产品
编 号：F018383
分子式：C14H10F3NO5
分子量：329.23
分子式：C14H10F3NO5
分子量：329.23
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
168
In-stock
10mg
264
In-stock
50mg
704
In-stock
100mg
1000
In-stock
结构图
CAS No: 104206-65-7
产品详情
生物活性：
Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism.
体内研究：
Nitisinone (5、10 mg/kg；口服；每周 5 天，持续 6 周) 在大鼠肝脏中以剂量和时间依赖性方式抑制 HPPD。 Nitisinone (4 mg/kg；口服；每天一次；一天间隔 1 个月) 在 OCA-1A 和 OCA-1B 模型中升高酪氨酸。 Nitisinone (4 mg/kg；口服每日一次；一天间隔 1 个月) 在 OCA-1B 小鼠模型中增加眼组织黑素体中的毛发和虹膜色素沉着和黑色素含量。注：眼皮肤白化病，1 型 (OCA1)。OCA1 有 2 种形式，OCA-1A 和 OCA-1B。前者缺乏功能性酪氨酸酶，因此缺乏黑色素，而后者则产生一些黑色素。Animal Model:Male Wistar rats (120-150 g).
Dosage:5, 10 mg/kg
Administration:Oral gavage; 5 days aweek for 6 weeks.
Result:Inhibited HPPD in a dose- and time- dependent manner in rat liver. (rat liver form animal model, incubate with 0-200 nM Nitisinone for 3 min).
Animal Model:C57BL/6J mice (WT mice), Tyrc-2J/c-2J mice (model of OCA-1A) and Tyrc-h/c-h mice (model of OCA-1B) (all are 3 to 4-month-age).
Dosage:4 mg/kg
Administration:Oral gavage; single daily; every other day for 1 month.
Result:Elevated plasma tyrosine levels 4- to 6- fold compared with placebo-treated controls, after 1 month in both OCA-1A and OCA-1B model.Increased pigmentation in the irides and pigmentation in areas of new hair growth upon physical, in OCA-1B model.Significant increased in the number of pigmented melanosomes in OCA-1B model.Showed substantial pigmentation in the irides of Tyrc-h/c-h pups born of Nitisinone-treated mothers.
体外研究：
Nitisinone (0.01-10 μM；72 h) 以剂量依赖性方式促进酪氨酸积累。
Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism.
体内研究：
Nitisinone (5、10 mg/kg；口服；每周 5 天，持续 6 周) 在大鼠肝脏中以剂量和时间依赖性方式抑制 HPPD。 Nitisinone (4 mg/kg；口服；每天一次；一天间隔 1 个月) 在 OCA-1A 和 OCA-1B 模型中升高酪氨酸。 Nitisinone (4 mg/kg；口服每日一次；一天间隔 1 个月) 在 OCA-1B 小鼠模型中增加眼组织黑素体中的毛发和虹膜色素沉着和黑色素含量。注：眼皮肤白化病，1 型 (OCA1)。OCA1 有 2 种形式，OCA-1A 和 OCA-1B。前者缺乏功能性酪氨酸酶，因此缺乏黑色素，而后者则产生一些黑色素。Animal Model:Male Wistar rats (120-150 g).
Dosage:5, 10 mg/kg
Administration:Oral gavage; 5 days aweek for 6 weeks.
Result:Inhibited HPPD in a dose- and time- dependent manner in rat liver. (rat liver form animal model, incubate with 0-200 nM Nitisinone for 3 min).
Animal Model:C57BL/6J mice (WT mice), Tyrc-2J/c-2J mice (model of OCA-1A) and Tyrc-h/c-h mice (model of OCA-1B) (all are 3 to 4-month-age).
Dosage:4 mg/kg
Administration:Oral gavage; single daily; every other day for 1 month.
Result:Elevated plasma tyrosine levels 4- to 6- fold compared with placebo-treated controls, after 1 month in both OCA-1A and OCA-1B model.Increased pigmentation in the irides and pigmentation in areas of new hair growth upon physical, in OCA-1B model.Significant increased in the number of pigmented melanosomes in OCA-1B model.Showed substantial pigmentation in the irides of Tyrc-h/c-h pups born of Nitisinone-treated mothers.
体外研究：
Nitisinone (0.01-10 μM；72 h) 以剂量依赖性方式促进酪氨酸积累。
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