A potent activator of SUR2-Kir6 and KATP channels; activates SUR2-Kir6 channels (EC50 = 45 nM for SUR2B-Kir6 channel activation); highly selective for SUR2 over SUR1 isoforms (IC50s = 9-46 nM and 1.02 mM

P1075 – 1 mg

Brand:
Cayman
CAS:
60559-98-0
Storage:
-20
UN-No:
Non-Hazardous - 2811 / 6.1

P1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-Kir6) with an EC50 value of 45 nM for SUR2B-Kir6 channel activation.{38539} It is highly selective for SUR2 over SUR1 isoforms (IC50s = 9-46 nM and 1.02 mM, respectively, in a radioligand binding assay). P1075 increases outflow facility, a marker of reduced intraocular pressure, in human eye anterior segments ex vivo.{38540} It also reduces infarct size in isolated rabbit hearts via activation of mitochondrial ATP-sensitive potassium channels (KATP; EC50s = 60-90 nM).{38541}  

 

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Description

A potent activator of SUR2-Kir6 and KATP channels; activates SUR2-Kir6 channels (EC50 = 45 nM for SUR2B-Kir6 channel activation); highly selective for SUR2 over SUR1 isoforms (IC50s = 9-46 nM and 1.02 mM, respectively, in a radioligand binding assay); increases outflow facility, a marker of reduced intraocular pressure, in human eye anterior segments ex vivo; reduces infarct size in isolated rabbit hearts via activation of mitochondrial KATP channels (EC50s = 60-90 nM)

Formal name: N-cyano-N’-(1,1-dimethylpropyl)-N”-3-pyridinyl-guanidine

Synonyms: 

Molecular weight: 231.3

CAS: 60559-98-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Activators||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cardiovascular System|Cardiovascular Diseases|Myocardial Infarction||Research Area|Neuroscience|Ophthalmology

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