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.
Compound Libraries
Ro 61-8048 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 421.45 |
| Formula | C17H15N3O6S2 |
| Storage | Store at +4°C |
| Purity | ≥99% (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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.15 | 100 | |
| ethanol | 4.21 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 421.45. Batch specific molecular weights may vary from batch to batch due to solvent 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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Product Datasheets
References
References are publications that support the products' biological activity.
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
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
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
Justinova et al (2013) Reducing cannabinoid abuse and preventing relapse by enhancing endogenous brain levels of kynurenic acid. Nat.Neurosci. 16 1652 PMID: 24121737
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, Ionotr, Hydroxylases, NMDA, Receptors, KMO, KMO, Tocris Bioscience
