Nitisinone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Nitisinone (SC0735) 是 4-羟苯基丙酮酸双加氧酶的抑制剂。

Nitisinone(SC0735) is an inhibitor of the enzyme 4-hydroxyphenylpyruvate dioxygenase.(In Vitro):Nitisinone (0.01-10 μM; 72 h) promotes tyrosine accumulation in a dose-dependent manner.(In Vivo):Nitisinone (5, 10 mg/kg; p.o.; 5 days aweek for 6 weeks) inhibits HPPD in a dose- and time- dependent manner in rat liver.Nitisinone (4 mg/kg; p.o.; single daily; one day interval for 1 month) elevates tyrosine in both OCA-1A and OCA-1B model.Nitisinone (4 mg/kg; p.o.; single daily; one day interval for 1 month) increases coat and iris pigmentation and melanin content in the melanosomes of ocular tissues in a mouse model of OCA-1B.

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Animal Model:Male Wistar rats (120-150 g).Dosage:5, 10 mg/kgAdministration: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.

NTBC | SC-0735

Others

Other Targets

4-hydroxyphenylpyruvate dioxygenase

Metabolic Disease

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104206-65-7

329.23

C14H10F3NO5

>98% (HPLC)

Soluble in DMSO

O=C1C(C(C2=CC=C(C(F)(F)F)C=C2[N+]([O-])=O)=O)C(CCC1)=O

2-(2-nitro-4-(trifluoromethyl)benzoyl)cyclohexane-1,3-dione

(-20℃)

With Ice Pack

≥ 2 years