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MedChemExpress - Model Ro 61-8048 -199666-03-0
MCE products for research use only. We do not sell to patients.
Ro 61-8048
MCE China：Ro 61-8048
Brand：MedChemExpress (MCE)
Cat. No.HY-12347
CAS：199666-03-0
Purity：99.76%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Shipping：Room temperature in continental US; may vary elsewhere.
Description：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.
In Vitro：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[1]. Ro 61-8048 (0.1-100 μM) strongly reduces QUIN neo-formation, suggesting that, in vitro, kynurenine hydroxylase activity is required for QUIN neosynthesis[3].
In Vivo：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[2]. 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[2].
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References：
[1]. S Röver, et al. 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. [Content Brief]
[2]. Melanie Hamann, et al. Effects of the kynurenine 3-hydroxylase inhibitor Ro 61-8048 after intrastriatal injections on the severity of dystonia in the dt sz mutant. Eur J Pharmacol. 2008 May 31;586(1-3):156-9. [Content Brief]
Brand introduction:
• MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
• More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
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• It has a professional experimental center and strict quality control and verification system；
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• The biological activity of the products has been verified by the experiments of customers in various countries；
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