
AS-041164PI3Kγ inhibitor |
Sample solution is provided at 25 µL, 10mM.
































Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure


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Cas No. | 6318-41-8 | SDF | Download SDF |
Chemical Name | 5-(1,3-benzodioxol-5-ylmethylene)-2,4-thiazolidinedione | ||
Canonical SMILES | O=C(/C(S1)=C/C2=CC=C3C(OCO3)=C2)NC1=O | ||
Formula | C11H7NO4S | M.Wt | 249.2 |
Solubility | ≤25mg/ml in DMSO;25mg/ml in dimethyl formamide | Storage | Store at -20°C |
Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
AS-041164 is a potent and selective PI3Kγ inhibitor with IC50 value of 0.07 μM [1].
The phosphatidylinositol 3-kinases (PI3Ks) are a family of lipid and protein kinases regulating numerous biological processes, including cell growth, differentiation, survival, proliferation, migration and metabolism. PI3Kγ, a unique member of class IB, is activated exclusively by G-protein coupled receptor (GPCRs) and can specifically bind to adaptors unrelated to p85 proteins [2].
AS-041164 is a highly potent and selective PI3Kγinhibitor that inhibits PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ with IC50 values of 240 nM, 1.45 μM, 70 nM and 1.70 μM, respectively [1].
In mice, orally administration of AS-041164 dose-dependently decreased r-hRANTES-induced neutrophil recruitment with ED50 value of 27.35 mg/kg. AS-041164 (30 mg/kg p.o.) also significantly reduced r-hRANTES-induced AKT phosphorylation. In a carrageenan-induced inflammation rat model, AS041164 at the dose of 100 mg/kg p.o significantly reduced paw thickness induced by carrageenan [1].
References:[1]. Ferrandi C, Ardissone V, Ferro P, et al. Phosphoinositide 3-kinase gamma inhibition plays a crucial role in early steps of inflammation by blocking neutrophil recruitment. J Pharmacol Exp Ther. 2007 Sep;322(3):923-30.[2]. Hirsch E, Ciraolo E, Ghigo A, et al. Taming the PI3K team to hold inflammation and cancer at bay. Pharmacol Ther. 2008 May;118(2):192-205.
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要是能上传一些真实药厂设备,也许对大家都有帮助。
下面上传《常用制剂设备》的图扫描。
http://www.k65.net/mail/url.php?n=eXpmMzcyMT0v
code:37217613
比较电泳设备.pdf(425.0k)
常用制药设备的PPT(带彩图).rar(751.71k)
最近要添加一些设备,请教各位大神推荐的厂家及其型号。
需要的设备如下:高速剪切混合机、湿法制粒机、干法制粒机、整粒机、包衣机、胶囊填充机、铝塑包装机。
先谢谢各位大神了
先说出自己这几天学习注射剂的心得:
关于注射剂仿制,先对照原研处方,处方设计尽量和原研一致,通过考察评价外观、色泽、澄明度、pH、含量、有关物质、细菌内毒素或热原、不溶性微粒和稳定性等,确定一个符合标准的相关标准高于原研药的处方。也就是说注射剂仿制就是通过处方和工艺的筛选找出一个满足标准(pH、含量、有关物质、细菌内毒素或热原等)的处方和工艺,这个是不是仿制的基本思路?
而这其中有还很多问题。只有思路还不进行实际研发。
比如处方设计中,一般常用辅料有哪些?
一般在什么情况下需要加入什么特殊的辅料?比如pH调节剂,抑菌剂等。
做研发的实验步骤是如何。有了一个初步的处方,我们第一步是配溶液?还有灭菌、封口这个步骤是怎样的?每一步都用什么设备,有几种工艺可以选,还一般的操作条件如温度速度时间等。
很多细节问题和思路问题,做注射剂的高手和新手们都来说说哦。这是一个开放的交流大家可以说的更远,说出自己的精华。
另外版主给加个积分呗,很多帖子我看不了!!!
下面是我觉得做注射剂必须了解的基本法规链接,给新手看滴,希望有帮助
http://www.sfda.gov.cn/WS01/CL0058/9348.html
关于印发《可见异物检查法补充规定》的通知
http://www.sfda.gov.cn/WS01/CL0055/27800.html
关于发布化学药品注射剂和多组分生化药注射剂基本技术要求的通知
http://www.sfda.gov.cn/WS01/CL0055/24969_9.html
关于开展注射剂类药品生产工艺和处方核查工作的通知

