Tolebrutinib
产品说明书
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同义名 : | SAR442168;PRN2246 |
| CAS号 : | 1971920-73-6 | |
| 货号 : | A1372178 | |
| 分子式 : | C26H25N5O3 | |
| 纯度 : | 97% | |
| 分子量 : | 455.508 | |
| MDL号 : | MFCD32710277 | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(230.51 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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Tolebrutinib, also known as SAR442168, is a potent, selective, orally active and brain-penetrating BTK inhibitor with IC50 values of 0.4 nM and 0.7 nM in Ramos B cells and HMC microglia cells, respectively.Tolebrutinib has shown efficacy against CNS immunity. Tolebrutinib is used in multiple sclerosis (MS) studies[1][2].Tolebrutinib blocks BCR-mediated immune cell activation (IC50=10 nM) and Fc receptor activation (IC50 of 166 and 9.6 nM for FcεR and FcγR, respectively)[2].PRN2246 inhibits microglia FcγR activation through persistent BTK occupancy with an IC50 value of 157 nM[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.20mL 0.44mL 0.22mL |
10.98mL 2.20mL 1.10mL |
21.95mL 4.39mL 2.20mL |
| 参考文献 |
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