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首页-小分子抑制剂&激动剂-Others-Other Targets-LYS-006
LYS-006

Chemical Structure : LYS-006

CAS No.: 1799681-85-8

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LYS-006 (LYS006)

货号: 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.

规格 价格 库存 数量
5 mg ￥1580 In stock
10 mg ￥2480 In stock
25 mg ￥4280 In stock
50 mg ￥7280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 392.775
分子式 C16H14ClFN6O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO (3.9 mg/mL)
Chemical Name/SMILES

(S)-3-amino-4-(5-(4-((5-chloro-3-fluoropyridin-2-yl)oxy)phenyl)-2H-tetrazol-2-yl)butanoic acid

参考文献

1. Christian Markert, et al. J Med Chem. 2021 Feb 25;64(4):1889-1903.

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