產品描述: CaCCinh-A01 is an inhibitor of both TMEM16A and calcium-activated chloride channel (CaCC) with IC50s of 2.1 and 10 μM, respectively. |
靶點:
IC50: 2.1 μM (TMEM16A), 10 μM (CaCC);Chloridechannel |
體外研究:
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 |
體內研究:
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. |
參考文獻:
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 |
保存條件:
-20℃ |
配置溶液濃度參考:
|
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: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |