RupatadineD4fumarate(UR-12592D4fumarate)是Rupatadinefumarate的氘代标记物。RupatadineFumarate(UR-12592Fumarate)富马酸盐是PAF/H1受体双抑制剂,Ki值分别为0.55μM和0.1μM。
Cas No. | 1795153-63-7 |
别名 | UR-12592 D4 fumarate |
Canonical SMILES | CC1=CN=CC(CN2C([2H])([2H])C/C(CC2([2H])[2H])=C3C4=CC=C(Cl)C=C4CCC5=CC=CN=C5\3)=C1.OC(/C=C/C(O)=O)=O |
分子式 | C30H26D4ClN3O4 |
分子量 | 536.05 |
储存条件 | Store at -20℃ |
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 | Rupatadine D4 fumarate (UR-12592 D4 fumarate) is a deuterium labeled Rupatadine fumarate. Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 μM(rabbit platelet membranes/guinea pig cerebellum membranes)[1][2][3]. [1]. Merlos M, et al. Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther. 1997 Jan;280(1):114-21.
[2]. Queralt M, et al. In vitro inhibitory effect of rupatadine on histamine and TNF-alpha release from dispersed canine skin mast cells and the human mast cell line HMC-1. Inflamm Res. 2000 Jul;49(7):355-60.
[3]. Lv XX, et al. Rupatadine protects against pulmonary fibrosis by attenuating PAF-mediated senescence in rodents. PLoS One. 2013 Jul 15;8(7):e68631. |