Asivatrep|1005168-10-4|(PAC-14028)-陌孚医药/Medlife

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Asivatrep (Synonyms: PAC-14028)

目录号: PL12470 纯度: ≥95%

CAS No. :1005168-10-4

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中文名称	Asivatrep
中文别名	PAC-14028
英文名称	Asivatrep
英文别名	PAC-14028;PAC14028;Asivatrep;3VF7K7Z10B;PAC 14028;(E)-N-[(1R)-1-[3,5-difluoro-4-(methanesulfonamido)phenyl]ethyl]-3-[2-propyl-6-(trifluoromethyl)pyridin-3-yl]prop-2-enamide;(R,E)-N-(1-(3,5-difluoro-4-(methylsulfonamido)phenyl)ethyl)-3-(2-propyl-6-(trifluoromethyl)pyridin-3-yl)acrylamide;GTPL9621;Example 230 [US7858621];DB12428;SB17027;Q27258085;2-Propenamide, N-((1R)-1-(3,5-difluoro-4-((methylsulfonyl)amino)phenyl)ethyl)-3-(2-propyl-6-(trifluo
Cas No.	1005168-10-4
分子式	C₂₁H₂₂F₅N₃O₃S
分子量	491.47
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Asivatrep (PAC-14028) 是高效的选择性的瞬时受体电位香草酸亚型1 (TRPV1) 拮抗剂。

生物活性

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

性状

Solid

体外研究(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. Asivatrep (PAC-14028) shows efficacies against diverse disease models including visceral pain, inflammatory bowel disease, and inflammatory pain. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. 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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[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.

溶解度数据	In Vitro: DMSO : 50 mg/mL (101.74 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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