βARK1 Inhibitor (methyl 5-[2-(5-nitro-2-furyl)vinyl]-2-furoate) 是一种 GRK2 (β-ARK1) 抑制剂。
Cas No. |
24269-96-3 |
别名 |
呋喃妥因-13C3 |
Canonical SMILES |
COC(C1=CC=C(/C=C/C2=CC=C([N+]([O-])=O)O2)O1)=O |
分子式 |
C12H9NO6 |
分子量 |
263.2 |
溶解度 |
DMF: 30 mg/mL,DMSO: 30 mg/mL,DMSO:PBS (pH 7.2) (1:2): 0.3 mg/mL,Ethanol: slightly soluble |
储存条件 |
Store at -20°C |
General tips |
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition |
Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
半岛bd体育手机客户端 描述 |
βARK1 inhibitor is an inhibitor of G protein-coupled receptor kinase 2/β-adrenergic receptor kinase 1 (GRK2/βARK1; IC50 = 126 ?M). 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 ?g/kg. 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 or neurotensin in the rat ventral tegmental area in vitro. |