| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | TAK-615 | ||||||||||||
| CAS | 1664335-55-0 | ||||||||||||
| Formula | C25H22FNO4 | ||||||||||||
| Molar Mass | 419.44 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |