货号	规格	价格	上海	北京	珠海	重庆	武汉
V45575-5mg	≥98%	￥980.00 V45575-5mg ￥980.00 3-5天	0 货期：3-5天	-	-	-	-
V45575-10mg	≥98%	￥1580.00 V45575-10mg ￥1580.00 3-5天	0 货期：3-5天	-	-	-	-
V45575-25mg	≥98%	￥3480.00 V45575-25mg ￥3480.00 3-5天	0 货期：3-5天	-	-	-	-
V45575-50mg	≥98%	￥5580.00 V45575-50mg ￥5580.00 3-5天	0 货期：3-5天	-	-	-	-
V45575-100mg	≥98%	￥8950.00 V45575-100mg ￥8950.00 3-5天	0 货期：3-5天	-	-	-	-

大包装询价收藏产品

加入购物车

到货通知，提交手机号入库后将短信通知。

产品描述：

GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC50=7.1). GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.

体外研究：

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[3].
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[2].
GSK143 (iv of 1 mg/kg; po of 3 mg/kg) has a T1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a Vss of 4.1 L/kg in rats[1].

体内研究：

GSK143 dihydrochloride (compound 20) inhibits ZAP-70 (pIC50=4.7), LCK (pIC50=5.3), LYN (pIC50=5.4), JAK1/2/3 (pIC50=5.8/5.8/5.7), Aurora B (pIC50=4.8), hWB (pIC50=6.6), hERG (pIC50=4.7).
GSK143 dihydrochloride (10-10000 nM; every 24 hours for 3 days) has an IC50 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.

参考文献：

1. John Liddle, et al. Discovery of GSK143, a Highly Potent, Selective and Orally Efficacious Spleen Tyrosine Kinase Inhibitor. Bioorg Med Chem Lett. 2011 Oct 15;21(20):6188-94.
2. Abraham M Varghese, et al. Highly Selective SYK Inhibitor, GSK143, Abrogates Survival Signals in Chronic Lymphocytic Leukaemia. Br J Haematol. 2018 Sep;182(6):927-930.
3. Sjoerd H W van Bree, et al. Inhibition of Spleen Tyrosine Kinase as Treatment of Postoperative Ileus. Gut. 2013 Nov;62(11):1581-90.

保存条件：

2-8°C, 避光, 干燥

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.408 ml	12.039 ml	24.078 ml
5 mM	0.482 ml	2.408 ml	4.816 ml
10 mM	0.241 ml	1.204 ml	2.408 ml
50 mM	0.048 ml	0.241 ml	0.482 ml

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。

参考文献

质检证书(COA)

输入产品批号：

如何获取质检证书(COA)?

请输入货号和一个与之匹配的批号。
例如:
批号：JS298415 货号：S20001-25g
在货品标签上如何找到货号和批号?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置