Glucocorticoid receptor agonist

Glucocorticoid receptor agonist is a Glucocorticoid receptor agonist that acts on Glucocorticoid receptor (GR), progesterone receptor (PR) and mineralocorticoid receptor (MR) with the IC₅₀ 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^[1].
In Vitro:Glucocorticoid receptor agonist ((R)-16) has effect on IL-6 and MMTV with the IC₅₀ values of 3.3 and 80 nM, respectively, also has effect on aromatase with the EC₅₀ value of 11 nM^[1].
In Vivo:Glucocorticoid receptor agonist ((R)-16) exhibits good pharmacokinetic properties in Sprague-Dawley rats^[1].
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^[1].
The pharmacokinetic parameters of Glucocorticoid receptor agonist ((R)-16) in Sprague-Dawley rat (5 mg/kg i.v. or 30 mg/kg p.o.)^[1].

Parameters	Cl (i.v.)(mL/min/kg)	VSS(iv) (L/kg)	T1/2(iv)(h)	Cmax(po) (ng/mL)	AUCinf(po) (h·ng/mL)	F(po)%
(R)-16	49	7.6	1.85	509	4879	48