Fenoldopam (mesylate) (SKF-82526) 是一种 D1 受体激动剂和新型赖氨酸特异性去甲基化酶 1 (LSD1) 抑制剂 (IC50\u003d0.8974 μM)。
| Cas No. | 67227-57-0 |
| 别名 | 非诺多泮甲磺酸盐; Fenoldopam methanesulfonate; SKF-82526 mesylate |
| Canonical SMILES | OC(C=C1)=CC=C1C2CNCCC3=C2C=C(O)C(O)=C3Cl.CS(=O)(O)=O |
| 分子式 | C16H16ClNO3•CH3SO3H |
| 分子量 | 401.9 |
| 溶解度 | DMF: 2 mg/mL,DMF:PBS(pH 7.2)(1:1): 0.5 mg/mL,DMSO: 1 mg/ml,Ethanol: 0.25mg/ml |
| 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 | Fenoldopam(SKF 82526) mesylate is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist.Target: D1 ReceptorFenoldopam is a selective dopamine-1 (DA1) agonist with natriuretic/diuretic properties. Fenoldopam stimulated cAMP accumulation in LLC-PK1 cells in a dose-dependent manner, an effect which could be blocked by the DA1-selective antagonist Sch 23390. Although fenoldopam was more potent than DA (EC50 55.5 +/- 7.75 nM vs. 1.65 +/- 0.64 microM) in stimulating cAMP accumulation in LLC-PK1 cells, the maximum stimulation obtained by fenoldopam was only 37% of the maximum stimulation obtained by DA(Emax 13.0 +/- 2.95 pmol/mg of protein vs. 35.6 +/- 10.19 pmol/mg of protein) [1]. Fenoldopam is a selective dopamine1 (DA1) receptor agonist. Most of the DA1 receptor agonist activity of fenoldopam resides in the R-enantiomer, which also shows weaker alpha 2-adrenoceptor antagonist activity Fenoldopam produces vasodilation in vascular beds that are rich in vascular DA1 receptors [2]. References:
[1]. Grenader, A. and D.P. Healy, Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells. J Pharmacol Exp Ther, 1991. 258(1): p. 193-8.
[2]. Nichols, A.J., R.R. Ruffolo, Jr., and D.P. Brooks, The pharmacology of fenoldopam. Am J Hypertens, 1990. 3(6 Pt 2): p. 116S-119S. |
