For research use only. Not for therapeutic Use.
LPA5 antagonist 2 (compound 65) is a high aqueous solubility LPA5 (lysophosphatidic acid receptor 5) antagonist. LPA5 antagonist 2 significantly attenuates nociceptive hypersensitivity and it can be used for the research of inflammatory and neuropathic pains[1].
LPA5 antagonist 2 (0-10 μM) inhibits hLPA5 calcium mobilization with an IC50 value of 69 nM and inhibits hLPA5 cAMP with an IC50 value of 340 nM[1].
LPA5 antagonist 2 (0-10 μM) shows no significant affinity for other receptors, exhibits good target selectivity for LPA5[1].
LPA5 antagonist 2 (5.3-17.8 mg/kg; i.p. once) alleviates CFA-induced inflammatory pain in vivo[1].
Catalog Number | I042821 |
CAS Number | 2839471-44-0 |
Synonyms | 4-(4-fluoropiperidine-1-carbonyl)-6,7-dimethoxy-2-(3-methyl-1-benzothiophen-5-yl)isoquinolin-1-one |
Molecular Formula | C26H25FN2O4S |
Purity | ≥95% |
InChI | InChI=1S/C26H25FN2O4S/c1-15-14-34-24-5-4-17(10-18(15)24)29-13-21(25(30)28-8-6-16(27)7-9-28)19-11-22(32-2)23(33-3)12-20(19)26(29)31/h4-5,10-14,16H,6-9H2,1-3H3 |
InChIKey | HELXFZDNFAKTSS-UHFFFAOYSA-N |
SMILES | CC1=CSC2=C1C=C(C=C2)N3C=C(C4=CC(=C(C=C4C3=O)OC)OC)C(=O)N5CCC(CC5)F |
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. 2022. |