An LPA5 antagonist
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AS-2717638

Item No. 37787

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6,7-dimethoxy-2-(5-methyl-1,2-benzisoxazol-3-yl)-4-(1-piperidinylcarbonyl)-1(2H)-isoquinolinone
CAS Number
2148339-28-8
Molecular Formula
C25H25N3O5
Formula Weight
447.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 2 mg/ml
λmax
253, 295 nm
SMILES
O=C1C2=C(C(C(N3CCCCC3)=O)=CN1C4=NOC5=C4C=C(C)C=C5)C=C(OC)C(OC)=C2
InChi Code
InChI=1S/C25H25N3O5/c1-15-7-8-20-18(11-15)23(26-33-20)28-14-19(24(29)27-9-5-4-6-10-27)16-12-21(31-2)22(32-3)13-17(16)25(28)30/h7-8,11-14H,4-6,9-10H2,1-3H3
InChi Key
QRMYHYZQUGJBBX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $80

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    5 mg

    $370

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    10 mg

    $701

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    25 mg

    $1,363

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    Product Description

    AS-2717638 is a lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50 = 0.038 µM).1 It is selective for LPA5 over LPA1, LPA2, and LPA3 (IC50s = >10 µM for all) but also binds to adenosine A1 and μ-opioid receptors at 10 µM. It induces analgesia in a rat model of allodynia induced by LPA or geranylgeranyl pyrophosphate (GGPP; Item No. 63330) when administered at doses of 3, 10, and 30 mg/kg. AS-2717638 (10 and 30 mg/kg) inhibits allodynia induced by prostaglandin E2 (PGE2; Item No. 14010), PGF2α, or AMPA in rats. It increases the paw withdrawal threshold and latency in the von Frey hair and plantar tests, respectively, in rats when administered at a dose of 10 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Murai, N., Hiyama, H., Kiso, T., et al. Analgesic effects of novel lysophosphatidic acid receptor 5 antagonist AS2717638 in rodents. Neuropharmacology 126, 97-107 (2017).