Ro 61-8048

製品コードS8172 バッチS817202

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H15N3O6S2
分子量 421.45 CAS No. 199666-03-0
Solubility (25°C)* 体外 DMSO 84 mg/mL (199.31 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO Corn oil
10.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Ro 61-8048 is a high-affinity kynurenine 3-hydroxylase (KMO) inhibitor with IC50 and Ki of 37 nM and 4.8 nM, respectively.
in vivo In gerbils and rats, Ro 61-8048 (30 mg/kg, p.o.) causes kynurenine 3-hydroxylase inhibition. [1] In models of focal or global brain ischemia, Ro 61-8048 (40 mg/kg, p.o.) reduce ischemic brain damage. [2] In a hamster model of paroxysmal dyskinesia, Ro 61-8048 (150 mg/kg i.p.) significantly reduces the severity of dystonia without leading to marked central side effects. [3] addition, prenatal inhibition of the kynurenine pathway by Ro 61-8048 leads to structural changes in the hippocampus of adult rat offspring. [4]

プロトコル(参考用のみ)

キナーゼアッセイ Kynurenine 3-Hydroxylase Activity Determination and in Vitro Inhibition
Kynurenine 3-hydroxylase activity is measured using a microplate version of the radioenzymatic method based on the release of tritiated water after hydroxylation of l-[3-3H]kynurenine. The assay is performed in 96 well/plate in a final volume of 100 μL of 0.1 M potassium phosphate buffer, pH 7.4. The reaction mixture consists of 100 μM unlabeled l-kynurenine sulfate, 0.1 μCi of l-[3-3H]kynurenine (sp act. 14.4−16.1 Ci/mmol; 1 Ci = 37 GBq), 200 μM NADPH, 0.4 unit/mL glucose 6-phosphate dehydrogenase, 3 mM glucose 6-phosphate, and 30 μg of the mitochondrial enzyme preparation. In most experiments, a preincubation period of 15 min at 37 °C in the presence of the appropriate concentration of the inhibitor is performed before starting the reaction by the addition of the substrate, and the incubation is prolonged for 10 min at 37 °C. To absorb the unreacted substrate, 150 mL of a 10% (w/v) suspension of activated charcoal are added to each well, and after shaking for 2 min, the plates are centrifuged for 10 min at 4000 rpm in a Eppendorf model 5403 centrifuge. An aliquot (50 mL) of the samples is then transferred to the well of a second plate, and after addition of 200 μL/well of scintillation fluid, sealing, and vigorous shaking for 20 min, the plates are counted for radioactivity using a Top-Count (Packard) counter. Enzyme activity kinetic constants are calculated by fitting the data obtained from saturation experiments to Michaelis−Menten equation using the Ultrafit computer program or after Lineweaver−Burke double reciprocal transformation of the data. Inhibition constants (Ki) are calculated from replots of the apparent Km values versus the inhibitor concentrations used. Determination of IC50 values is performed by fitting the experimental data from inhibition curves using at least eight different inhibitor concentrations to logistic sigmoid equation using a computer program.
動物実験 動物モデル Male albino rats and female gerbils
投薬量 30 μmol/kg
投与方法 p.o.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Modification of kynurenine pathway via inhibition of kynurenine hydroxylase attenuates surgical brain injury complications in a male rat model. [ J Neurosci Res, 2020, 98(1):155-167] PubMed: 31257634
Targeting tryptophan catabolic kynurenine pathway enhances antitumor immunity and cytotoxicity in multiple myeloma. [ Leukemia, 2019, 10.1038/s41375-019-0558-x] PubMed: 31462737
Blast Preconditioning Protects Retinal Ganglion Cells and Reveals Targets for Prevention of Neurodegeneration Following Blast-Mediated Traumatic Brian Injury [ Invest Ophthalmol Vis Sci, 2019, 60(13):4159-4170] PubMed: 31598627

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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