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(+)-ZK 216348

Axon 2239
CAS:  669073-68-1
  • Optical Purity:  99.8%
  • Soluble in DMSO
  • MF:  C24H23F3N2O5
  • MW:  476.45

Description

Selective nonsteroidal glucocorticoid receptor (GR) agonist for the treatment of experimental colitis with IC50 values of 20, 20, and 80 nM for GR, Progesterone (PR) and Mineralocorticoid (MR) receptors respectively. (+)-ZK 216348 shows antiinflammatory activity comparable to prednisolone for both systemic and topical application, with a significant dissociation between transrepression and transactivation of antiinflammatory effects both in vitro and in vivo.(+)-ZK 216348 showed no negative effects on intestinal epithelial migration or proliferation. (-)-ZK 216348 is completely inactive (IC50 >1000 nM for GR, PR, and MR.

More Information

Parent CAS No. 669073-68-1
Chemical Name (+)-4-(2,3-dihydrobenzofuran-7-yl)-2-hydroxy-4-methyl-N-(4-methyl-1-oxo-1H-benzo[d][1,2]oxazin-6-yl)-2-(trifluoromethyl)pentanamide
SMILES O1C2=C(C(C)(C)CC(C(F)(F)F)(O)C(NC3=CC=C4C(=O)ON=C(C)C4=C3)=O)C=CC=C2CC1
MFCD N.A.
InChi InChI=1S/C24H23F3N2O5/c1-13-17-11-15(7-8-16(17)20(30)34-29-13)28-21(31)23(32,24(25,26)27)12-22(2,3)18-6-4-5-14-9-10-33-19(14)18/h4-8,11,32H,9-10,12H2,1-3H3,(H,28,31)
InChiKey VRZVKIJRJRBQJT-UHFFFAOYSA-N
CID 9805004
Short Description Glucocorticoid agonist

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