PF-6870961 hydrochloride is a potent inverse agonist of GHSR1a, exhibiting Ki values of 73.6 nM for human GHSR, 239 nM for rat GHSR, and 217 nM for dog GHSR. It effectively inhibits GHSR1a-induced inositol phosphate (IP) accumulation with an IC50 of 300 nM and demonstrates a strong inhibition of constitutive GHSR1a β-arrestin mobilization with an IC50 of 1.10 nM. This compound is relevant for research applications exploring the physiological roles of GHSR1a in metabolic and neuroendocrine processes.
PF-6870961 hydrochloride is a potent inverse agonist of GHSR1a, exhibiting Ki values of 73.6 nM for human GHSR, 239 nM for rat GHSR, and 217 nM for dog GHSR. It effectively inhibits GHSR1a-induced inositol phosphate (IP) accumulation with an IC50 of 300 nM and demonstrates a strong inhibition of constitutive GHSR1a β-arrestin mobilization with an IC50 of 1.10 nM. This compound is relevant for research applications exploring the physiological roles of GHSR1a in metabolic and neuroendocrine processes.
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