| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S87955-5mg |
≥98% | ￥660.00 |
货期：3-5天 | - | - | - | - |
|
S87955-10mg |
≥98% | ￥1070.00 |
货期：3-5天 | - | - | - | - |
|
S87955-25mg |
≥98% | ￥1980.00 |
货期：3-5天 | - | - | - | - |
|
S87955-50mg |
≥98% | ￥3300.00 |
货期：3-5天 | - | - | - | - |
|
S87955-100mg |
≥98% | ￥4730.00 |
货期：3-5天 | - | - | - | - |
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| 产品描述： | Brepocitinib (PF-06700841) P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. Brepocitinib P-Tosylate also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively | ||||||||||||||||||||
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| 靶点： | JAK1:17 nM (IC50);JAK2:77 nM (IC50);JAK3:6.9 μM (IC50);JAK | ||||||||||||||||||||
| 体外研究： | Brepocitinib (Compound 23) potently inhibits TYK2/JAK2 mediated IL-12/pSTAT4 and IL-23/pSTAT3 (human whole blood (HWB) IC50s of 65 and 120 nM, respectively). Brepocitinib has good potency against IL6/pStat1 in the CD3+ cellular subset (IC50 of 81 nM), but lower inhibition of IL6/pSTAT3, again in the CD3+ cellular subset (IC50 of 641 nM). Brepocitinib also inhibits the JAK1/JAK3 driven γ-common chain cytokines, represented by IL-15/pStat5 and IL-21/pSTAT3 with reasonable potency (HWB IC50s of 238 and 204 nM, respectively). Brepocitinib inhibits EPO/pSTAT5 (JAK2 homodimer) in HWB spiked with CD34+ progenitor cells (IC50 of 577 nM). IL10/pSTAT3 (TYK2/JAK1) and IL27/pSTAT3 (JAK1/JAK2/TYK2) are also inhibited by Brepocitinib with IC50s of 305 nM and 86 nM, respectively | ||||||||||||||||||||
| 体内研究： | Brepocitinib (Compound 23; 3-30 mg/kg; oral administration; for 7 consecutive days; female Lewis rats) treatment significantly reduces paw volume increase in a dose-dependent manner. The plasma concentrations in animals dosed with Brepocitinib at peak (30 min) and trough (24 h) time intervals post final dose respectively are as follows: 3 mg/kg, 3.54 μM, 0.0221 μM; 10 mg/kg, 10.95 μM, 0.06 μM; and 30 mg/kg, 23.89 μM, 0.06 μM. Animal Model: Female Lewis rats with induced arthritis Dosage: 3 mg/kg, 10 mg/kg, or 30 mg/kg Administration: Oral administration; for 7 consecutive days Result: Increased in paw volume was significantly lower and dose-dependent. | ||||||||||||||||||||
| 参考文献： | 1. Fensome A, et al. Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841). J Med Chem. 2018 Oct 11;61(19):8597-8612. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20°C | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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