Bioactivity | LTA4H-IN-1 is a potent inhibitor of leukotriene A4 hydrolase (LTA4H) extracted from patent WO2015092740A1, example 29, has an IC50 of 2 nM. LTA4H-IN-1 can be used for the research of inflammatory and autoimmune disorders[1]. | ||||||||||||
Target | IC50: 2 nM (LTA4H) | ||||||||||||
Invitro | LTA4H-IN-1 (15 min) inhibits the hydrolysis of 7-amino-4-methylcoumarin (AMC) derivative of Arginine (Arg-AMC) which is catalyzed by LTA4H, with an IC50 of 2 nM[1].LTA4H-IN-1 (30 min) inhibits LTB4 biosynthesis in a human whole blood assay (hWB), with an IC50 of 167 nM[1]. | ||||||||||||
In Vivo | LTA4H-IN-1 (0.3 mg/kg; a single p.o.) inhibits the -43% release of LTB4 compared with vehicle control in mice[1]. | ||||||||||||
Name | LTA4H-IN-1 | ||||||||||||
CAS | 1799681-85-8 | ||||||||||||
Formula | C16H14ClFN6O3 | ||||||||||||
Molar Mass | 392.77 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Bollbuck B, et, al. Heteroaryl butanoic acid derivatives as leukotriene A4 hydrolase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. WO2015092740A1. |