Description | Befetupitant (Ro67-5930) is a potent and selective tachykinin 1 receptor (NK1R) antagonist for the study of corneal neovascularization. |
In vivo | 在碱烧伤模型中,对Befetupitant(一种高度选择性的NK1R拮抗剂)进行了测试。经过Befetupitant局部应用4天后,以两种浓度(0.4和1.6 mg/mL)明显减少了血管生成和淋巴管生成(P<0.05)。然而,Befetupitant及其载体DMSO即使在健康对照组中也诱导了角膜不透明,这是通过裂隙灯检查观察到的。此外,荧光素和苏木精-伊红染色确认了DMSO的毒性,通过揭示上皮损伤和基质中的炎症细胞浸润。尽管Befetupitant在减少碱烧伤模型中的角膜新生血管化(CNV)方面有效,但由于DMSO载体的毒性,决定不在缝合模型中测试它[1]。 |
Synonyms | Ro67-5930 |
molecular weight | 565.55 |
Molecular formula | C29H29F6N3O2 |
CAS | 290296-68-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
Solubility | DMSO: 6.88 mg/mL (12.16 mM), Sonication is recommended. |
References | 1. Bignami F, et al. NK1 receptor antagonists as a new treatment for corneal neovascularization. Invest Ophthalmol Vis Sci. 2014 Sep 16;55(10):6783-94. |