P-1075

Research use only, not for human use.

P-1075 is a potent sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6) activator (EC50 = 45 nM).

P-1075 is a potent sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6) activator (EC50 = 45 nM). P-1075 opens opens mitoKATP channels and may be cardioprotective.

P1075 (3 nM) induces monophasic inhibition curves by competition-binding experiments, in the presence of MgATP.P1075 (100 μM; 10 min) leads to rabbit cardiomyocytes to produce ROS in a KATP-dependent fashion.P1075 (150 nM) reduces infarct size in isolated rabbit hearts compared to control animals (10.6% of the area at risk vs. 31.5%, P < 0.05). Cell Viability Assay Cell Line:COS-7 cells Concentration:3-15 nM Incubation Time:Result:Showed IC50 value of 15 nM and Hill coefficient of 1.0.Cell Viability Assay Cell Line:Adult rabbit cardiomyocytes Concentration:100 μM Incubation Time:10 min Result:Led to a 44% increase in ROS generation (P<0.001 vs. untreated cells).

P1075 (intravenous injection; 1μg/kg; once) treatment shows the reduction of infarct size in ischemia model. Animal Model:Male Sprague-Dawley rats subjected to 30 minutes of ischemia and 2 hours of reperfusion Dosage:1μg/kg Administration:Intravenous injection; 1μg/kg; once Result:Reduced infarct size (41.8%) compared to the vehicle.

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Cell Cycle/DNA Damage

Potassium Channel

Human Endogenous Metabolite

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60559-98-0

231.303

C12H17N5

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (1080.85 mM)

CCC(C)(C)N\C(NC#N)=N\c1cccnc1

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(-20℃)

With Ice Pack

≥ 2 years