UCB9608
产品说明书
 |
同义名 : | - |
| CAS号 : | 1616413-96-7 | |
| 货号 : | A789351 | |
| 分子式 : | C20H26N8O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 410.473 | |
| MDL号 : | MFCD01744844 | |
| 存储条件： |
Pure form Keep in dark place,Inert atmosphere,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 65 mg/mL(158.35 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The phosphatidylinositol 4-kinases (PI4Ks) play prominent roles in compartment identity. PI4KIIIβ is one of four mammalian PI4K enzymes that phosphorylate phosphatidylinositol to generate phosphatidylinositol 4-phosphate (PI4P). PI4KIIIβ localizes primarily at the Golgi and is essential for Golgi formation and function. PI4KIIIβ activity is essential for replication of a range of RNA viruses, including enteroviruses, SARS coronavirus, and hepatitis C virus[1]. UCB9608 is a potent, selective and orally active PI4KIIIβ inhibitor, with an IC50 value of 11 nM. UCB9608 is selective for PI4KIIIβ over PI3KC2 α, β, and γ lipid kinases. UCB9608 inhibits human mixed lymphocyte reaction, with an IC50 value of 37 nM. UCB9608 improves metabolic stability and exhibits excellent pharmacokinetic profile, acts as a potent immunosuppressive agent[2]. UCB9608 had very low CLb, commensurate with its low CLint in MLM, leading to a half-life of 1.4 h, with high bioavailability, and low inter-individual variability. UCB9608 could achieve high and consistently reproducible exposures in Balb/C mice. It could also prevent the rejection of a heterotopic murine cardiac allograft at a dose of 5 mpk. The excellent ADME properties of UCB9608 make it an ideal molecule to develop the understanding of the role of this novel class of PI4KIIIβ inhibitors on immune cell activation[2]. | ||
| 作用机制 | The amino pyrimidine of UCB9608 makes a bidentate interaction with the Val613 backbone. The urea NH and carbonyl of UCB9608 form H-bonds with the main-chain Gly675 carbonyl and the side-chain NH2 of Asn390 respectively. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.44mL 0.49mL 0.24mL |
12.18mL 2.44mL 1.22mL |
24.36mL 4.87mL 2.44mL |
| 参考文献 |
|---|