计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
2-8°C储存,避光,干燥。低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC 50 of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC 50 =7.1) GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice
In Vitro
GSK143 dihydrochloride (compound 20) inhibits ZAP-70 (pIC 50 =4.7), LCK (pIC 50 =5.3), LYN (pIC 50 =5.4), JAK1/2/3 (pIC 50 =5.8/5.8/5.7), Aurora B (pIC 50 =4.8), hWB (pIC 50 =6.6), hERG (pIC 50 =4.7). GSK143 dihydrochloride (10-10000 nM; every 24 hours for 3 days) has an IC 50 of 323 nM in CLL cells. GSK 143 dihydrochloride (1 μM; 30 mins) abrogates early signalling events including SYK phosphorylation and calcium flux. GSK143 dihydrochloride (0.1-10 μM; for 30 min) reduces cytokine expression in bone marrow derived macrophages in a concentration-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Chronic lymphocytic leukaemia (CLL) cells Concentration: 10, 100, 1000, 10000 nM Incubation Time: Every 24 hours for 3 days Result: Had an IC 50 of 323 nM.
In Vivo
GSK143 (0.1-10 mg/kg; orally; 1.5 hours) reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis of 1 mg/kg. GSK143 (3, 10, 30, 100 mg/kg; oral; 1 hour before ovalbumin challenge) reduces the cutaneous reverse passive Arthus reaction in a dose dependent manner by approximately 50% and 70% at 10 mg/kg and 30 mg/kg, respectively. GSK143 (iv of 1 mg/kg; po of 3 mg/kg) has a T 1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a V ss of 4.1 L/kg in rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Wild type C57NL/BL6 mice, 10-12 weeks oldDosage: 0.1, 1, 3, 10 mg/kg Administration: Orally; 1.5 hours before intestinal manipulation (IM) Result: Reduced inflammation and prevented recruitment of immune cells in the intestinal muscularis. Animal Model: Male CD rats (175-200 g) Dosage: 1 mg/kg of iv; 3 mg/kg of po (Pharmacokinetic Analysis) Administration: IV or PO Result: Had a T 1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a V ss of 4.1 L/kg.
Form:Solid
IC50& Target:pIC50: 7.5 (SYK) and 7.1 (pErk)
规格
别名
GSK143 二盐酸盐
规格或纯度
≥99%
英文名称
GSK143 dihydrochloride
生化机理
GSK143 二盐酸盐是一种口服活性高选择性脾酪氨酸激酶（SYK）抑制剂，pIC 50 为 7.5。GSK143 二盐酸盐可抑制磷酸化的 Erk（pErk：pIC 50 =7.1）。GSK143 二盐酸盐可减轻炎症反应并预防心肌梗死。
储存条件
2-8°C储存,避光,干燥
运输条件
低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
415.32
技术文档
高级数据
化学和物理性质
溶解性
H2O : 100 mg/mL (240.78 mM; Need ultrasonic) DMSO : ≥ 50 mg/mL (120.39 mM)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品的纯度是多少？
本产品的化学纯度（含量）为 ≥99%。批次的具体数值以分析证书（COA）为准。
本产品应如何储存？
请于2–8 °C、避光、干燥条件下保存。请与干燥剂一同密封保存，本品对湿气敏感。
本产品如何运输？
本产品采用湿冰冷藏运输。收货后请立即拆包，并按上述储存条件保存。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 2341796-81-2，分子式为 C17H24Cl2N6O2，分子量为 415.32 g/mol。
如何获取批次专用COA？
每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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