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AM966

CAS No. : 1228690-19-4

MCE 国际站：AM966

产品活性：AM966 是一种高亲和性的选择性LPA₁-拮抗剂，抑制LPA-刺激的细胞内钙释放，IC₅₀ 为 17 nM。

研究领域：GPCR/G Protein

作用靶点：LPL Receptor

In Vitro: AM966 is a potent, selective, orally bioavailable LPA₁ receptor antagonist. AM966 inhibits LPA₁-mediated chemotaxis of human A2058 melanoma cells (IC₅₀=138±43 nM), IMR-90 human lung fibroblasts (IC₅₀=182±86 nM) and CHO mLPA₁ cells (IC₅₀=469±54 nM). LPA-induced ERK1/2 activation is completely blocked by AM966 (100 nM), which selectively antagonizes LPA₁ over LPA_2-5, with an IC₅₀ value of 3.8±0.4 nM. Pre-treatment with AM966 (100 nM) completely blocks ERK1/2 phosphorylation induced by Mianserin.

In Vivo: AM966 (30 mg/kg, BID) reduces vascular leakage, inflammation and lung injury and inflammation in a 3 day Bleomycin (HY-108345) model. AM966 inhibits lung fibrosis, maintains mouse body weight and decreases lung inflammation 14 days after Bleomycin lung injury. AM966 reduces vascular leakage, tissue injury and pro-fibrotic cytokine production in the 14 day Bleomycin study. AM966 demonstrates greater efficacy compared to Pirfenidone (HY-B0673) in the 14 day Bleomycin model. AM966 decreases mortality and fibrosis at late time points after Bleomycin injury.

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货号: HY-15277

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