Glucocorticoid receptor agonist

小分子

糖皮质激素受体激动剂

Glucocorticoid receptor agonist

G656320-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

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 Vitro Glucocorticoid 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 Vivo Glucocorticoid 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.

糖皮质激素受体激动剂是一种糖皮质激素受体激动剂，作用于糖皮质激素受体（GR）、孕酮受体（PR）和矿质类固醇受体（MR），IC 50 值分别为 2.1、1200 和 210 nM。糖皮质激素

1245526-82-2(DMSO)

C20H20F4N2O2

396.38 g/mol

CC(C)(CC(CC1=CC2=C(N1)C=NC=C2)(C(F)(F)F)O)C3=C(C=CC(=C3)F)O