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SAR-100842

CAS No. : 1195941-38-8

MCE 站：SAR-100842

产品活性：SAR-100842 是一种溶血磷脂酸 1 (LPA1/Edg-2) 受体抑制剂。

研究领域：GPCR/G Protein

作用靶点：LPL Receptor

In Vitro: SAR-100842 (Compound Example 14) is an Edg-2 receptor inhibitor extracted from patent WO2009135590A1, has an IC₅₀ of <0.1 μM. SAR-100842 (SAR100842) is a lysophaphatidic acid receptor 1 (LPA1) inhibitor, which can be used for the treatment of systemic sclerosis and related fibrotic diseases. In LPAR1-based in vitro inhibition of LPA-stimulated Ca²⁺ flux in a cell based assay, SAR-100842 (SAR100842) has an IC₅₀ of 65 nM; and shows no activity up to 10 μM on LPA2, LPA3 or LPA5 in similar calcium assays. Increasing doses of SAR-100842 do not significantly affect proliferation of either cell line over time. There is a significant decrease in the ability of cells to migrate in a wound healing assay in a dose dependent manner, 64% reduction (p<0.0001) with 5 μM SAR-100842 after 72 hours in MDA-MB-231T and 67% reduction (p<0.0001) with 50 μM SAR-100842 after 48 hours in 4T1-Luc2. In a Boyden chamber assay for motility, 50 μM SAR100842 reduces the migration of MDA-MD-231T cells through a collagen membrane by 1.92-fold (p=0.0004) and 3.15-fold (p<0.0001) to FBS and LPA chemoattractants, respectively. In 4T1-Luc2 cells 50 μM SAR-100842 reduces migration by 10.8-fold (p=0.01) and 13.6-fold (p=0.007) to FBS and LPA, respectively.

In Vivo: SAR-100842 (SAR100842) has a half-life of 4.9 h and a C_max of 5600 ng/mL after a 30 mg/kg oral dosing in mice.

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