An inhibitor of GRK2/βARK1 (IC50 = 126 µM); selective for GRK2/βARK1 over PKA at concentrations up to 1 mM; decreases systolic blood pressure in ob/ob and nicotinamide plus streptozotocin-induced mouse models of type 2 diabetes at 200 µg/kg; improves clonidine-induced relaxation of precontracted isolated aortic rings and improves glucose tolerance in the ob/ob mouse model; inhibits serotonin- or neurotensin-induced DIR in the rat ventral tegmental area in vitro

βARK1 Inhibitor – 5 mg

Brand:
Cayman
CAS:
24269-96-3
Storage:
-20
UN-No:
Non-Hazardous - /

βARK1 inhibitor is an inhibitor of G protein-coupled receptor kinase 2/β-adrenergic receptor kinase 1 (GRK2/βARK1; IC50 = 126 µM).{43745} It is selective for GRK2/βARK1 over PKA at concentrations up to 1 mM. βARK1 inhibitor decreases systolic blood pressure in ob/ob and nicotinamide plus streptozotocin-induced mouse models of type 2 diabetes when administered at a dose of 200 µg/kg.{43746} It also improves clonidine-induced relaxation of precontracted isolated aortic rings and improves glucose tolerance in the ob/ob mouse model. βARK1 inhibitor inhibits dopamine inhibition reversal (DIR) induced by serotonin (Item No. 14332) or neurotensin (Item No. 24717) in the rat ventral tegmental area in vitro.{43747}  

 

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Description

An inhibitor of GRK2/βARK1 (IC50 = 126 µM); selective for GRK2/βARK1 over PKA at concentrations up to 1 mM; decreases systolic blood pressure in ob/ob and nicotinamide plus streptozotocin-induced mouse models of type 2 diabetes at 200 µg/kg; improves clonidine-induced relaxation of precontracted isolated aortic rings and improves glucose tolerance in the ob/ob mouse model; inhibits serotonin- or neurotensin-induced DIR in the rat ventral tegmental area in vitro

Formal name: 5-[2-(5-nitro-2-furanyl)ethenyl]-2-furancarboxylic acid, methyl ester

Synonyms: 

Molecular weight: 263.2

CAS: 24269-96-3

Purity: ≥95% (mixture of isomers)

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Neuroscience

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