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编 号:F088986
分子式:C20H20F4N2O2
分子量:396.38
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10mM*1mL in DMSO
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5mg
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10mg
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生物活性:
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.

体内研究:
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.). ParametersCl (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)-16497.61.85509487948

体外研究:
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.
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