воскресенье, 20 января 2008 г.

5-(3-cyclopentyl-2-thioxo-2,3-dihydro-1h-benzimidazol-5-yl)-1-methyl-1h-pyrrole-2-carbonitrile: a novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist.

PubMed d‚nouement develop A professional care of the and the Search PubMedProteinNucleotideCoreNucleotideGSSESTStructureGenomeBooksCancerChromosomesConserved DomainsdbGaP3D DomainsGeneGenome ProjectGENSATGEO ProfilesGEO DataSetsHomoloGeneJournalsMeSHNCBI network SiteNLM CatalogOMIAOMIMPMCPopSetProbeProtein ClustersPubChem BioAssayPubChempoundPubChem SubstanceSNPTaxonomyToolKitUniGeneUniSTS on GO perceptive , , , , , , , , , , , , .Screening Sciences, Wyeth enquiry S-2250B, 500 Arcola carriageway Collegeville, PA 19426, USA.Clothed recently discovered 5-(3-cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (14) as a efficacious demanding and orally quick non-steroidal progesterone receptor (PR) agonist.And its analog 13 sub-nanomolar in vitro potency (EC(50) 0.In the T47D alkaline phosphatase assay, alike resemble to that of the steroidal PR agonist medroxyprogesterone acetate (MPA).Disparity to MPA, 14 was enthusiastically demanding (>500-fold) on the PR remaining both glucocorticoid and androgen receptors.The rat uterine decidualization andplementponent C3 models, 14 had vocalized ED(50) values of 0.0.Severally and was from 6- to 20- clasp more efficacious than MPA.
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