Nitisinone (Synonyms: NTBC; Nitisone; SC0735)

Name: Nitisinone
Brand: MedChemExpress
SKU: HY-B0607
Rating: 5.0 (2 reviews)

Cat. No.: HY-B0607 Purity: 99.93%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 104206-65-7

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Nitisinone:

2 Publications Citing Use of MCE Nitisinone

Cell Proliferation/Viability Assay

IHC

: Nitisinone purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2024 Feb 15:965:176326. [Abstract]; The concentrations of Nitisinone (NTBC) used in this study (25, 50, and 100 μM) did not have any significant effect on cell viability.

: Nitisinone purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2024 Feb 15:965:176326. [Abstract]; The representative fluorescence images demonstrated that Nitisinone (NTBC) could significantly improve the increase in MMP3 (3.38 ± 0.38) and MMP13 (2.25 ± 0.21) and decrease in Collagen II (0.91 ± 0.09) and Aggrecan (0.82 ± 0.09), thereby improving the degradation of extracellular matrix.

: Nitisinone purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2024 Feb 15:965:176326. [Abstract]; The results showed that the levels of iNOS and COX2 in the 100 μM Nitisinone (NTBC) group were only 0.09 times and 0.23 times that in the untreated group, respectively.

: Nitisinone purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2024 Feb 15:965:176326. [Abstract]; Western blotting results showed that Nitisinone (NTBC) inhibited the expression of cGAS, STING, and INF-α.

: Nitisinone purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2024 Feb 15:965:176326. [Abstract]; Nitisinone (NTBC: 100 μM) inhibited the expression of cGAS and p-P65, leading to increased expression of type II collagen and decreased expression of MMP13.

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References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	108 μM Compound: 7	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 37983010]
HUVEC	IC₅₀	338 μM Compound: 7	Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 37983010]
L02	IC₅₀	104 μM Compound: 7	Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 37983010]
MC-38	IC₅₀	96 μM Compound: 7	Antiproliferative activity against mouse MC-38 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against mouse MC-38 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 37983010]

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.

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.

104206-65-7

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
10 mM	0.3037 mL	1.5187 mL	3.0374 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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

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(per animal)

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: 99.93%

Select Batch:

Data Sheet (284 KB) SDS (393 KB)

COA (256 KB) RP-HPLC (246 KB) MS (71 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[4]. Aktuglu-Zeybek A, et al. Nitisinone: a review. Orphan Drugs: Research and Reviews, 2017, 7.

Complete Stock Solution Preparation Table

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

Nitisinone Related Classifications

Metabolic Disease

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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Nitisinone (Synonyms: NTBC; Nitisone; SC0735)

Customer Review

Other Forms of Nitisinone:

Nitisinone Related Antibodies

2 Publications Citing Use of MCE Nitisinone

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Nitisinone Related Antibodies

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Complete Stock Solution Preparation Table

Nitisinone Related Classifications

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