CaCCinh-A01 is an inhibitor of both TMEM16A and calcium-activated chloride channel (CaCC) with IC50s of 2.1 and 10 μM, respectively.
IC50&Target
IC50: 2.1 μM (TMEM16A), 10 μM (CaCC)
体外研究
30 μM CaCCinh-A01 and 100 μM tannic acid strongly inhibit CaCC current following ATP stimulation. 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.
分子式
C18H21NO4S
分子量
347.43
CAS号
407587-33-1
运输条件
Room temperature in continental US; may vary elsewhere.