产品描述:
TDI-11861 is an inhibitor of soluble adenylyl cyclase (sAC; IC50 = 3.3 nM), a bicarbonate-regulated cytosolic enzyme also known as AC10.{49825} It is selective for sAC over the transmembrane ACs (tmACs) AC1, AC2, AC5, AC8, and AC9 at 100 nM, a panel of 322 kinases (IC50s = >1,000 nM for all), and 46 other targets, including G protein-coupled receptors (GPCRs), nuclear receptors, and ion channels, with 50% response concentration values (RC50s) of greater than 9 µM. TDI-11861 has an increased residence time when binding to sAC in a surface plasmon resonance (SPR) assay and a slower dissociation rate in a jump dilution recovery assay compared with the sAC inhibitor TDI-10229 (Item No. 37674), indicating a lower risk of post-copulation female genital tract dilution. It inhibits capacitation-induced cAMP accumulation in isolated mouse and human sperm when used at a concentration of 5 µM and reduces sodium bicarbonate-induced increases in mouse and human sperm beat frequency.{49826} Oral administration of a single dose of TDI-11861 (50 mg/kg) induces temporary infertility in male mice without affecting mating behavior.