Nitisinone

SKU: orb1227076

Description

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.

Key Properties

• CAS Number: 104206-65-7
• MW: 329.23
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₀F₃NO₅
• SMILES: O=C1C(C(C2=CC=C(C(F)(F)F)C=C2[N+]([O-])=O)=O)C(CCC1)=O
• Target: 4-hydroxyphenylpyruvate dioxygenase
• Solubility: Soluble in DMSO

Bioactivity

• In Vivo:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NTBC | SC-0735

Quick Database Links

Gene Symbol

4-hydroxyphenylpyruvate dioxygenase