st 7

Specific PXR antagonist 70 is a selective pregnane X receptor (PXR) antagonist with an IC50 of 540 nM and Ki of 390 nM for human PCR and enhances the chemosensitivity of cancer cells.

AST 7062601 is a potent Ucp1 inducer that promotes endogenous Ucp1 expression in primary mouse brown adipocytes.AST 7062601 may be useful in the study of obesity.

CCR1 antagonist 7 (compound 16r) is a chemokine receptor 1 (CCR1) antagonist with an IC50 of 4 nM [1].

PAR4 antagonist7 (Compound 20f) is a selective PAR4 antagonist (IC50: 1.72 nM), effective in inhibiting platelet aggregation induced by PAR4 agonists. It exhibits good metabolic stability and has not shown any tendency to cause bleeding in mice.

TGR5 agonist 7 (Compound 22-Na) is an intestine-restricted, orally active agonist of the G protein-coupled bile acid receptor TGR5 (GPBAR1 or GPR131) with an EC50 of less than 1 μM. In mouse models, it demonstrates blood glucose-lowering effects, making it useful for diabetes research.

EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4, with an IC50 of 1.1 nM. This compound inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 of 0.9 nM. In RAW 264.7 macrophages, it reduces the expression of PGE2-induced IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C motif) ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase 1 (Arg1) mRNA. In the CT26 mouse colon cancer model, EP4 receptor antagonist 7, combined with an anti-PD-1 antibody, inhibits tumor growth and enhances CD8+ T cell infiltration into the tumor.

TRPV3 antagonist 74a (TRPV3 74a) is a specific TRPV3 antagonist for the study of neurological disorders.

CXCR4 antagonist 7 (Compound PARA-B) is a potent CXCR4 inhibitor (IC50 = 9.3 nM) [1] applicable in research on HIV infection, inflammatory diseases, cancer, and WHIM syndrome.

CXCR2 antagonist 7 (compound 19) is a potent CXCR2 antagonist with strong binding affinity (IC50 = 0.044 μM) and calcium mobilization (IC50 = 0.66 μM) [1].

PPARγ agonist 7 (Compound 3a) is a highly potent and selective peroxisome proliferator-activated receptor gamma (PPARγ) agonist, which specifically stimulates adiponectin production in human bone marrow mesenchymal stem cells (hBM-MSCs), demonstrating an innovative full agonist profile with an EC50 value of 4.34 μM [1].

Estrogen Receptor Antagonist 7 (Compound 13) is a potent antagonist of estrogen receptors (ER), demonstrating antiproliferative effects against breast and ovarian cancer cells, along with anticancer and anti-uterotrophic activities [1].

Pparδ agonist 7 is a potent agonist of Pparδ, a member of the peroxisome proliferator-activated receptor (PPAR) intranuclear receptor transcription factor superfamily, which regulates metabolic homeostasis, inflammation, cell growth, and differentiation in vivo. [Tubulin aggregation-IN-19]

GLP-1 receptor agonist 7 is a potent glucagon-like peptide-1 (GLP-1) agonist, demonstrating research potential for GLP-1 related diseases, disorders, and conditions, including diabetes.

APJ receptor agonist 7 (compound 37) is an orally active apelin receptor (APJ) agonist with a Ki of 0.059 μM and an arrestin EC50 of 0.063 μM.

TLR7 8 agonist 7, a compound that functions as a TLR7 8 agonist, plays a pivotal role in activating various immune cells and is instrumental in the synthesis of immune-stimulating antibody conjugate (ISAC) molecules. This compound holds significant potential for research in immunology.

Compound (S)-10a, a GluN2B subunit-selective NMDA receptor antagonist, exhibits a K i of 93 nM and an IC 50 of 72 nM. It is potentially useful for research into neurodegenerative diseases [1].

Compound 24, also known as Mu opioid receptor antagonist 7, is a potent, centrally-acting µ-opioid receptor (µOR) antagonist with an inhibitory concentration (IC50) of 29 ± 3.0 nM. It is valuable for pain and opioid use disorder research [1].

Nurr1 agonist 7 (compound 110) is an agonist targeting the Nurr1 receptor, exhibiting an EC50 of 0.12 μM [1].

Compound 8, an AhR agonist 7, demonstrates potent activation of AhR with an EC50 of 13nM [1].

AR antagonist 7 (86) serves as an androgen receptor (AR) antagonist and is utilized in hair loss research [1].

EP3 antagonist 7 (Compound II), an EP3 receptor antagonist, is applicable in researching conditions such as itching, pain, dysuria, or stress disorders [1].

Compound 1, also known as GPR40 agonist 7, is an orally active agonist of the G protein-coupled receptor 40 (GPR40). It effectively enhances the secretion of insulin and GLP-1, exhibiting a hypoglycemic effect in vivo with an ED 50 of 0.58 mg kg [1].