UCB-9260
目录号: PL11957 纯度: ≥99%
CAS No. :1515888-53-5
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中文名称
UCB-9260
英文名称
UCB-9260
英文别名
UCB-9260;s3231;[1-[(2,5-dimethylphenyl)methyl]-6-(1-methylpyrazol-4-yl)benzimidazol-2-yl]-pyridin-4-ylmethanol;BDBM50552392
Cas No.
1515888-53-5
分子式
C26H25N5O
分子量
423.51
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
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。
生物活性
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 K d  of 13?nM.
性状
Solid
体外研究(In Vitro)
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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
UCB-9260 (150?mg/kg; p.o.;twice daily for 7 days) shows a significant reduction of the clinical score.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. OConnell 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.
溶解度数据
In Vitro: DMSO : 125 mg/mL (295.15 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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