S89027 |
CaCCinh-A01 |
源叶(MedMol) | 98% |
- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)