LTA4H-IN-1

• CAT Number: I031274
• CAS Number: 1799681-85-8
• Molecular Formula: C16H14ClFN6O3
• Molecular Weight: 392.77
• Purity: ≥95%
• Synonyms: (3S)-3-amino-4-[5-[4-(5-chloro-3-fluoropyridin-2-yl)oxyphenyl]tetrazol-2-yl]butanoic acid
• InChI: InChI=1S/C16H14ClFN6O3/c17-10-5-13(18)16(20-7-10)27-12-3-1-9(2-4-12)15-21-23-24(22-15)8-11(19)6-14(25)26/h1-5,7,11H,6,8,19H2,(H,25,26)/t11-/m0/s1
• InChIKey: ZEGMEJVULDALSH-NSHDSACASA-N
• SMILES: C1=CC(=CC=C1C2=NN(N=N2)CC(CC(=O)O)N)OC3=C(C=C(C=N3)Cl)F

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].
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].
LTA4H-IN-1 (0.3 mg/kg; a single p.o.) inhibits the -43% release of LTB4 compared with vehicle control in mice[1].

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.