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Ro 61-8048

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Chemical Structure| 199666-03-0 同义名 : -
CAS号 : 199666-03-0
货号 : A927595
分子式 : C17H15N3O6S2
纯度 : 99%+
分子量 : 421.447
MDL号 : MFCD11040807
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(142.37 mM)，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：

2% DMSO+30% PEG 300+5% Tween 80+water 10 mg/mL

生物活性
靶点

  • Hydroxylase

    KMO, Ki:4.8 nM

    KMO, IC50:37 nM
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 Ki 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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.86mL

2.37mL

1.19mL

23.73mL

4.75mL

2.37mL
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