|3,4-二甲氧基-N-(4-(3-硝基苯基)噻唑-2-基)苯磺酰胺|CsnPharm

CAS No.: 199666-03-0

Ro 61-8048 Catalog No. CSN13615

Synonyms: Ro 61-8048

Ro 61-8048 is an inhibitor of kynurenine 3-hydroxylase which can potently and competitively inhibit kynurenine 3-monooxygenase with Ki value and IC50 value of 4.8 nM and 37 nM, respectively.

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技术信息

生物活性

描述Kynurenine 3-hydroxylase is a component of the kynurenine pathway involved in neuronal injury. Ro 61-8048 is an inhibitor of kynurenine 3-hydroxylase with an IC50 value of 37 ± 3nM. It acts as a competitive inhibitor of kynurenine 3-hydroxylase with a K_i value of 4.8 ± 2.1nM. The ED50 values (μmol/kg, p.o.) of Ro 61-8048 for the ex vivo inhibition of kynurenine 3-hydroxylase activity in rat kidney and liver are 1.2 (0.8 – 1.3) and 4.7 (3.6 – 5.6), respectively. Ro 61-8048 also inhibited kynurenine 3-hydroxylase activity in Gerbils brain, kidney, and liver with ED50 values (μmol/kg, p.o.) of 5.5 (3.3 – 9.2), 0.8 (0.5 – 1.2), and 0.4 (0.3 – 0.5). In rat hippocampus after implantation of a transversal microdialysis probe, Ro 61-8048 at a dose of 50μmol/kg (p.o.) led to a 4-fold increase in kynurenic acid levels.^[3]
作用机制Ro 61-8048 is a competitive inhibitor of kynurenine 3-hydroxylase.^[3]
参考文献

[1] Richter A, Hamann M. The kynurenine 3-hydroxylase inhibitor Ro 61-8048 improves dystonia in a genetic model of paroxysmal dyskinesia. Eur J Pharmacol. 2003 Sep 30;478(1):47-52.
[2] Cozzi A, Carpenedo R, et al. Kynurenine hydroxylase inhibitors reduce ischemic brain damage: studies with (m-nitrobenzoyl)-alanine (mNBA) and 3,4-dimethoxy-[-N-4-(nitrophenyl)thiazol-2yl] benzenesulfonamide (Ro 61-8048) in models of focal or global brain ischemia. J Cereb Blood Flow Metab. 1999 Jul;19(7):771-7.
[3] Röver S, Cesura AM, Huguenin P, Kettler R, Szente A. Synthesis and biochemical evaluation of N-(4-phenylthiazol-2-yl)benzenesulfonamides as high-affinity inhibitors of kynurenine 3-hydroxylase. J Med Chem. 1997 Dec 19;40(26):4378-85

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3728 mL
- 11.8639 mL
- 23.7277 mL
- 5 mM
- 0.4746 mL
- 2.3728 mL
- 4.7455 mL
- 10 mM
- 0.2373 mL
- 1.1864 mL
- 2.3728 mL

技术信息

CAS号

199666-03-0

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H15N3O6S2

运输

蓝冰

分子量

421.45

别名

Ro 61-8048

溶解度

DMSO	255.0 mg/mL (605.1 mM)
Water	insoluble

动物实验配方

2% DMSO+30% PEG 300+5% Tween 80+water

10 mg/mL

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Ro 61-8048 Catalog No. CSN13615

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