420360-M

KMO Inhibitor I, Ro 61-8048

The KMO Inhibitor I, Ro 61-8048, also referenced under CAS 199666-03-0, controls the biological activity of KMO. This small molecule/inhibitor is primarily used for Neuroscience applications.

• Synonym(s): KMO Inhibitor I, Ro 61-8048, Kynurenine-3-Hydroxylase Inhibitor I, Ro 61-8048, 3,4-Dimethoxy-N-[4-(3-nitrophenyl)-2-thiazolyl]-benzenesulfonamide, Kynurenine-3-Monooxygenase Inhibitor I, Ro 61-8048, Dimethoxy-nitrophenyl-thiazolyl-benzenesulfonamide
• Empirical Formula (Hill Notation): C₁₇H₁₅N₃O₆S₂
• CAS Number: 199666-03-0
• Molecular Weight: 421.45
• MDL number: MFCD11040807
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥99% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 100 mg/mL; ethanol: 12.5 mg/mL
• storage temp.: 2-8°C
• InChI: 1S/C17H15N3O6S2/c1-25-15-7-6-13(9-16(15)26-2)28(23,24)19-17-18-14(10-27-17)11-4-3-5-12(8-11)20(21)22/h3-10H,1-2H3,(H,18,19)
• InChI key: NDPBMCKQJOZAQX-UHFFFAOYSA-N

Description

General description

A cell-permeable thiazolylbenzenesulfonamide compound that acts as a potent, competitive and reversible inhibitor of kynurenine-3-monooxygenase activity (K_i = 4.8 nM; IC₅₀ = 37 nM). Reported to increase the circulating levels of kynurenic acid (KYNA), an excitatory amino acid receptors antagonist, lower reactive oxygen species [ROS], reduce neuronal loss and enhance the survival rate in several neuronal disease models. An orally bioavilable KMO Inhibitor II, JM6, a prodrug of Ro 61-8048 is also available (Cat. No. 420361).

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Campesan, S., et al. 2011. Chem. Biol.21, 961.
Zwilling, D., et al. 2011. Cell145, 863.
Giorgini, F., et al. 2005. Nat. Genet.37, 526.
Cozzi, A.,. et al. 1999. J. Cereb. Blood Flow Metab.19, 771,
Rover, S., et al. 1997. J. Med. Chem.40, 4378.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3