| Bioactivity | UCB-9260, an orally active compound, inhibits TNF signaling by stabilising an asymmetric form of the trimer. UCB-9260 is selective for TNF over other superfamily members, and binds TNF with a similar Kd of 13 nM[1]. | |||||||||
| Invitro | UCB-9260 (0-10 μM) inhibits NF-κB with a geometric mean IC50 of 202 nM after TNF (10 pM) stimulation in in Hek-293 cells[1].UCB-9260 inhibits TNF-dependent cytotoxicity with a geometric mean IC50 of 116 nM and a geometric mean IC50 of 120 nM, using human and mouse TNF, respectively[1]. | |||||||||
| In Vivo | UCB-9260 (150 mg/kg; p.o.;twice daily for 7 days) shows a significant reduction of the clinical score[1].UCB-9260 (10-300 mg/kg; p.o.) dose-dependently inhibits human and mouse TNF-induced neutrophil recruitment to the peritoneal compartment in adult male Balb/c mice[1]. Animal Model: | |||||||||
| Name | UCB-9260 | |||||||||
| CAS | 1515888-53-5 | |||||||||
| Formula | C26H25N5O | |||||||||
| Molar Mass | 423.51 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. O'Connell J, et al.Small molecules that inhibit TNF signalling by stabilising an asymmetric form of the trimer.Nat Commun. 2019 Dec 19;10(1):5795. |