SAR-100842

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. . SCHAEFER, Matthias, et al. ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS. WO2009135590A1. . Kihara Y, et al. Lysophospholipid receptors in drug discovery. Exp Cell Res. 2015 May 1;333(2):171-7. . Brooks D, et al. Limited fibrosis accompanies triple-negative breast cancer metastasis in multiple model systems and is not a preventive target. Oncotarget. 2018 May 4;9(34):23462-23481.

Product information

CAS Number: 1195941-38-8

Molecular Weight: 445.51

Formula: C27H27NO5

Chemical Name: 2-{4-methoxy-3-[2-(3-methylphenyl)ethoxy]benzamido}-2,3-dihydro-1H-indene-2-carboxylic acid

Smiles: CC1C=CC=C(CCOC2=CC(=CC=C2OC)C(=O)NC2(CC3C=CC=CC=3C2)C(O)=O)C=1

InChiKey: SOJDTNUCCXWTMG-UHFFFAOYSA-N

InChi: InChI=1S/C27H27NO5/c1-18-6-5-7-19(14-18)12-13-33-24-15-20(10-11-23(24)32-2)25(29)28-27(26(30)31)16-21-8-3-4-9-22(21)17-27/h3-11,14-15H,12-13,16-17H2,1-2H3,(H,28,29)(H,30,31)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.