Ro 61-8048

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Cat.No. 3254 - Ro 61-8048 | C17H15N3O6S2 | CAS No. 199666-03-0
Description: Potent kynurenine 3-monooxygenase (KMO) inhibitor
Chemical Name: 3,4-Dimethoxy-N-[4-(3-nitrophenyl)-2-thiazolyl]benzenesulfonamide
Purity: ≥99% (HPLC)
Datasheet
Citations
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Literature

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

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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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


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Citations for Ro 61-8048

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