Molecular Formula | C17H28ClNO2 |
Molar Mass | 313.86272 |
Appearance | powder |
Color | white |
Storage Condition | desiccated |
In vitro study | ICI 118551 inhibits cAMP accumulation with IC 50 of 1.7 μM in IMCD cells. ICI 118551 (10 μM) induces a prominent vasorelaxation of norepinephrine (NE)-precontracted PA but not AO. In failing human heart, ICI 118551 has significant effects on beat duration, with time-to-peak contraction and time-to-90% relaxation reduced compared with basal contraction. Negative Inotropic Effect of ICI 118551 Is Not cAMP-Related. Overexpression of β2AR in rabbit myocytes enhances negative inotropic effects of ICI 118551. |
In vivo study | ICI 118551 (0.2 mg/kg) injected into the jugular vein of the mice, reduces systolic pressure in the pulmonary circuit but not systemic arterial pressure. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.186 ml | 15.931 ml | 31.861 ml |
5 mM | 0.637 ml | 3.186 ml | 6.372 ml |
10 mM | 0.319 ml | 1.593 ml | 3.186 ml |
5 mM | 0.064 ml | 0.319 ml | 0.637 ml |
biological activity | ICI 118,551 hydrochloride is a highly selective β2 adrenergic receptor antagonist that binds to β2, the Ki values of β1 and β3 adrenergic receptors are 0.7,49.5 and 611 nM, respectively. |
Target | Ki: 0.7nM (β2 receptor), 49.5 nM (β1 receptor), 611 nM (β3 receptor) |