在線訂購 免費訂購熱線:021-59541103 021-60443211
標簽:PF-06651600
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q: 3004967995
Email:3004967995@qq.com
詳細地址:上海嘉定區嘉羅公路1661
化學性質:
規格 | 5mg 10mg 25mg 50mg |
CAS | 1792180-81-4 |
別名 | N/A |
化學名 | N/A |
分子式 | C15H19N5O |
分子量 | 285.34 |
溶解度 | DMSO : 150 mg/mL (525.69 mM) |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
PF-06651600 is a potent JAK3-selective inhibitor with an IC50 of 33.1 nM.
PF-06651600 is a potent JAK3-selective inhibitor which can inhibit the JAK3 kinase activity with an IC50 of 33.1 nM but without activity (IC50>10.000 nM) against JAK1, JAK2, and TYK2. PF-06651600 inhibits the phosphorylation of STAT5 elicited by IL-2, IL-4, IL-7, and IL-15 with IC50 values of 244, 340, 407, and 266 nM, respectively. PF-06651600 also inhibits the phosphorylation of STAT3 elicited by IL-21 with an IC50 of 355 nM. Functional assessment in T-cell differentiation assays demonstrate that PF-06651600 suppresses Th1 and Th17 differentiation as measured by IFNγ, after 5 days under Th1 conditions, and IL-17 production, after 6 days under Th17 conditions, with IC50 values of 30 nM and 167 nM, respectively. PF-06651600 also suppresses Th1 and Th17 function as measured by the inhibition of IFNγ production (IC50=48 nM) and IL-17 production (IC50=269 nM) in cells that have been previously differentiated and rested before being treated with PF-06651600[1].
In the rat adjuvant-induced arthritis (AIA) model, PF-06651600 reduces paw swelling with an unbound EC50 of 169 nM. Similarly, PF-06651600 significantly reduces disease severity in the experimental autoimmune encephalomyelitis (EAE) mouse model when dosed either therapeutically at 30 or 100 mg/kg or prophylactically at 20 and 60 mg/kg. The efficacy of PF-06651600 in these two rodent models of inflammatory and autoimmune diseases illustrates that JAK3-selective inhibition can be sufficient to have disease modifying effects in human diseases[1].
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原創作者:上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業部
賬 號:2169 2341 6278