Glucocorticoid receptor agonist_product_DataBase

Bioactivity

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].

Invitro

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

Name

Glucocorticoid receptor agonist

CAS

1245526-82-2

Formula

C20H20F4N2O2

Molar Mass

396.38

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Doris Riether, et al. Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics. J Med Chem. 2010 Sep 23;53(18):6681-98.

PeptideDB

Glucocorticoid receptor agonist

CAS: 1245526-82-2 F: C20H20F4N2O2 W: 396.38