Ro46-2005是一种新型非肽类内皮素拮抗剂,抑制人血管平滑肌细胞(ETA受体),IC50分别为220nM。
| Cas No. | 150725-87-4 |
| Canonical SMILES | O=S(C1=CC=C(C(C)(C)C)C=C1)(NC2=NC=NC(OCCO)=C2OC3=CC=CC(OC)=C3)=O |
| 分子式 | C23H27N3O6S |
| 分子量 | 473.54 |
| 溶解度 | DMSO : ≥ 28 mg/mL (59.13 mM) |
| 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 | Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.IC50 value: 220 nM (ETA) [2]Target: Endothelinin vitro: Ro 46-2005 proves to be equipotent (IC50 200-500 nM) for inhibition of [125I]ET-1 binding on the two known ET receptor subtypes (ETA and ETB). Ro 46-2005 also inhibits the functional consequences of ET-1 stimulation: the ET-l-induced release of arachidonic acid from rat mesangial cells was inhibited with an IC50 of 1.8 μM.[1] [1]. Breu V, et al. In vitro characterization of Ro 46-2005, a novel synthetic non-peptide endothelin antagonist of ETA and ETBreceptors. FEBS Lett. 1993 Nov 15;334(2):210-214. [2]. Clozel M, et al. Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist. Nature. 1993 Oct 21;365(6448):759-761. [3]. N.R. Sibson, et al. MRI Determination of the Mechanisms Underlying TNF-a-induced Changes in Cerebral Blood Volume, Tissue Water Diffusion and BBB Permeability. Proc. Intl. Soc. Mag. Reson. Med. 10 (2002) |
