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Merck
CN

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.

别名:

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

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关于此项目

经验公式(希尔记法):
C17H15N3O6S2
化学文摘社编号:
分子量:
421.45
UNSPSC Code:
12352200
MDL number:
NACRES:
NA.28
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SMILES string

[S](=O)(=O)(Nc2[s]cc(n2)c3cc(ccc3)[N+](=O)[O-])c1cc(c(cc1)OC)OC

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

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

Quality Level

General description

A cell-permeable thiazolylbenzenesulfonamide compound that acts as a potent, competitive and reversible inhibitor of kynurenine-3-monooxygenase activity (Ki = 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 ).

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

存储类别

11 - Combustible Solids

wgk

WGK 3


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