Ro 46-2005 proves to be equipotent (IC50 200-500 nM) for inhibition of [125I]ET-1 binding on the two known ET receptor subtypes (ETA and ETB). Ro 46-2005 also inhibits the functional consequences of ET-1 stimulation: the ET-l-induced release of arachidonic acid from rat mesangial cells was inhibited with an IC50 of 1.8 μM.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
In vitro characterization of Ro 46-2005, a novel synthetic non-peptide endothelin antagonist of ETA and ETB receptors.
Breu V,et.al. FEBS Lett. 1993 Nov 15;210-4. PMID: 8224248.
|Related Endothelin Receptor Products|
Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.
Bosentan is an endothelin (ET) receptors antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.
Macitentan is an orally-active, tissue-targeting dual ET receptor antagonist.
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