Aspartic acid-2 is modified with the group α-amino-γ-oxo-4-phenyl-1-piperazinebutanoyl.
- Watanabe. T. et al. (1995) Br. J. Pharmacol. 114, 949.
- Alomone Labs TAK-044 inhibits Endothelin-B receptor-mediated Ca2+ mobilization in CHO cells.Cells were loaded with Calcium-6 dye, incubated with different concentrations of TAK-044 (#SPE-320), and stimulated by 30 nM Endothelin-1 (EC80). Changes in intracellular Ca2+ were monitored as changes in relative fluorescence (RLU) using FLIPRTETRA. IC50 was determined as 0.66 µM.
TAK-044 is a synthetic peptide that acts as a non-selective ET-B (endothelin B) and ET-A (endothelin A) receptor antagonist, receptors that belong to the G-protein coupled receptor (GPCR) superfamily. In a study conducted on rats the compound showed high inhibitory effects on the extension of myocardial infarct size after coronary artery occlusion-reperfusion1. TAK-044 inhibits radiolabelled ET-1 binding from the rabbit ventricular and cerebellar preparation with an IC50 value of 3.8 nM and 130 nM, respectively1.
Endothelin receptors include two subtypes: ET-A and ET-B. ET-A receptors are predominantly detected in peripheral tissues, especially in vascular smooth muscle tissues to mediate vasoconstriction. They are also present in several regions of the brain. ET-B receptors play an important role in regulating renal function and blood pressure and are expressed in sensory nerves. They are mainly present in medium- and large-sized cell bodies of human trigeminal ganglia2,3.
TAK-044 (#SPE-320) is a highly pure, synthetic, and biologically active cyclic peptide.