An LPA1, LPA3, and LPA5 antagonist
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H2L 5765834

Item No. 45940

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,3-dihydro-2-[3-(4-nitrophenoxy)phenyl]-1,3-dioxo-1H-isoindole-5-carboxylic acid
CAS Number
420841-84-5
Molecular Formula
C21H12N2O7
Formula Weight
404.3
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
O=C(N1C2=CC(OC(C=C3)=CC=C3[N+]([O-])=O)=CC=C2)C4=CC(C(O)=O)=CC=C4C1=O
InChi Code
InChI=1S/C21H12N2O7/c24-19-17-9-4-12(21(26)27)10-18(17)20(25)22(19)14-2-1-3-16(11-14)30-15-7-5-13(6-8-15)23(28)29/h1-11H,(H,26,27)
InChi Key
HFYPTENHTPNXGP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $59

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    5 mg

    $148

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    10 mg

    $236

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    25 mg

    $443

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    Product Description

    H2L 5765834 is an antagonist of lysophosphatidic acid receptor 1 (LPA1), LPA3, and LPA5 (IC50s = 94, 752, and 463 nM, respectively).1 It is selective for these receptors over LPA2 and LPA4. H2L 5765834 (50 µM) reverses increases in viability induced by overexpression of the gene encoding autotaxin, also known as ectonucleotide pyrophosphatase/phosphodiesterase family member 2 (ENPP2), in MIN6 pancreatic β-cells.2 It decreases mechanical hypersensitivity in an NCTC clone 2472 murine fibrosarcoma model of cancer-associated pain.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fells, J.I., Tsukahara, R., Liu, J., et al. Structure-based drug design identifies novel LPA3 antagonists. Bioorg. Med. Chem. 17(21), 7457-7464 (2009).

    2. Zhou, Y., Zeng, Y., Chen, Y., et al. Phosphodiesterase ENPP2, which is co-upregulated in obese and pregnant mice, is essential for islet beta cell compensation during obesity. Diabetologia 69(4), 1000-1020 (2026).

    3. Khasabova, I.A., Khasabov, S.G., Johns, M., et al. Exosome-associated lysophosphatidic acid signaling contributes to cancer pain. Pain 164(12), 2684-2695 (2023).