Size | Price | Stock |
---|---|---|
1mg | $180 | In-stock |
5mg | $420 | In-stock |
10mg | $600 | In-stock |
50mg | $1800 | In-stock |
100mg | $2520 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
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Cat. No. : | HY-12777 |
M.Wt: | 491.47 |
Formula: | C21H22F5N3O3S |
Purity: | >98 % |
Solubility: | DMSO : 50 mg/mL (101.74 mM; Need ultrasonic) |
Asivatrep (PAC-14028) is a potent and selective transient receptor potential vanilloid type I (TRPV1) antagonist. In Vitro: Asivatrep (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]. Asivatrep (PAC-14028) shows efficacies against diverse disease models including visceral pain, inflammatory bowel disease, and inflammatory pain[2]. In Vivo: Asivatrep (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 Asivatrep (PAC-14028) is relatively well-absorbed through oral route[1]. Asivatrep (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].
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