四氢胡椒碱 T5786

Product Introduction
Bioactivity


英文名: TETRAHYDROPIPERINE

描述: Tetrahydropiperine (Cosmoperine) 是胡椒碱的环己基类似物，也是一种天然芳基戊酰胺，从Piper longum 分离得到。它对细胞色素 P450 (CYP) 同工型 CYP1A1/芳基烃羟化酶 (AHH；IC50=23 µM)具有抑制作用。

动物实验: The test compounds were PIP [5-(3,4-methylenedioxyphenyl)-2,4-pentadienoylpiperidine], tetrahydropiperine [THP, 5-(3,4-methylenedioxyphenyl)-pentanoylpiperidine], a cyclohexyl analogue of piperine [CHP, 5-(3,4-methylenedioxyphenyl)-2,4-pentadienoylcyclohexylamine], and reduced CHP [rCHP, 5-(3,4-methylenedioxyphenyl)-2,4-pentanoylcyclohexylamine].?Sparsely pigmented, HRA/Skh-II mice were randomized to receive topical treatment with test compounds or vehicle twice a day for five days a week, with or without ultraviolet (UV) irradiation on 3 days a week.?Treatment was either continuous or interrupted to evaluate fading and repigmentation.?Skin inflammation and pigmentation were evaluated regularly during treatment.?DOPA+ melanocytes were determined histologically at the termination of treatment[3].

体内活性: TETRAHYDROPIPERINE is an agonist of transient receptor potential vanilloid type 1 (TRPV1; EC50 = 6.3 μM)[1]. It inhibits the cytochrome P450 (CYP) isoform CYP1A1/arylhydrocarbon hydroxylase (AHH; IC50 = 23 μM) and 7-methoxycoumarin O-demethylase (MOCD) activity (IC50 = 25 μM) in rat liver microsomes[2].Tetrahydropiperine increases skin pigmentation in a mouse model of vitiligo when 100 μl of a 175 mM solution is administered topically, an effect that can be enhanced by subsequent suberythemal ultraviolet radiation (UVR)[3].

存储条件: keep away from direct sunlightPowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 57 mg/mL (196.97 mM)


关键字: Inhibitor | Cytochrome P450 | AHH | CYP | arylhydrocarbon | CYP1A1 | TETRAHYDROPIPERINE | CYPs | Piperine | aryl pentanamide | hydroxylase | inhibit

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途