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UCB-9260
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
UCB-9260图片
CAS NO:1515888-53-5
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议

产品介绍

UCB-9260 是一种口服活性小分子,通过稳定三聚体的不对称形式抑制肿瘤坏死因子 (TNF) 信号传导。UCB-9260 对肿瘤坏死因子的选择性高于其他超家族成员,并与肿瘤坏死因子结合,其 Kd 值为 13 nM。

Cas No.1515888-53-5
分子式C26H25N5O
分子量423.51
溶解度DMSO : 125 mg/mL (295.15 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
文献引用
产品描述

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].

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].

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].

[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.