2. Metabolic Enzyme/Protease
  3. HPPD
  4. Nitisinone

Nitisinone  (Synonyms: NTBC; Nitisone; SC0735)

Cat. No.: HY-B0607 Purity: 99.83%
COA Handling Instructions

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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.

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Nitisinone Chemical Structure

Nitisinone Chemical Structure

CAS No. : 104206-65-7

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Based on 2 publication(s) in Google Scholar

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Nitisinone Related Antibodies

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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].

In Vitro

Nitisinone (0.01-10 μM; 72 h) promotes tyrosine accumulation in a dose-dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Nitisinone Related Antibodies

Cell Viability Assay[1]

Cell Line: Human primary fibroblasts (HFb)
Concentration: 0.01-10 µM
Incubation Time: 72 h
Result: Exhibited massive intracellular accumulation of tyrosine in human cell cultures.
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[2].
Nitisinone (4 mg/kg; p.o.; single daily; one day interval for 1 month) elevates tyrosine in both OCA-1A and OCA-1B model[3].
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[3].
Note: Oculocutaneous albinism, type 1 (OCA1). There are 2 forms of OCA1, OCA-1A and OCA-1B. Individuals with the former lack functional tyrosinase and therefore lack melanin, while individuals with the latter produce some melanin[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats (120-150 g)[2].
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)[3].
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.
Clinical Trial
Molecular Weight

329.23

Formula

C14H10F3NO5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (126.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0374 mL 15.1870 mL 30.3739 mL
5 mM 0.6075 mL 3.0374 mL 6.0748 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.83%

COA (256 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0374 mL 15.1870 mL 30.3739 mL 75.9348 mL
5 mM 0.6075 mL 3.0374 mL 6.0748 mL 15.1870 mL
10 mM 0.3037 mL 1.5187 mL 3.0374 mL 7.5935 mL
15 mM 0.2025 mL 1.0125 mL 2.0249 mL 5.0623 mL
20 mM 0.1519 mL 0.7593 mL 1.5187 mL 3.7967 mL
25 mM 0.1215 mL 0.6075 mL 1.2150 mL 3.0374 mL
30 mM 0.1012 mL 0.5062 mL 1.0125 mL 2.5312 mL
40 mM 0.0759 mL 0.3797 mL 0.7593 mL 1.8984 mL
50 mM 0.0607 mL 0.3037 mL 0.6075 mL 1.5187 mL
60 mM 0.0506 mL 0.2531 mL 0.5062 mL 1.2656 mL
80 mM 0.0380 mL 0.1898 mL 0.3797 mL 0.9492 mL
100 mM 0.0304 mL 0.1519 mL 0.3037 mL 0.7593 mL
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Nitisinone Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nitisinone104206-65-7NTBC Nitisone SC0735SC0735SC 0735SC-0735HPPD4-Hydroxyphenylpyruvate dioxygenaseHT1AKUOCAhuman primary fibroblaststyrosinealbinismInhibitorinhibitorinhibit

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