Luteolin 7-sulfate, derived from the marine plant Phyllospadix iwatensis Makino, suppresses TYR gene expression by intervening in a signaling pathway involving the cAMP-responsive element binding protein (CREB) and microphthalmia-associated transcription factor (MITF). This inhibition ultimately leads to a decrease in melanin synthesis.
Selective medium-chain free fatty acid receptor GPR84 agonist (EC50 = 139 nM). Exhibits no response at GPR40, GPR41, GPR119 or GPR120 at 100 μM. Activates calcium mobilization, inhibits cAMP accumulation, and induces ERK1/2 phosphorylation, receptor desensitization and internalization in vitro. Liu et al (2016) Design and synthesis of 2-alkylpyrimidine-4,6-diol and 6-alkylpyridine-2,4-diol as potent GPR84 agonists. ACS Med.Chem.Lett. 7 579 PMID:27326330 |Zhang et al (2016) Discovery and characterization of a novel small-molecule agonist for medium-chain free fatty acid receptor G protein-coupled receptor 84. J.Pharmacol.Exp.Ther. 357 337 PMID:26962172
DPC-AJ1951 is a peptide agonist of the parathyroid hormone (PTH) PTH-related peptide receptor (PPR; EC50 = 0.15 nM in HEK293 cells expressing human PPR). It induces cAMP production in SAOS-2 and UMR106 cells that endogenously express human and rat PPR, respectively (EC50s = 2.2 and 1.1 nM, respectively). DPC-AJ1915 stimulates osteoclast-mediated bone resorption in fetal rat long-bone explant cultures and increases collagen synthesis and cell proliferation in neonatal mouse parietal bone explants. In vivo, DPC-AJ1951 normalizes serum calcium levels in thyroidparathyroidectomized rats.
L-858,051 is a water-soluble analog of forskolin , a cell-permeant activator of adenylate cyclase. L-858,051 activates adenylate cyclase (EC50 = 3 μM), inhibits glucose transport, and blocks cytochalasin B binding in rat adipocyte membranes. L-858,051 is used to activate adenylate cyclase and initiate signaling through elevated cAMPsynthesis in a variety of cell types in culture.
C-Type Natriuretic Peptide (CNP) (1-22), human (TFA), is a 22 amino acid fragment of CNP and functions as an agonist for the natriuretic peptide receptor B (NPR-B). It can inhibit cAMPsynthesis, which is induced by histamine, 5-HT, or Forskolin. Additionally, CNP exhibits strong endothelial-derived relaxation properties and acts as a growth inhibitor.