A selective LPA1 receptor antagonist
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

AM095

Item No. 22141

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4'-[3-methyl-4-[[[(1R)-1-phenylethoxy]carbonyl]amino]-5-isoxazolyl]-[1,1'-biphenyl]-4-acetic acid
CAS Number
1228690-36-5
Molecular Formula
C27H24N2O5
Formula Weight
456.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
297 nm
SMILES
O=C(O)CC(C=C1)=CC=C1C(C=C2)=CC=C2C3=C(NC(O[C@H](C)C4=CC=CC=C4)=O)C(C)=NO3
InChi Code
InChI=1S/C27H24N2O5/c1-17-25(28-27(32)33-18(2)20-6-4-3-5-7-20)26(34-29-17)23-14-12-22(13-15-23)21-10-8-19(9-11-21)16-24(30)31/h3-15,18H,16H2,1-2H3,(H,28,32)(H,30,31)/t18-/m1/s1
InChi Key
LNDDRUPAICPXIN-GOSISDBHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    5 mg

    $90

    Add

    10 mg

    $168

    Add

    25 mg

    $392

    Add
    Product Description

    AM095 is an orally bioavailable antagonist of lysophosphatidic acid receptor 1 (LPA1) with IC50 values of 25 and 23 nM in CHO cells expressing human or mouse receptors, respectively.1 It is selective for LPA1 over LPA2, LPA3, LPA4, and LPA5 (IC50s = >10,000 nM for human LPA2-5). It inhibits chemotaxis of CHO cells overexpressing LPA1 and of A2058 human melanoma cells (IC50s = 778 and 233 nM, respectively) and prevents LPA-induced increases in plasma histamine levels in mice (ED50 = 8.3 mg/kg).2 It also decreases collagen and protein levels in bronchoalveolar lavage fluid (BALF) in a mouse model of bleomycin-induced lung injury (ED50s = ~10 mg/kg for both) and decreases kidney fibrosis in a mouse model of unilateral ureteral obstruction when administered at a dose of 30 mg/kg for eight days.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Castelino, F.V., Seiders, J., Bain, G., et al. Genetic deletion or pharmacologic antagonism of LPA1 ameliorates dermal fibrosis in a scleroderma mouse model. Arthritis Rheum. 63(5), 1405-1415 (2011).

    2. Swaney, J.S., Chapman, C., Correa, L.D., et al. Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. J. Pharmacol. Exp. Ther. 336(3), 693-700 (2011).