Description
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.
Product information
CAS Number: 669073-68-1
Molecular Weight: 476.45
Formula: C24H23F3N2O5
Chemical Name: 4-(2,3-dihydro-1-benzofuran-7-yl)-2-hydroxy-4-methyl-N-(4-methyl-1-oxo-1H-2,3-benzoxazin-6-yl)-2-(trifluoromethyl)pentanamide
Smiles: CC(C)(CC(O)(C(=O)NC1=CC2=C(C=C1)C(=O)ON=C2C)C(F)(F)F)C1=CC=CC2CCOC=21
InChiKey: VRZVKIJRJRBQJT-UHFFFAOYSA-N
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
In human peripheral blood mononuclear cells (PBMCs), ZK 216348 inhibits TNF-α and IL-12 with IC50 of 89 nM and 52 nM, respectively. Participation of an active GR in the antiinflammatory response of ZK 216348 is further investigated in Caco-2 cells, where the TNF-α-induced expression of the proinflammatory cytokine IL-8 is suppressed in the presence of ZK 216348.
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.
Products are for research use only. Not for human use.
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