(+)-ZK 216348
(+)-ZK 216348 Basic information
- Product Name:
- (+)-ZK 216348
- Synonyms:
-
- (+)-ZK 216348
- 7-Benzofuranbutanamide, 2,3-dihydro-α-hydroxy-γ,γ-dimethyl-N-(4-methyl-1-oxo-1H-2,3-benzoxazin-6-yl)-α-(trifluoromethyl)-, (+)-
- CAS:
- 669073-68-1
- MF:
- C24H23F3N2O5
- MW:
- 476.45
- Mol File:
- 669073-68-1.mol
(+)-ZK 216348 Chemical Properties
- Density
- 1.39±0.1 g/cm3(Predicted)
- pka
- 10.33±0.29(Predicted)
- form
- Solid
- color
- White to off-white
(+)-ZK 216348 Usage And Synthesis
Uses
ZK 216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC50s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects[1][2].
in vivo
ZK 216348 (1-30 mg/kg; subcutaneous injection; for 24 hours; NMRI mice and Wistar rats) treatment inhibits ear edema in both mice and rats. A markedly superior side-effect profile is found in ZK 216348 with regard to increases in blood glucose, spleen involution, and, to a lesser extent, skin atrophy[1].
| Animal Model: | NMRI mice (26-28 g) and Wistar rats (140-160 g) injection with Croton oil[1] |
| Dosage: | 1 mg/kg, 3 mg/kg, 10 mg/kg and 30? mg/kg |
| Administration: | Subcutaneous injection; for 24 hours |
| Result: | Inhibited ear edema in mice and rats. |
References
[1] Sch?cke H, et al. Dissociation of transactivation from transrepression by a selective glucocorticoid receptor agonist leads to separation of therapeutic effects from side effects. Proc Natl Acad Sci U S A. 2004 Jan 6;101(1):227-32. DOI:10.1073/pnas.0300372101
[2] Reuter KC, et al. Selective glucocorticoid receptor agonists for the treatment of inflammatory bowel disease: studies in mice with acute trinitrobenzene sulfonic acid colitis. J Pharmacol Exp Ther. 2012 Apr;341(1):68-80. DOI:10.1124/jpet.111.183947
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