PAC-14028|cas 1005168-10-4

PAC-14028|cas 1005168-10-4

DC Chemicals, Website: www.dcchemicals.com

Product Name: PAC-14028|Cas Number: 1005168-10-4| Catalog Number: DC10399|Other Nmaes: PAC14028; PAC 14028

PAC-14028 is a potent and selective transient receptor potential vanilloid type I (TRPV1) antagonist.

PAC-14028 could prevent barrier damages, accelerate skin barrier recovery and suppress pruritus, showing a potential for the treatment of atopic dermatitis. It could suppress serum IgE increase, epidermal infiltration of inflammatory cells and mast cell degranulation associated with atopic dermatitis[1]. PAC-14028 shows efficacies against diverse disease models including visceral pain, inflammatory bowel disease, and inflammatory pain[2].PAC-14028 shows a plasma half-life of 2.1 h in rats while it is extended slightly to 3.8 h in minipigs. Oral bioavailability at 10 mg/kg dose is determined to be 52.7% and 64.2% in rats and minipigs, respectively suggesting that PAC-14028 is relatively well-absorbed through oral route[1]. PAC-14028 could inhibit capsaicin-evoked calcium influx in keratinocytes at sub-micromolar concentrations. This potent TRPV1 antagonistic activity in keratinocytes is manifested in vivo as the blockade of capsaicin-induced blood perfusion increase, and the accelerated barrier recovery from tape-stripping-induced barrier damages in hairless mice[3].