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/ Nitisinone

尼替西农 /Nitisinone {[allProObj[0].p_purity_real_show]}

货号：A384235 同义名： NTBC;Nitisone

Nitisinone is an inhibitor of the enzyme 4-hydroxyphenylpyruvate dioxygenase.

Nitisinone 化学结构 CAS号：104206-65-7
Nitisinone 化学结构
CAS号：104206-65-7
Nitisinone 3D分子结构
CAS号：104206-65-7
Nitisinone 化学结构 CAS号：104206-65-7
Nitisinone 3D分子结构 CAS号：104206-65-7
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Nitisinone 纯度/质量文件 产品仅供科研

货号：A384235 标准纯度： {[allProObj[0].p_purity_real_show]}
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Nitisinone 生物活性

描述 Nitisinone is an orally active, competitive, and reversible inhibitor of 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) with an IC50 of 173 nM. It increases tyrosine levels in a dose-dependent manner and is utilized in research related to hereditary tyrosinemia type 1 (HT-1), a rare genetic disorder, and albinism[1].[2].[3].[4].
体内研究

Administered orally at doses of 5 and 10 mg/kg, five days a week for six weeks, Nitisinone consistently inhibits 4-HPPD in rat liver in both a dose- and time-dependent manner[2].

Nitisinone, at a dose of 4 mg/kg administered orally once daily with a day's interval for a month, increases tyrosine levels in both OCA-1A and OCA-1B models[3].

The same dosing regimen of Nitisinone (4 mg/kg; orally; once daily; one day interval for one month) also enhances coat and iris pigmentation and increases melanin content in the melanosomes of ocular tissues in a mouse model of OCA-1B[3].
体外研究

Nitisinone (ranging from 0.01 to 10 μM over 72 hours) enhances tyrosine accumulation in a dose-responsive manner[1].

Nitisinone 参考文献

[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.

Nitisinone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.04mL

0.61mL

0.30mL

15.19mL

3.04mL

1.52mL

30.37mL

6.07mL

3.04mL

Nitisinone 技术信息

CAS号104206-65-7
分子式C14H10F3NO5
分子量 329.23
别名 NTBC;Nitisone;brand name: Orfadin.;SC0735
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C
溶解度

DMSO: 40 mg/mL(121.5 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 2.7 mg/mL clear

PO 0.5% CMC-Na 50 mg/mL suspension

Tags: Nitisinone | NTBC;Nitisone;brand name: Orfadin.;SC0735 | HPPD | AmBeed-信号通路专用抑制剂 | Nitisinone 纯度/质量文件 | Nitisinone 生物活性 | Nitisinone 参考文献 | Nitisinone 实验方案 | Nitisinone 技术信息

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