1. GPCR/G Protein
  2. LPL Receptor

SAR-100842 

Cat. No.: HY-100185 Purity: 99.69%
Handling Instructions

SAR-100842 is a lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor.

For research use only. We do not sell to patients.

SAR-100842 Chemical Structure

SAR-100842 Chemical Structure

CAS No. : 1195941-38-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 1178 In-stock
Estimated Time of Arrival: December 31
1 mg USD 751 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1202 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1923 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

SAR-100842 is a lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor.

IC50 & Target

LPA1/Edg-2 Receptor[1][2]

In Vitro

SAR-100842 (Compound Example 14) is an Edg-2 receptor inhibitor extracted from patent WO2009135590A1, has an IC50 of <0.1 μM[1]. 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[2]. 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[3].

In Vivo

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[3].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 83.3 mg/mL (186.98 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2446 mL 11.2231 mL 22.4462 mL
5 mM 0.4489 mL 2.2446 mL 4.4892 mL
10 mM 0.2245 mL 1.1223 mL 2.2446 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[3]

Mice[3]
To study SAR-100842 in the ovarian cancer lines, 6-8 week old athymic nu/nu mice receive either 1.0×106 SKVO3 cells or 3.5×106 OVCAR5 cells (n=33 mice per line) in an intraperitoneal injection. On day two post cell injection, mice are randomized to three groups. Group one begin vehicle on day 2, group two begin 30 mg/kg SAR-100842 twice daily on day two for the duration of the experiment, and group three begin 30 mg/kg SAR-100842 twice daily on day 10 for the duration of the experiment. On day 70 post cell injection all mice are euthanized and necropsied. Liver, abdominal lymph nodes or masses, omentum, peritoneum and any other organ suspected of harboring tumor are collected, fixed in 10% NBF and prepared for histological analysis[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

445.51

Formula

C₂₇H₂₇NO₅

CAS No.

1195941-38-8

SMILES

O=C(C1(NC(C2=CC=C(OC)C(OCCC3=CC=CC(C)=C3)=C2)=O)CC4=C(C=CC=C4)C1)O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
SAR-100842
Cat. No.:
HY-100185
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SAR-100842

Cat. No.: HY-100185