A dichlorobenzimidazolopyrrolidinamide compound that acts as a highly potent PrCP-selective inhibitor (IC50 = 1nM against human PrCP; IC50 = 2 and 8nM against mouse PrCP, respectively, in the absence or presence of 1% mouse serum albumin), presumably via non-covalent catalytic site interaction, while exhibiting no significant potency toward panels of ion channels, receptors, and enzymes, including homologous serine proteases QPP, FAP, PEP, ACE2, DPP4, DPP8, and DPP9 (IC50 >25uM). Oral administration (100mg/kg/d for 5 d) is reported to result in significant food intake reduction and body fat loss among high fat diet-induced obese mice in vivo.
Solubility:DMSO (100mg/ml)
Proton NMR Spectroscopic:Conforms to structure
Liquid Chromatography Mass Spectrometry:Conforms to structure
Storage and Stability:Lyophilized and reconstituted products are stable for 6 months after receipt at -20°C. Reconstitute with DMSO. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap.
