PF-04859989
| Code | Size | Price |
|---|
| TAR-T24617-5mg | 5mg | £850.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T24617-50mg | 50mg | £1,661.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T24617-100mg | 100mg | £2,079.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃
Documents
Further Information
Bioactivity:
PF-04859989 is a brain-penetrable irreversible inhibitor of kynurenine amino transferase II. PF-04859989 is ~1000-fold selective for KAT II over human KAT I, KAT III, and KAT IV. PF-04859989 has IC50 values of 23 nM for hKAT II and 263 nM for rKAT II.
CAS:
34783-48-7
Formula:
C9H10N2O2
Molecular Weight:
178.191
Purity:
0.98
SMILES:
N[C@H]1Cc2ccccc2N(O)C1=O
References
1. Nematollahi A, Sun G, Jayawickrama GS, Hanrahan JR, Church WB. Study of the Activity and Possible Mechanism of Action of a Reversible Inhibitor of Recombinant Human KAT-2: A Promising Lead in Neurodegenerative and Cognitive Disorders. Molecules. 2016 Jun 29;21(7). pii: E856. doi: 10.3390/molecules21070856. PubMed PMID: 27367665.
2. Linderholm KR, Alm MT, Larsson MK, Olsson SK, Goiny M, Hajos M, Erhardt S, Engberg G. Inhibition of kynurenine aminotransferase II reduces activity of midbrain dopamine neurons. Neuropharmacology. 2016 Mar;102:42-7. doi: 10.1016/j.neuropharm.2015.10.028. Epub 2015 Oct 24. PubMed PMID: 26514401.
3. Kozak R, Campbell BM, Strick CA, Horner W, Hoffmann WE, Kiss T, Chapin DS, McGinnis D, Abbott AL, Roberts BM, Fonseca K, Guanowsky V, Young DA, Seymour PA, Dounay A, Hajos M, Williams GV, Castner SA. Reduction of brain kynurenic acid improves cognitive function. J Neurosci. 2014 Aug 6;34(32):10592-602. doi: 10.1523/JNEUROSCI.1107-14.2014. PubMed PMID: 25100593.
4. Koshy Cherian A, Gritton H, Johnson DE, Young D, Kozak R, Sarter M. A systemically-available kynurenine aminotransferase II (KAT II) inhibitor restores nicotine-evoked glutamatergic activity in the cortex of rats. Neuropharmacology. 2014 Jul;82:41-8. doi: 10.1016/j.neuropharm.2014.03.004. Epub 2014 Mar 16. PubMed PMID: 24647121; PubMed Central PMCID: PMC4372264.