CAS No. : 1005168-10-4

(Synonyms: PAC-14028)

Price and Availability of CAS No. : 1005168-10-4
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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)
Introduction of 1005168-10-4 :

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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