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 ( K d high affinity of 1.7 nM and K d low affinity of 14.5 nM)
In Vitro
TAK-615 specifically binds to membranes expressing the human LPA1 receptor with estimated Kd high affinity (KdHi) of 1.7±0.5 nM and K d low affinity (KdLo) of 14.5±12.1 nM. TAK-615 is only able to partially inhibit the LPA response (~ 40% at 10 µM with an IC 50 of 23±13 nM in β-arrestin assay; 60% at 10 µM, IC 50 of 91±30 nM in calcium mobilisation assay). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:LPA1 Receptor 1.7-14.5 nM (Kd)
规格
规格或纯度
10mM in DMSO
英文名称
TAK-615
生化机理
TAK-615 是一种用于肺纤维化研究的 LPA1 受体负异位调节剂(NAM)。TAK-615 与 LPA1 受体的结合亲和力很高(K d 高亲和力为 1.7 nM,K d 低亲和力为 14.5 nM)。