| Chemical Properties | Back Directory | [Boiling point ]
769.1±60.0 °C(Predicted) | [density ]
1.348±0.06 g/cm3(Predicted) | [solubility ]
DMSO: soluble
Methanol: soluble | [form ]
Solid | [pka]
2.56±0.36(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
TK05 is a potent and selective inhibitor of leukotriene C4 synthase (LTC4S) with an IC50 of 95 nM[1]. | [Biological Activity]
TK05 is a potent and selective inhibitor of leukotriene C4 synthase (LTC4S) with an IC50 of 95 nM[1].
TK05 reduces LTC4 production in a dose-dependent manner with an IC50 value of 318 ± 60 nM in MM6 Cells[1].
TK05 (0.12-6 mg/kg; given i.p.; only once) significantly reduces LTE4 levels[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. |
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