| Bioactivity | LPA5 antagonist 1 (Compound 66) is a potent and selective lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50=32 nM). LPA5 antagonist 1 shows high brain permeability and anti-nociceptive activity. LPA5 antagonist 1 can be used in inflammatory and neuropathic pain research[1]. |
| Target | IC50: 32 nM (LPA5) |
| Invitro | LPA5 antagonist 2 (0-10 μM) inhibits hLPA5 calcium mobilization with an IC50 value of 32 nM[1].LPA5 antagonist 2 (0-10 μM) shows good target selectivity for LPA5[1]. |
| In Vivo | LPA5 antagonist 1 (intraperitoneal injection; 17.8 mg/kg; once) treatment shows good brain exposure in vivo[1].LPA5 antagonist 1 (intraperitoneal injection; 5.6, 10, and 17.8 mg/kg; once) treatment reduces mechanical allodynia in inflammatory pain model[1]. Animal Model: |
| Name | LPA5 antagonist 1 |
| Formula | C28H26N2O4S |
| Molar Mass | 486.58 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Zhang DH, et al. Isoquinolone derivatives as lysophosphatidic acid receptor 5 (LPA5) antagonists: Investigation of structure-activity relationships, ADME properties and analgesic effects. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. Volume 243, 5 December 2022, 114741. |