Ro 61-8048 (CAS 199666-03-0)
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Ro 61-8048, a member of the thiazole family of compounds, is a small organic molecule that has been extensively studied for its potential applications in medicine and scientific research. It acts as a competitive inhibitor of KMO (kynurenine 3-hydroxylase), exhibiting a Ki value of 4.8 nM and an IC50 value of 37 nM. By inhibiting KMO, Ro 61-8048 effectively raises the levels of kynurenic acid, which can then antagonize the glycine site of NMDA receptors. The versatility of Ro 61-8048 has been explored in various scientific research applications. Its interactions with proteins, enzymes, and DNA have been investigated, revealing a wide range of biological activities. Studies have demonstrated its potential as an anti-cancer, anti-inflammatory, and anti-microbial agent. Additionally, Ro 61-8048 serves as useful for studying proteins, enzymes, and DNA, facilitating further research in these areas. Although the precise mechanism of action of Ro 61-8048 is not yet fully elucidated, it is believed to engage in covalent bonding with proteins, enzymes, and DNA. This interaction leads to the inhibition of their activity, ultimately resulting in the observed biological effects.
Ro 61-8048 (CAS 199666-03-0) References
- 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., et al. 1999. J Cereb Blood Flow Metab. 19: 771-7. PMID: 10413032
- 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. and Moroni, F. 1999. Neuropharmacology. 38: 1225-33. PMID: 10462134
- Kynurenine 3-mono-oxygenase inhibitors attenuate post-ischemic neuronal death in organotypic hippocampal slice cultures. | Carpenedo, R., et al. 2002. J Neurochem. 82: 1465-71. PMID: 12354294
- The kynurenine 3-hydroxylase inhibitor Ro 61-8048 improves dystonia in a genetic model of paroxysmal dyskinesia. | Richter, A. and Hamann, M. 2003. Eur J Pharmacol. 478: 47-52. PMID: 14555184
- Prolonged kynurenine 3-hydroxylase inhibition reduces development of levodopa-induced dyskinesias in parkinsonian monkeys. | Grégoire, L., et al. 2008. Behav Brain Res. 186: 161-7. PMID: 17868931
- 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., et al. 2008. Eur J Pharmacol. 586: 156-9. PMID: 18353306
- 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., et al. 2009. J Mol Neurosci. 38: 128-42. PMID: 18704766
- Kynurenine pathway inhibition reduces central nervous system inflammation in a model of human African trypanosomiasis. | Rodgers, J., et al. 2009. Brain. 132: 1259-67. PMID: 19339256
- Metabolism and pharmacokinetics of JM6 in mice: JM6 is not a prodrug for Ro-61-8048. | Beconi, MG., et al. 2012. Drug Metab Dispos. 40: 2297-306. PMID: 22942319
- Attenuating Nicotine Reinforcement and Relapse by Enhancing Endogenous Brain Levels of Kynurenic Acid in Rats and Squirrel Monkeys. | Secci, ME., et al. 2017. Neuropsychopharmacology. 42: 1619-1629. PMID: 28139681
- Biochemistry and structural studies of kynurenine 3-monooxygenase reveal allosteric inhibition by Ro 61-8048. | Gao, J., et al. 2018. FASEB J. 32: 2036-2045. PMID: 29208702
- Structural Basis for Inhibitor-Induced Hydrogen Peroxide Production by Kynurenine 3-Monooxygenase. | Kim, HT., et al. 2018. Cell Chem Biol. 25: 426-438.e4. PMID: 29429898
- Influx of kynurenine into the brain is involved in the reduction of ethanol consumption induced by Ro 61-8048 after chronic intermittent ethanol in mice. | Gil de Biedma-Elduayen, L., et al. 2022. Br J Pharmacol. 179: 3711-3726. PMID: 35189673
- Blast-related traumatic brain injury is mediated by the kynurenine pathway. | Zhang, Y., et al. 2022. Neuroreport. 33: 569-576. PMID: 35894672
- Synthesis and biochemical evaluation of N-(4-phenylthiazol-2-yl)benzenesulfonamides as high-affinity inhibitors of kynurenine 3-hydroxylase. | Röver, S., et al. 1997. J Med Chem. 40: 4378-85. PMID: 9435907
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Ro 61-8048, 10 mg | sc-204240 | 10 mg | $166.00 | |||
Ro 61-8048, 50 mg | sc-204240A | 50 mg | $515.00 |