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BFF 122
- Optical Purity: Optically pure
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C17H19FN4O4
- MW: 362.36
Description
BFF 122 is a potent and selective kynurenine aminotransferase II (KAT II) inhibitor with reported IC50 values of approximately 1 µM for KAT II and greater than 30 µM for KAT I. Intrastriatal administration decreases newly formed kynurenic acid without altering 3-hydroxykynurenine or quinolinic acid production in naïve rats.
KAT II regulates synthesis of kynurenic acid, a neuroactive tryptophan metabolite that modulates glutamatergic and cholinergic neurotransmission. BFF 122 is relevant for kynurenine pathway and CNS neurochemical studies.
Key Features
- Selective KAT II inhibitor
- Reduced activity against KAT I
- Decreases newly formed kynurenic acid in vivo
- Does not alter 3-HK or quinolinic acid in cited rat studies
Applications
- KAT II enzyme assays
- Kynurenine pathway research
- Kynurenic acid neurochemistry studies
- CNS tryptophan metabolism models
More Information
| Parent CAS No. | 1152314-49-2 |
|---|---|
| Chemical Name | (S)-10-(4-aminopiperazin-1-yl)-9-fluoro-3-methyl-7-oxo-3,7-dihydro-2H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid |
| SMILES | O1C2=C(N3CCN(N)CC3)C(F)=CC3C(=O)C(C(O)=O)=CN(C2=3)[C@@H](C)C1 |&1:23,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C17H19FN4O4/c1-9-8-26-16-13-10(15(23)11(17(24)25)7-22(9)13)6-12(18)14(16)20-2-4-21(19)5-3-20/h6-7,9H,2-5,8,19H2,1H3,(H,24,25)/t9-/m0/s1 |
| InChiKey | ICQVSZFWVUBYSI-VIFPVBQESA-N |
| CID | 46829291 |
| Short Description | KAT II inhibitor |
References
- L. Amori et al. On the relationship between the two branches of the kynurenine pathway in the rat brain in vivo. J. Neurochem. 2009, 109, 316-325.
- F. Rossi et al. Crystal structure-based selective targeting of the pyridoxal 5'-phosphate dependent enzyme kynurenine aminotransferase II for cognitive enhancement. J. Med. Chem. 2010, 53, 5684-5689.
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