Befetupitant (Ro67-5930)
(Synonyms: Ro67-5930) 目录号 : GC33724
Befetupitant (Ro67-5930) 是一种高亲和力、非肽、竞争性速激肽 1 受体 (NK1R) 拮抗剂。
Cas No.:290296-68-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. | |
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.
| Cas No. | 290296-68-3 | SDF | |
| 别名 | 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 | ||
| 分子式 | C29H29F6N3O2 | 分子量 | 565.55 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。