产品
编 号：F247066
分子式：C17H15N3O6S2
分子量：421.45
分子式：C17H15N3O6S2
分子量：421.45
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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50mg
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100mg
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200mg
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结构图
CAS No: 199666-03-0
产品详情
生物活性：
Ro 61-8048 is an orally active and selective inhibitor of kynurenine 3-hydroxylase, with an IC50 of 37 nM. Ro 61-8048 provokes a significant increase of extracellular kynurenic acid concentrations.
体内研究：
Ro 61-8048 (50, 100 and 150 mg/kg i.p.) significantly reduces the severity of dystonia in dtsz hamsters without leading to marked central side effects.Ro 61-8048 (100 mg/kg i.p.) provokes a two- to threefold increase of the endogeneous broad spectrum glutamate receptor antagonist kynurenic acid in the striatum, cerebellum and brainstem of mutant hamsters.Animal Model:Male and female dtsz mutant Syrian golden hamsters.
Dosage:50, 100 and 150 mg/kg.
Administration:I.P., one dose.
Result:Significantly reduced the individual maximum severity of dystonia reached at the end of the observation period of 3 h at doses of 50, 100 and 150 mg/kg i.p..100 and 150 mg/kg significantly decreased the severity, indicating a fast onset of action. Adelayed onset of dystonic attacks was observed after treatment with 150 mg/kg but not after administration of 50 and 100 mg/kg.At lower doses of 10 and 25 mg/kg, the compound failed to exert any antidystonic effects.Caused a moderate sedation and hypolocomotion 5 to 70 min after administration of 100and 150 mg/kg, while no central adverse effects were observable at a dose of 50 mg/kg or lower doses.
体外研究：
In gerbils, a dose of 30 μmol/kg po (12.64 μg/kg Ro 61-8048, compound 16) leads to inhibition of the cerebral enzyme which peaked after 2h (～85% inhibition) and persisted for up to 8 h.Ro 61-8048 (0.1-100 μM) strongly reduces QUIN neo-formation, suggesting that, in vitro, kynurenine hydroxylase activity is required for QUIN neosynthesis.
Ro 61-8048 is an orally active and selective inhibitor of kynurenine 3-hydroxylase, with an IC50 of 37 nM. Ro 61-8048 provokes a significant increase of extracellular kynurenic acid concentrations.
体内研究：
Ro 61-8048 (50, 100 and 150 mg/kg i.p.) significantly reduces the severity of dystonia in dtsz hamsters without leading to marked central side effects.Ro 61-8048 (100 mg/kg i.p.) provokes a two- to threefold increase of the endogeneous broad spectrum glutamate receptor antagonist kynurenic acid in the striatum, cerebellum and brainstem of mutant hamsters.Animal Model:Male and female dtsz mutant Syrian golden hamsters.
Dosage:50, 100 and 150 mg/kg.
Administration:I.P., one dose.
Result:Significantly reduced the individual maximum severity of dystonia reached at the end of the observation period of 3 h at doses of 50, 100 and 150 mg/kg i.p..100 and 150 mg/kg significantly decreased the severity, indicating a fast onset of action. Adelayed onset of dystonic attacks was observed after treatment with 150 mg/kg but not after administration of 50 and 100 mg/kg.At lower doses of 10 and 25 mg/kg, the compound failed to exert any antidystonic effects.Caused a moderate sedation and hypolocomotion 5 to 70 min after administration of 100and 150 mg/kg, while no central adverse effects were observable at a dose of 50 mg/kg or lower doses.
体外研究：
In gerbils, a dose of 30 μmol/kg po (12.64 μg/kg Ro 61-8048, compound 16) leads to inhibition of the cerebral enzyme which peaked after 2h (～85% inhibition) and persisted for up to 8 h.Ro 61-8048 (0.1-100 μM) strongly reduces QUIN neo-formation, suggesting that, in vitro, kynurenine hydroxylase activity is required for QUIN neosynthesis.
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