TDI-11861, CAS 2857049-72-8

Formulation: A solid

Formal Name: (3R)-4-[2-[2-[[3-(2-amino-6-chloro-4-pyrimidinyl)-1-(difluoromethyl)-1H-pyrazol-4-yl]methyl]phenoxy]ethyl]-3-morpholinemethanol

Purity: ≥95%

Formula Markup: C22H25ClF2N6O3

Formula Weight: 494,9

Shelf life (days): 1460

CAS Number: 2857049-72-8

Notes: 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.

• Artikelnummer: CAY39922-500
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 39922-500
• Verpackungseinheit: 500 µg
• Mengeneinheit: STK