Urotensin-II receptor antagonist-1 is a selective antagonist of the human Urotensin II receptor, exhibiting a Ki value of 16 nM in HEK293 cells expressing the recombinant receptor. This compound demonstrates significant biological activity by inhibiting cytochrome P450 enzymes, CYP2D6 and CYP3A4, with IC50 values of 0.75 μM and 1.4 μM, respectively. Additionally, it inhibits the κ-opioid receptor with an EC50 of 3.2 μM and targets cardiac sodium channels with a Ki of 2.5 μM. Research applications include studies of cardiovascular physiology and drug metabolism.
Urotensin-II receptor antagonist-1 is a selective antagonist of the human Urotensin II receptor, exhibiting a Ki value of 16 nM in HEK293 cells expressing the recombinant receptor. This compound demonstrates significant biological activity by inhibiting cytochrome P450 enzymes, CYP2D6 and CYP3A4, with IC50 values of 0.75 μM and 1.4 μM, respectively. Additionally, it inhibits the κ-opioid receptor with an EC50 of 3.2 μM and targets cardiac sodium channels with a Ki of 2.5 μM. Research applications include studies of cardiovascular physiology and drug metabolism.
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