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Befetupitant (Ro67-5930) (Synonyms: Ro67-5930)

Catalog No.GC33724

Befetupitant (Ro67-5930) is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist.

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Befetupitant (Ro67-5930) Chemical Structure

Cas No.: 290296-68-3

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1mg
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5mg
$2,087.00
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10mg
$3,613.00
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20mg
$6,333.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Animal experiment:

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.

Background

Befetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist.

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].

[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.

Chemical Properties

Cas No. 290296-68-3 SDF
Synonyms Ro67-5930
Canonical SMILES CN(C(C(C)(C)C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)=O)C2=CN=C(N3CCOCC3)C=C2C4=C(C)C=CC=C4
Formula C29H29F6N3O2 M.Wt 565.55
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.7682 mL 8.841 mL 17.6819 mL
5 mM 0.3536 mL 1.7682 mL 3.5364 mL
10 mM 0.1768 mL 0.8841 mL 1.7682 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

Review for Befetupitant (Ro67-5930)

Average Rating: 5 ★★★★★ (Based on Reviews and 7 reference(s) in Google Scholar.)

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