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Chemical Structure : LYS-006
CAS No.: 1799681-85-8
Catalog No.: PC-72651Not For Human Use, Lab Use Only.
LYS-006 (LYS006) is a potent, highly selective leukotriene A4 hydrolase (LTA4H) inhibitor with biochemical IC50 <3 nM.
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| 5 mg | $298 | In stock | |
| 25 mg | $598 | In stock | |
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LYS-006 (LYS006) is a potent, highly selective leukotriene A4 hydrolase (LTA4H) inhibitor with biochemical IC50 of 0.12 nM.
LYS-006 demonstrates high potency (IC50=53 nM) in human whole blood ionophore-stimulated LTB4 release assay.
LYS-006 shows an exquisite selectivity profile at 10 uM on a panel of >150 GPCRs, transporters, ion channels, nuclear receptors, and enzymes in vitro, does not inhibit other Zn2+ containing MMPs including MMP1, 2, 8, 9, 12, 13, 14 and TACE at 30 uM. LYS006 dependently inhibited ex vivo LTB4 formation, inhibited LTB4 production by 90% at dose >1 mg/kg, reduced MPO in skin homogenates y in neutrophilic skin inflammation models.
LYS-006 (0.1-3 mg/kg) suppressed neutrophilic inflammation in arachidonic acid induced skin inflammation model.
LYS006 has the potential for a best-in-class LTA4H inhibitor and is currently investigated in phase II clinical trials in inflammatory acne, hidradenitis suppurativa, ulcerative colitis, and NASH.
| M.Wt | 392.775 | |
| Formula | C16H14ClFN6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO (3.9 mg/mL) |
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| Chemical Name/SMILES |
(S)-3-amino-4-(5-(4-((5-chloro-3-fluoropyridin-2-yl)oxy)phenyl)-2H-tetrazol-2-yl)butanoic acid |
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1. Christian Markert, et al. J Med Chem. 2021 Feb 25;64(4):1889-1903.
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