Bioactivity | CaCCinh-A01 is an inhibitor of both TMEM16A and calcium-activated chloride channel (CaCC) with IC50s of 2.1 and 10 μM, respectively. | ||||||||||||
Target | IC50: 2.1 μM (TMEM16A), 10 μM (CaCC) | ||||||||||||
Invitro | 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[2]. | ||||||||||||
In Vivo | 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[3]. Animal Model: | ||||||||||||
Name | CaCCinh-A01 | ||||||||||||
CAS | 407587-33-1 | ||||||||||||
Formula | C18H21NO4S | ||||||||||||
Molar Mass | 347.43 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
|
||||||||||||
Reference | [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. |