产品
编 号：F002780
分子式：C21H22F5N3O3S
分子量：491.47
分子式：C21H22F5N3O3S
分子量：491.47
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
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10mg
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结构图
CAS No: 1005168-10-4
产品详情
生物活性：
Asivatrep (PAC-14028) is a potent and selective transient receptor potential vanilloid type I (TRPV1) antagonist.
体内研究：
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. 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.
体外研究：
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. Asivatrep (PAC-14028) shows efficacies against diverse disease models including visceral pain, inflammatory bowel disease, and inflammatory pain.
Asivatrep (PAC-14028) is a potent and selective transient receptor potential vanilloid type I (TRPV1) antagonist.
体内研究：
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. 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.
体外研究：
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. Asivatrep (PAC-14028) shows efficacies against diverse disease models including visceral pain, inflammatory bowel disease, and inflammatory pain.
产品资料
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