SAR-100842
目录号 : KG11876 CAS No. : 1195941-38-8 纯度 : 98%
SAR-100842 is a lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor. 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. SAR-100842 (SAR100842) has a half-life of 4.9 h and a Cmax of 5600 ng/mL after a 30 mg/kg oral dosing in mice.
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1mg
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5mg
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分子式
C27H27NO5
分子量
445.51
CAS号
1195941-38-8
中文名称
2-{4-methoxy-3-[2-(3-methylphenyl)ethoxy]benzamido}-2,3-dihydro-1H-indene-2-carboxylic acid
储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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