BQ-123 TFA is a potent and selectiveendothelin A (ETA) receptorantagonist with anIC₅₀of 7.3 nM and aK_iof 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension^[1][2][3].

IC50: 7.3 nM (Endothelin A receptors)^[1]
Ki: 25 nM (Endothelin A receptors)^[2]

Sustained infusions of BQ-123 (0.16-164 nmol/kg per min, intravenously, for 6 h) produces dose-dependent reductions in mean arterial pressure in spontaneously hypertensive rats (SHR), the maximal reduction being obtained with a dose of 16 nmol/kg per min^[4].
BQ-123 (3 mg/kg; i.v.; given 15 minutes before pentylenetetrazole (PTZ)) impedes the formation and spread of seizure to a great degree in PTZ (50 mg/kg; i.p.) +BQ-123 groups^[5].

724.72

C₃₃H₄₃F₃N₆O₉

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.