Ro 61-8048

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ro 61-8048 是一种有效的选择性犬尿氨酸羟化酶抑制剂，IC50 为 37 nM。

Ro 61-8048 is a potent and selective inhibitors of kynurenine hydroxylase with IC50 of 37 nM.

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 (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 100 and 150 mg/kg, while no central adverse effects were observable at a dose of 50 mg/kg or lower doses.

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Immunology/Inflammation

Hydroxylase

KMO| KMO

Neurological Disease

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199666-03-0

421.45

C17H15N3O6S2

>98% (HPLC)

DMSO: 59 mg/mL

COC1=C(OC)C=C(C=C1)S(=O)(=O)NC1=NC(=CS1)C1=CC(=CC=C1)[N+]([O-])=O

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(-20℃)

With Ice Pack

≥ 2 years