| 产品描述： | CI 976 is a potent orally active and selective ACAT inhibitor(IC50: 73 nM) and a potent lysophospholipid acyltransferase(LPAT) inhibitor. CI 976 inhibits Golgi-associated LPAT activity (IC50: 15 μM) and multiple membrane trafficking steps |
| 靶点： |
ACAT:73 nM, Golgi-associated LPAT:15 μM;Acyltransferase |
| 体外研究： |
In the chronic cholesterol-fed rat model, CI 976 decreases non-high density lipoprotein (HDL)-cholesterol and increases HDL-cholesterol in rats with pre-established dyslipidemia |
| 体内研究： |
PD 128042 (CI 976) (10-30 mg/kg; gavage, in the chronic cholesterol-fed rat model) decreases non-high density lipoprotein (HDL)-cholesterol and increases HDL-cholesterol in rats with pre-established dyslipidemia. |
| 参考文献： |
1. Chambers K, et al. A unique lysophospholipid acyltransferase (LPAT) antagonist, CI-976, affects secretory and endocytic membrane trafficking pathways. J Cell Sci. 2005;118(Pt 14):3061-3071. 2. O'Brien PM, et al. Inhibitors of acyl-CoA:cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 8. Incorporation of amide or amine functionalities into a series of disubstituted ureas and carbamates. Effects on ACAT inhibition in vitro and efficacy in vivo. J Med Chem. 1994;37(12):1810-1822. 3. Drecktrah D, et al. Inhibition of a Golgi complex lysophospholipid acyltransferase induces membrane tubule formation and retrograde trafficking. Mol Biol Cell. 2003;14(8):3459-3469. 4. Krause BR, et al. In vivo evidence that the lipid-regulating activity of the ACAT inhibitor CI-976 in rats is due to inhibition of both intestinal and liver ACAT. J Lipid Res. 1993;34(2):279-294. |
| 溶解性： |
Soluble in DMSO、Ethanol、DMF |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.541 ml |
12.705 ml |
25.409 ml |
| 5 mM |
0.508 ml |
2.541 ml |
5.082 ml |
| 10 mM |
0.254 ml |
1.27 ml |
2.541 ml |
| 50 mM |
0.051 ml |
0.254 ml |
0.508 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
