For research use only. Not for therapeutic Use.
TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with high affinity (Kd high affinity of 1.7 nM and Kd low affinity of 14.5 nM)[1].
TAK-615 specifically binds to membranes expressing the human LPA1 receptor with estimated Kd high affinity (KdHi) of 1.7±0.5 nM and Kd low affinity (KdLo) of 14.5±12.1 nM[1].
TAK-615 is only able to partially inhibit the LPA response (~ 40% at 10 µM with an IC50 of 23±13 nM in β-arrestin assay; 60% at 10 µM, IC50 of 91±30 nM in calcium mobilisation assay) [1].
| Catalog Number | I015019 |
| CAS Number | 1664335-55-0 |
| Synonyms | 4-[[cyclopropylmethyl-[4-(2-fluorophenoxy)benzoyl]amino]methyl]benzoic acid |
| Molecular Formula | C25H22FNO4 |
| Purity | ≥95% |
| InChI | InChI=1S/C25H22FNO4/c26-22-3-1-2-4-23(22)31-21-13-11-19(12-14-21)24(28)27(15-17-5-6-17)16-18-7-9-20(10-8-18)25(29)30/h1-4,7-14,17H,5-6,15-16H2,(H,29,30) |
| InChIKey | LEZVXIZCJXKBJY-UHFFFAOYSA-N |
| SMILES | C1CC1CN(CC2=CC=C(C=C2)C(=O)O)C(=O)C3=CC=C(C=C3)OC4=CC=CC=C4F |
| Reference | [1]. Jonathan Ellery, et al. Identification of Compounds Acting as Negative Allosteric Modulators of the LPA 1 Receptor. Eur J Pharmacol. 2018 Aug 15;833:8-15. |
