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Tocris/Ro 61-8048/3254/10/10 mg

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货号: 3254/10

品牌: Tocris

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Description: Potent kynurenine 3-monooxygenase (KMO) inhibitor

Chemical Name: 3,4-Dimethoxy-N-[4-(3-nitrophenyl)-2-thiazolyl]benzenesulfonamide

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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.

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

Product Datasheets

Certificate of Analysis / Product Datasheet

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 dt^sz 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

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