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CAS No. : 1245526-82-2
MCE 国际站:Glucocorticoid receptor agonist
产品活性:Glucocorticoid receptor agonist 是 Glucocorticoid 受体激动剂,作用于 Glucocorticoid receptor (GR)、progesterone receptor (PR) 和 mineralocorticoid receptor (MR) 的 IC50 值分别为 2.1nM, 1200 和 210 nM。Glucocorticoid receptor agonist 具有类固醇样抗炎特性,可用于改善代谢,减少体脂和血清胰岛素的增加水平。
研究领域:Immunology/Inflammation | Vitamin D Related/Nuclear Receptor
作用靶点:Glucocorticoid Receptor
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.
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) | 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 |
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