Endogenous Metabolite Agonist

GL64 is a selective agonist of ADGRD1 (EC₅₀ = 3.98 μM). GL64 has low selectivity for ADGRD2, ADGRG5, ADGRG6, CELSR1, CELSR2, CELSR3, and ADGRG4 isoforms. GL64 activates ADGRD1 by mimicking the satchel sequence. GL64 regulates osteoclast maturation through the cAMP-PKA-NFATC1 pathway. GL64 effectively inhibits osteoclastogenesis and prevents bone loss both in vitro and in vivo. GL64 is useful in the study of osteoclast-related diseases.

4-Hydroxytryptamine creatinine sulfate, a tryptamine derivative, is a neurotransmitter agonist.

S-8666 is an orally active uricosuric antihypertensive diuretic. The S-8666 has both S-(-)- and R-(+)-isomers. The diuretic and sodium-excretion activities of it are entirely dominated by the S-(-)-isomer, while the R-(+)-isomer shows no significant activity. S-8666 relies on the organic acid transport system to be secreted through the proximal tubule. S-8666 exhibits a clear uric acid excretion-promoting activity and diuretic effect in various species (such as rats and chimpanzees).