Ro 61-8048

Name: Ro 61-8048
Brand: Tocris Bioscience
SKU: 3254

Tocris Bioscience, part of Bio-Techne | Catalog # 3254

Citations (13)

COA / SDS

Potent kynurenine 3-monooxygenase (KMO) inhibitor

Key Product Details

Description:	Potent kynurenine 3-monooxygenase (KMO) inhibitor
Chemical Name:	3,4-Dimethoxy-N-[4-(3-nitrophenyl)-2-thiazolyl]benzenesulfonamide
Purity:	≥98% (HPLC)
Molecular Weight:	421.45

View Full Technical Details for Ro 61-8048

Technical Data
Citations

Biological Activity for Ro 61-8048

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.

Compound Libraries for Ro 61-8048

Ro 61-8048 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Ro 61-8048

M. Wt	421.45
Formula	C₁₇H₁₅N₃O₆S₂
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	199666-03-0
PubChem ID	5282337
InChi Key	NDPBMCKQJOZAQX-UHFFFAOYSA-N
Smiles	O=S(NC1=NC(C2=CC=CC([N+]([O-])=O)=C2)=CS1)(C3=CC=C(OC)C(OC)=C3)=O

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Ro 61-8048

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	42.15	100
	ethanol	4.21	10

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for Ro 61-8048

References are publications that support the biological activity of the 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