Nitisinone is an inhibitor of the enzyme 4-hydroxyphenylpyruvate dioxygenase.
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描述 | Nitisinone is an orally active, competitive, and reversible inhibitor of 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) with an IC50 of 173 nM. It increases tyrosine levels in a dose-dependent manner and is utilized in research related to hereditary tyrosinemia type 1 (HT-1), a rare genetic disorder, and albinism[1].[2].[3].[4]. |
体内研究 | Administered orally at doses of 5 and 10 mg/kg, five days a week for six weeks, Nitisinone consistently inhibits 4-HPPD in rat liver in both a dose- and time-dependent manner[2]. Nitisinone, at a dose of 4 mg/kg administered orally once daily with a day's interval for a month, increases tyrosine levels in both OCA-1A and OCA-1B models[3]. The same dosing regimen of Nitisinone (4 mg/kg; orally; once daily; one day interval for one month) also enhances coat and iris pigmentation and increases melanin content in the melanosomes of ocular tissues in a mouse model of OCA-1B[3]. |
体外研究 | Nitisinone (ranging from 0.01 to 10 μM over 72 hours) enhances tyrosine accumulation in a dose-responsive manner[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.04mL 0.61mL 0.30mL |
15.19mL 3.04mL 1.52mL |
30.37mL 6.07mL 3.04mL |
CAS号 | 104206-65-7 |
分子式 | C14H10F3NO5 |
分子量 | 329.23 |
别名 | NTBC;Nitisone;brand name: Orfadin.;SC0735 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 40 mg/mL(121.5 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
IP 2% DMSO+2% Tween80+30% PEG300+water 2.7 mg/mL clear PO 0.5% CMC-Na 50 mg/mL suspension |