TK05

Names

[ CAS No. ]:
1245734-61-5

[ Name ]:
TK05

Biological Activity

[Description]:

TK05 is a potent and selective inhibitor of leukotriene C4 synthase (LTC4S) with an IC50 of 95 nM[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Gutathione S-transferase

Research Areas >> Inflammation/Immunology

[Target]

IC50: 95 nM (Leukotriene C4 synthase)[1]

[In Vitro]

TK05 reduces LTC4 production in a dose-dependent manner with an IC50 value of 318 ± 60 nM in MM6 Cells[1].

[In Vivo]

TK05 (0.12-6 mg/kg; given i.p.; only once) significantly reduces LTE4 levels[1]. Animal Model: Zymosan A induced peritonitis mouse model[1] Dosage: 0.12 mg/kg; 6 mg/kg Administration: Given i.p.; only once Result: 0.12 mg/kg of TK05 significantly reduced LTE4 levels, whereas 6 mg/kg body weight of the compound resulted in almost complete inhibition compared with mice treated with only Zymosan A.

[References]

[1]. Kleinschmidt TK, et al. Tandem Benzophenone Amino Pyridines, Potent and Selective Inhibitors of Human Leukotriene C4 Synthase. J Pharmacol Exp Ther. 2015 Oct;355(1):108-16.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₁H₂₅ClN₂O₅

[ Molecular Weight ]:
540.99

Related Compounds

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