| Description | Asivatrep is an effective and selective transient receptor potential vanilloid type I antagonist. |
| In vitro | Asivatrep displays efficacies against diverse disease models including visceral pain, inflammatory bowel disease, and inflammatory pain. Asivatrep could prevent barrier damages, accelerate skin barrier recovery, and inhibit pruritus, displaying a potential for the treatment of atopic dermatitis. It could inhibit serum IgE increase, epidermal infiltration of inflammatory cells, and mast cell degranulation associated with atopic dermatitis[1][2]. |
| In vivo | Asivatrep displays a plasma half-life of 2.1 h in rats while it is extended slightly to 3.8 h in minipigs. Asivatrep 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 increases, and the accelerated barrier recovery from tape-stripping-induced barrier damages in hairless mice. Oral bioavailability at 10 mg/kg dose is determined to be 52.7% and 64.2% in rats and minipigs, respectively showing that Asivatrep is relatively well-absorbed through oral route[1][3]. |
| Synonyms | PAC-14028 |
| molecular weight | 491.47 |
| Molecular formula | C21H22F5N3O3S |
| CAS | 1005168-10-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 50 mg/mL (101.74 mM), Sonication is recommended. |
| References | 1. Park YH, et al. Oral and topical pharmacokinetic studies of a novel TRPV1 antagonist, PAC-14028 in rats and minipigs using liquid chromatography/tandem mass spectrometric method. J Pharm Biomed Anal. 2012 Mar 5;61:8-14. 2. Lim KM, et al. Development of PAC-14028, a novel transient receptor potential vanilloid type 1 (TRPV1) channel antagonist as a new drug for refractory skin diseases. Arch Pharm Res. 2012 Mar;35(3):393-6. 3. Yun JW, et al. TRPV1 antagonist can suppress the atopic dermatitis-like symptoms by accelerating skin barrier recovery. J Dermatol Sci. 2011 Apr;62(1):8-15. |