| Bioactivity | Befetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist. |
| In Vivo | Befetupitant, a different, highly selective NK1R antagonist, is tested in the alkali burn model. Topical application of Befetupitant for 4 days is effective (P<0.05) in reducing hemangiogenesis and lymphangiogenesis at both concentrations (0.4 and 1.6 mg/mL). Befetupitant and its vehicle DMSO, however, induced corneal opacity even in healthy controls, as observed at slit-lamp examination. Moreover, fluorescein and hematoxylin-eosin staining showed epithelial damage and inflammatory cellular infiltration in the stroma, respectively, confirming DMSO toxicity. Topical application of Befetupitant reduces corneal neovascularization (CNV) in the alkali burn model but is toxic owing to the vehicle (DMSO); hence, Befetupitant is not tested in the suture model[1]. |
| Name | Befetupitant |
| CAS | 290296-68-3 |
| Formula | C29H29F6N3O2 |
| Molar Mass | 565.55 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |