Glucocorticoid receptor agonist (C09-1135-950)

Glucocorticoid receptor agonist is a Glucocorticoid receptor agonist that acts on Glucocorticoid receptor ( GR ), progesterone receptor ( PR ) and mineralocorticoid receptor ( MR ) with the IC 50 values of 2.1 , 1200 and 210 nM, respectively. Glucocorticoid receptor agonist has steroid-like anti-inflammatory properties and may be used to improve metabolism and reduce increased levels of body fat and serum insulin.In VitroGlucocorticoid receptor agonist ((R)-16) has effect on IL-6 and MMTV with the IC 50 values of 3.3 and 80 nM, respectively, also has effect on aromatase with the EC 50 value of 11 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoGlucocorticoid receptor agonist ((R)-16) exhibits good pharmacokinetic properties in Sprague-Dawley rats . Glucocorticoid receptor agonist ((R)-16) (30 and 10 mg/kg, p.o., daily, 5 weeks) can reduce the increased levels of body fat and serum insulin and shows an effective inhibition of TNF-α production in LPS-stimulated mouse model . The pharmacokinetic parameters of Glucocorticoid receptor agonist ((R)-16) in Sprague-Dawley rat (5 mg/kg i.v. or 30 mg/kg p.o.) . Parameters Cl (i.v.)(mL/min/kg) V SS (iv) (L/kg) T 1/2 (iv)(h) C max (po) (ng/mL) AUC inf (po) (h·ng/mL) F(po)% (R)-16 49 7.6 1.85 509 4879 48 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Specification: 10mM in DMSO Molecular Formula: C20H20F4N2O2 Molecular Weight: 396.38