gpr84 antagonist 8

GPR84 antagonist 8 is a selective GPR84 antagonist.

Estrogen receptor antagonist 8 acts as an estrogen receptor (ER) antagonist with anti-uterine activity and potential anti-tumorigenic activity and can be used to study ovarian dysfunction.

TLR7 8 9 antagonist 2 is an orally active and highly bioavailable vTLR7 8 9 antagonist. It 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.

MrgprX2 antagonist-8 is an MrgprX2 antagonist that can be used to study inflammatory diseases.

GPR84 Antagonist 3 (compound 42), a potent inhibitor of the G-protein-coupled receptor 84 (GPR84), exhibits a pIC50 value of 8.28, indicating strong antagonistic activity by inhibiting GTPγS. Additionally, it possesses a favorable pharmacokinetic profile, suitable for further research and development [1].

Muopioid Receptor Antagonist 8 (368) serves as an antagonist to the μ-opioid receptor, significantly inhibiting the activation of Gi induced by met-enkephalin at the µOR.

Compound (R)-10a, an NMDA receptor antagonist, exhibits selectivity for the GluN2B subunit, possessing a Ki of 265 nM and an IC50 of 62 nM. This compound is utilized in research pertaining to neurodegenerative diseases [1].

CXCR2 antagonist 8 is a potent and selective CXCR2 antagonist suitable for researching insulin resistance [1].

GPR84 antagonist 1 is a highly selective, high-affinity competitive antagonist of human GPR84.

TLR7 8 antagonist 2 (Compound 15) is a highly potent and orally active agonist of TLR7 8 with IC50 values of 4.9 nM for TLR7 and 0.6 nM for TLR8, making it a promising candidate for treating and investigating autoimmune diseases like lupus erythematosus, which involves inappropriate activation of TLR7 and TLR8. Consequently, TLR7 8 antagonist 2 is a valuable tool for autoimmune disease research [1].

TLR7 8 Antagonist 1 (Compound 16c), an imidazoquinoline derivative, is a potent TLR7 8 agonist with IC50 values of 3.91 and 2.19 μM for TLR7 and TLR8, respectively. rel-O-2050 (TLR-2050) is a key target for drug development in infectious diseases, cancer, and autoimmune diseases.

CCR1 antagonist 8, a third azaindazole series compound, is a CCR1 antagonist (IC50: 1.8 nM in Ca2+ flux assay).

CXCR4 antagonist 8 (Compound 3) is a potent inhibitor of CXCR4, exhibiting an IC50 value of 57 nM in antagonism and effectively inhibiting CXCL12-induced cytosolic calcium increase with an IC50 of 0.24 nM. Additionally, Compound 3 is efficacious in inhibiting CXCL12 CXCR4-mediated cell migration [1].

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.

GPR84antagonist 9 is an orally active GPR84 antagonist with an IC50 value of 0.012 μM. It can be utilized in research on inflammatory pain diseases.