AS-2717638

AS-2717638 is a lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50 = 0.038 µM). 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, Cay-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, Cay-14010), PGF2alpha, 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.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: (Request formulation change), A solid. Solubility: DMF: 2 mg/ml, DMSO: 2 mg/ml. lambdamax: 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.