Ro 61-8048

Cat. No. 3254

Ro 61-8048 C17H15N3O6S2 [199666-03-0]

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Chemical Name: 3,4-Dimethoxy-N-[4-(3-nitrophenyl)-2-thiazolyl]benzenesulfonamide

Biological Activity

Potent and competitive kynurenine 3-monooxygenase (kynurenine 3-hydroxylase; KMO) inhibitor (Ki = 4.8 nM, IC50 = 37 nM). Increases kynurenic acid levels to concentrations that antagonize the glycine site of NMDA receptors. Brain penetrant and exhibits antidystonic, anticonvulsant and neuroprotective activities.

Technical Data

M.Wt:
421.45
Formula:
C17H15N3O6S2
Solubility:
Soluble to 100 mM in DMSO and to 10 mM in ethanol
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
199666-03-0

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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Justinova et al (2013) Reducing cannabinoid abuse and preventing relapse by enhancing endogenous brain levels of kynurenic acid. Nat.Neurosci. 16 1652. PMID: 24121737.

Hamann et al (2008) Effects of kynurenine 3-hydroxylase inhibitor Ro 61-8048 after intrastriatal injections on the severity of dystonia in the dtsz mutant. Eur.J.Pharmacol. 586 156. PMID: 18353306.

Carpenedo et al (2002) Kynurenine 3-mono-oxygenase inhibitors attenuate post-ischaemic neuronal death in organotypic hippocampal slice cultures. J.Neurochem. 82 1465. PMID: 12354294.

Rover et al (1997) Synthesis and biochemical evaluation of N-(4-phenylthiazol-2-yl)benzenesulfonamides as high affinity inhibitors of kynurenine 3-hydroxylase. J.Med.Chem. 40 4378. PMID: 9435907.

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Keywords: Ro 61-8048, supplier, Potent, kynurenine, 3-hydroxylase, inhibitors, inhibits, NMDA, antagonists, increases, kynurenic, acid, levels, Tryptophan, Hydroxylase, 11-β, 11-beta, LTB-omega-Hydroxylase, Kynurenine, 3-Hydroxylase, Hydroxylases, Glutamate, Receptors, N-Methyl-D-Aspartate, iGluR, Ionotropic, Ro61-8048, KMO, Tocris Bioscience, Hydroxylase Inhibitor products

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