.003 μM, respectively. This compound is utilized in research on allergic inflammation [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].

A1AR antagonist 4 (compound 22) is a highly developed chemical compound that acts as a potent and selective antagonist of the A1 adenosine receptor (A1AR). It possesses a pIC50 value of 5.51 and a pKi value of 6.29 [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].

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.

AR antagonist 4 (Compound 67-b) is an orally active androgen receptor (AR) antagonist that acts on wild-type AR (IC50: 246.6 nM).

CXCR4 antagonist 4 is an orally active and potent CXCR4 antagonist with an IC50 of 24 nM. CXCR4 antagonist 4 inhibits CYP 2D6 activity, increases PAMPA permeability, and effectively blocks entry of human immunodeficiency virus (IC50=7 nM).

PDM11 (1-[2-(4-Chloro-phenyl)-vinyl]-3,5-diMeth) is an antagonist of aryl hydrocarbon receptor (AhR)