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Asivatrep

产品编号 T16426 CAS 1005168-10-4

别名: PAC-14028

Asivatrep is an effective and selective transient receptor potential vanilloid type I antagonist.

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Asivatrep, CAS 1005168-10-4

规格	价格/CNY	货期
2 mg	￥ 1,820	5日内发货
5 mg	￥ 2,890	5日内发货
25 mg	￥ 9,620	6-8周
50 mg	￥ 12,500	6-8周
100 mg	￥ 17,500	6-8周
1 mL * 10 mM (in DMSO)	￥ 3,130	5日内发货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Asivatrep is an effective and selective transient receptor potential vanilloid type I antagonist.
体外活性	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].
体内活性	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].

别名	PAC-14028
分子量	491.47
分子式	C21H22F5N3O3S
CAS No.	1005168-10-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (101.74 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0347 mL	10.1736 mL	20.3471 mL	50.8678 mL
	5 mM	0.4069 mL	2.0347 mL	4.0694 mL	10.1736 mL
	10 mM	0.2035 mL	1.0174 mL	2.0347 mL	5.0868 mL
	20 mM	0.1017 mL	0.5087 mL	1.0174 mL	2.5434 mL
	50 mM	0.0407 mL	0.2035 mL	0.4069 mL	1.0174 mL
	100 mM	0.0203 mL	0.1017 mL	0.2035 mL	0.5087 mL

计算器

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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. 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.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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