betaARK1 Inhibitor

betaARK1 inhibitor is an inhibitor of G protein-coupled receptor kinase 2/beta-adrenergic receptor kinase 1 (GRK2/betaARK1, IC50 = 126 µM). It is selective for GRK2/betaARK1 over PKA at concentrations up to 1 mM. betaARK1 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. It also improves clonidine-induced relaxation of precontracted isolated aortic rings and improves glucose tolerance in the ob/ob mouse model. betaARK1 inhibitor inhibits dopamine inhibition reversal (DIR) induced by serotonin (Cay-14332) or neurotensin (Cay-24717) in the rat ventral tegmental area in vitro.Formal Name: 5-[2-(5-nitro-2-furanyl)ethenyl]-2-furancarboxylic acid, methyl ester. CAS Number: 24269-96-3. Molecular Formula: C12H9NO6. Formula Weight: 263.2. Purity: >95% (mixture of isomers). Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/mL, DMSO: 30 mg/mL, DMSO:PBS (pH 7.2) (1:2): 0.3 mg/mL, Ethanol: slightly soluble. lambdamax: 228, 298, 395 nm. SMILES: COC(C1=CC=C(/C=C/C2=CC=C([N+]([O-])=O)O2)O1)=O. InChi Code: InChI=1S/C12H9NO6/c1-17-12(14)10-6-4-8(18-10)2-3-9-5-7-11(19-9)13(15)16/h2-7H,1H3/b3-2+. InChi Key: YDJPHSNZGRVPCK-NSCUHMNNSA-N.