Nitisinone

• UNSPSC Description:

  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[1][2][3][4].

• Target Antigen:

  HPPD

• Type:

  Reference compound

• Related Pathways:

  Metabolic Enzyme/Protease

• Applications:

  Metabolism-sugar/lipid metabolism

• Field of Research:

  Metabolic Disease

• Assay Protocol:

  https://www.medchemexpress.com/Nitisinone.html

• Purity:

  99.83

• Solubility:

  DMSO : 41.67 mg/mL (ultrasonic)|H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C)

• Smiles:

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

• Molecular Weight:

  329.23

• References & Citations:

  [1]Laschi M, et al. Inhibition of para-Hydroxyphenylpyruvate Dioxygenase by Analogues of the Herbicide Nitisinone As a Strategy to Decrease Homogentisic Acid Levels, the Causative Agent of Alkaptonuria. ChemMedChem. 2016 Apr 5;11(7):674-8.|[2]Ellis MK, et al. Inhibition of 4-hydroxyphenylpyruvate dioxygenase by 2-(2-nitro-4-trifluoromethylbenzoyl)-cyclohexane-1,3-dione and 2-(2-chloro-4-methanesulfonylbenzoyl)-cyclohexane-1,3-dione. Toxicol Appl Pharmacol. 1995 Jul;133(1):12-9. |[3]Onojafe IF, et al. Nitisinone improves eye and skin pigmentation defects in a mouse model of oculocutaneous albinism. J Clin Invest. 2011 Oct;121(10):3914-23. |[4]Aktuglu-Zeybek A, et al. Nitisinone: a review. Orphan Drugs: Research and Reviews, 2017, 7.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  Launched

• CAS Number:

  104206-65-7