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 |
| 产品描述 | βARK1 inhibitor is an inhibitor of G protein-coupled receptor kinase 2/β-adrenergic receptor kinase 1 (GRK2/βARK1; IC50 = 126 µM). 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. 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. |
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