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290296-68-3

290296-68-3 structure
290296-68-3 structure
  • Name: Befetupitant
  • Chemical Name: 2-[3,5-bis(trifluoromethyl)phenyl]-N,2-dimethyl-N-[4-(2-methylphenyl)-6-morpholin-4-ylpyridin-3-yl]propanamide
  • CAS Number: 290296-68-3
  • Molecular Formula: C29H29F6N3O2
  • Molecular Weight: 565.55000
  • Catalog: Signaling Pathways GPCR/G Protein Neurokinin Receptor
  • Create Date: 2017-08-09 04:30:24
  • Modify Date: 2024-01-04 18:02:16
  • Befetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist.
Name 2-[3,5-bis(trifluoromethyl)phenyl]-N,2-dimethyl-N-[4-(2-methylphenyl)-6-morpholin-4-ylpyridin-3-yl]propanamide
Synonyms Ro 67-5930
Befetupitant
UNII-RSH7NDI7MI
Description Befetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist.
Related Catalog
Target

NK1R[1]
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].
Animal Admin Mice[1] Female, 6- to 8-week-old, C57BL/6 mice are used for all experiments (total: 283 mice). A corneal alkali burn is created for the Lanepitant experiment. Animals are then randomized into three groups (n=6), receiving 10 μL Befetupitant 0.4 or 1.6 mg/mL in 100% DMSO or 10 μL vehicle (DMSO) as control, topically six times a day for 4 days. Topical Befetupitant and DMSO toxicity is evaluated in two groups of six healthy animals receiving in the left eye 10 μL topical Befetupitant 0.4 mg/mL or 100% DMSO, six times a day for 9 days.
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.

Density 1.283g/cm3
Boiling Point 599.8ºC at 760mmHg
Molecular Formula C29H29F6N3O2
Molecular Weight 565.55000
Flash Point 316.6ºC
Exact Mass 565.21600
PSA 45.67000
LogP 6.93680
Vapour Pressure 2.39E-14mmHg at 25°C
Index of Refraction 1.537
Storage condition 2-8℃

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title: CAS No. 290296-68-3 | Chemsrc address: https://m.chemsrc.com/en/baike/302780.html

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