| 产品描述： | CaCCinh-A01 is an inhibitor of both TMEM16A and calcium-activated chloride channel (CaCC) with IC50s of 2.1 and 10 μM, respectively. |
| 靶点： |
IC50: 2.1 μM (TMEM16A), 10 μM (CaCC);Chloridechannel |
| 体外研究： |
30 μM CaCCinh-A01 and 100 μM tannic acid strongly inhibit CaCC current following ATP stimulation[1]. Calcium-dependent chloride current is reduced by 38±14, 66±10, and 91±1% by 0.1, 1, and 10 μM CaCCinh-A01, respectively. ATP-induced short-circuit currents are reduced by 38±7 and 78±3% at 10 and 30 μM CaCCinh-A01, respectively |
| 体内研究： |
CaCCinh-A01 (vein injection; 5 mg/kg; caudal vein injection within 15 min after the onset of reperfusion) significantly reduces infarction when compared with MCAO-saline treatment at 24 h or 72 h in middle cerebral artery occlusion model in mice. Animal Model: Two-month-old male C57/BL6J mice Dosage: 5 mg/kg Administration: Vein injection; 5 mg/kg; caudal vein injection within 15 min after the onset of reperfusion Result: Attenuated brain infarct size, improved neurological outcomes and lowered BBB permeability after ischemic stroke in mice. |
| 参考文献： |
1. TMEM16A inhibitors reveal TMEM16A as a minor component of calcium-activated chloridechannel conductance in airway and intestinal epithelial cells. J Biol Chem. 2011 Jan 21;286(3):2365-74. 2. De La Fuente R, et al. Small-molecule screen identifies inhibitors of a human intestinal calcium-activated chloridechannel. Mol Pharmacol. 2008 Mar;73(3):758-68. 3. Pin-Yi Liu, et al. TMEM16A Inhibition Preserves Blood-Brain Barrier Integrity After Ischemic Stroke.Front Cell Neurosci. 2019 Aug 6;13:360. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.878 ml |
14.391 ml |
28.783 ml |
| 5 mM |
0.576 ml |
2.878 ml |
5.757 ml |
| 10 mM |
0.288 ml |
1.439 ml |
2.878 ml |
| 50 mM |
0.058 ml |
0.288 ml |
0.576 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)
北京