| Identification | Back Directory | [Name]
Glucocorticoid receptor agonist | [CAS]
1245526-82-2 | [Synonyms]
Glucocorticoid receptor agonist
1H-Pyrrolo[2,3-c]pyridine-2-ethanol, α-[2-(5-fluoro-2-hydroxyphenyl)-2-Methylpropyl]-α-(trifluoroMethyl)-, (αR)-
(ALPHAR)-ALPHA-[2-(5-FLUORO-2-HYDROXYPHENYL)-2-METHYLPROPYL]-ALPHA-(TRIFLUOROMETHYL)-1H-PYRROLO[2,3-C]PYRIDINE-2-ETHANOL
alpha-[2-(5-Fluoro-2-hydroxyphenyl)-2-methylpropyl]-alpha-(trifluoromethyl)-(alphaR)-1H-pyrrolo[2,3-c]pyridine-2-ethanol | [Molecular Formula]
C20H20F4N2O2 | [MOL File]
1245526-82-2.mol | [Molecular Weight]
396.38 |
| Chemical Properties | Back Directory | [Boiling point ]
563.1±50.0 °C(Predicted) | [density ]
1.373 | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Powder | [pka]
10.16±0.43(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
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 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 |
| [storage]
Store at -20°C | [References]
[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. DOI:10.1021/jm100751q |
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