For research use only. Not for therapeutic Use.
Ro 61-8048(CAT: I002532) is a potent and selective inhibitor of kynurenine hydroxylase, an enzyme involved in the metabolism of the amino acid tryptophan. By inhibiting kynurenine hydroxylase, Ro 61-8048 modulates the kynurenine pathway, which is implicated in various physiological and pathological processes, including neuroinflammation and neurodegenerative diseases. Ro 61-8048 has shown potential therapeutic effects in preclinical studies, particularly in the context of neuroinflammatory conditions.
| Catalog Number | I002532 |
| CAS Number | 199666-03-0 |
| Synonyms | 3,4-dimethoxy-N-(4-(3-nitrophenyl)thiazol-2-yl)benzenesulfonamide |
| Molecular Formula | C₁₇H₁₅N₃O₆S₂ |
| Purity | ≥95% |
| Target | Hydroxylases |
| Solubility | DMSO: ≥ 59 mg/mL |
| Storage | Store at +4C |
| IC50 | 37 nM [1] |
| InChI | InChI=1S/C17H15N3O6S2/c1-25-15-7-6-13(9-16(15)26-2)28(23,24)19-17-18-14(10-27-17)11-4-3-5-12(8-11)20(21)22/h3-10H,1-2H3,(H,18,19) |
| InChIKey | NDPBMCKQJOZAQX-UHFFFAOYSA-N |
| SMILES | COC1=C(C=C(C=C1)S(=O)(=O)NC2=NC(=CS2)C3=CC(=CC=C3)[N+](=O)[O-])OC |
| Reference | </br>1:Metabolism and pharmacokinetics of JM6 in mice: JM6 is not a prodrug for Ro-61-8048. Beconi MG, Yates D, Lyons K, Matthews K, Clifton S, Mead T, Prime M, Winkler D, O/’Connell C, Walter D, Toledo-Sherman L, Munoz-Sanjuan I, Dominguez C.Drug Metab Dispos. 2012 Dec;40(12):2297-306. doi: 10.1124/dmd.112.046532. Epub 2012 Aug 31. PMID: 22942319 Free Article</br>2:Is Ro 61-8048 a potential fast-acting antidepressant? Yang J, Li W, Zhou Z, Yang C.J Neurol Sci. 2012 Apr 15;315(1-2):180; author reply 181-2. doi: 10.1016/j.jns.2011.11.037. Epub 2011 Dec 12. No abstract available. PMID: 22169632 </br>3:Implication of NMDA receptors in the antidyskinetic activity of cabergoline, CI-1041, and Ro 61-8048 in MPTP monkeys with levodopa-induced dyskinesias. Ouattara B, Belkhir S, Morissette M, Dridi M, Samadi P, Grégoire L, Meltzer LT, Di Paolo T.J Mol Neurosci. 2009 Jun;38(2):128-42. doi: 10.1007/s12031-008-9137-8. Epub 2008 Aug 14. PMID: 18704766 </br>4:Effects of the kynurenine 3-hydroxylase inhibitor Ro 61-8048 after intrastriatal injections on the severity of dystonia in the dt sz mutant. Hamann M, Sander SE, Richter A.Eur J Pharmacol. 2008 May 31;586(1-3):156-9. doi: 10.1016/j.ejphar.2008.02.052. Epub 2008 Feb 29. PMID: 18353306 </br>5:The kynurenine 3-hydroxylase inhibitor Ro 61-8048 improves dystonia in a genetic model of paroxysmal dyskinesia. Richter A, Hamann M.Eur J Pharmacol. 2003 Sep 30;478(1):47-52. PMID: 14555184 </br>6:Quinolinic acid formation in immune-activated mice: studies with (m-nitrobenzoyl)-alanine (mNBA) and 3,4-dimethoxy-[-N-4-(-3-nitrophenyl)thiazol-2yl]-benzenesul fonamide (Ro 61-8048), two potent and selective inhibitors of kynurenine hydroxylase. Chiarugi A, Moroni F.Neuropharmacology. 1999 Aug;38(8):1225-33. PMID: 10462134 </br>7:Kynurenine hydroxylase inhibitors reduce ischemic brain damage: studies with (m-nitrobenzoyl)-alanine (mNBA) and 3,4-dimethoxy-[-N-4-(nitrophenyl)thiazol-2yl]-benzenesulfonamide (Ro 61-8048) in models of focal or global brain ischemia. Cozzi A, Carpenedo R, Moroni F.J Cereb Blood Flow Metab. 1999 Jul;19(7):771-7. PMID: 10413032 |
