Ro 61-8048

Key Product Details

Product Description

Ro 61-8048 is a potent and competitive kynurenine 3-monooxygenase (kynurenine 3-hydroxylase; KMO) inhibitor (K_i = 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. Ro 61-8048 decreases nicotine self-administration in vivo. Ro 61-8048 prevents post-operative brain edema and consequent neuronal apoptosis in a rat model of surgically induced brain injury.

Product Specifications for Ro 61-8048

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for Ro 61-8048

The following data is based on the product molecular weight 421.45.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.37 mL	11.86 mL	23.73 mL
5 mM	0.47 mL	2.37 mL	4.75 mL
10 mM	0.24 mL	1.19 mL	2.37 mL
50 mM	0.05 mL	0.24 mL	0.47 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 9 publications citing the usage of this product.

• Zakhary Modification of kynurenine pathway via inhibition of kynurenine hydroxylase attenuates surgical brain injury complications in a male rat model. J Neurosci Res 2020 PMID: 31257634
• Secci Attenuating nicotine reinforcement and relapse by enhancing endogenous brain levels of kynurenic acid in rats and squirrel monkeys. Neuropsychopharmacology 2017 PMID: 28139681
• Justinova Reducing cannabinoid abuse and preventing relapse by enhancing endogenous brain levels of kynurenic acid. Nat.Neurosci. 2013 PMID: 24121737
• Hamann Effects of kynurenine 3-hydroxylase inhibitor Ro 61-8048 after intrastriatal injections on the severity of dystonia in the dt^sz mutant. Eur.J.Pharmacol. 2008 PMID: 18353306
• Carpenedo Kynurenine 3-mono-oxygenase inhibitors attenuate post-ischaemic neuronal death in organotypic hippocampal slice cultures. J.Neurochem. 2002 PMID: 12354294
• Rover Synthesis and biochemical evaluation of N-(4-phenylthiazol-2-yl)benzenesulfonamides as high affinity inhibitors of kynurenine 3-hydroxylase. J.Med.Chem. 1997 PMID: 9435907

Product Documents for Ro 61-8048