Osanetant (hydrate)
(Synonyms: SR 142801) 目录号 : GC48405
An NK3 receptor antagonist
Sample solution is provided at 25 µL, 10mM.
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Osanetant is a neurokinin-3 (NK3) receptor antagonist (Ki = 0.21 nM in CHO cells expressing the human receptor).1 It is selective for NK3 over NK1 and NK2 receptors (Kis = >100 and 0.02 µM, respectively).2 Osanetant inhibits contractions and acetylcholine release induced by neurokinin B in isolated guinea pig ileal strips in a concentration-dependent manner.1 It inhibits ovalbumin-induced increases in bronchoalveolar lavage fluid (BALF) neutrophil, eosinophil, and lymphocyte infiltration in an ovalbumin-sensitized mouse model of allergic asthma.3 Osanetant (5 and 10 mg/kg) increases the duration of social interaction, as well as reduces immobility time in the tonic immobility test, indicating anxiolytic-like and antidepressant-like activities, respectively, in gerbils.4
1.Emonds-Alt, X., Bichon, D., Ducoux, J.P., et al.SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptorLife Sci.56(1)PL27-PL32(1995) 2.Griebel, G., and BeeskÉ, S.Is there still a future for neurokinin 3 receptor antagonists as potential drugs for the treatment of psychiatric diseases•Pharmacol. Ther.133(1)116-123(2012) 3.NÉnan, S., Germain, N., Lagente, V., et al.Inhibition of inflammatory cell recruitment by the tachykinin NK3-receptor antagonist, SR 142801, in a murine model of asthmaEur. J. Pharmacol.421(3)201-205(2001) 4.SalomÉ, N., Stemmelin, J., Cohen, C., et al.Selective blockade of NK2 or NK3 receptors produces anxiolytic- and antidepressant-like effects in gerbilsPharmacol. Biochem. Behav.83(4)533-539(2006)
| Cas No. | SDF | ||
| 别名 | SR 142801 | ||
| Canonical SMILES | O=C(C1=CC=CC=C1)N(CCC2)C[C@]2(C3=CC(Cl)=C(C=C3)Cl)CCCN4CCC(C5=CC=CC=C5)(N(C)C(C)=O)CC4.O | ||
| 分子式 | C35H41Cl2N3O2•H2O | 分子量 | 624.7 |
| 溶解度 | DMSO: 15 mg/ml | 储存条件 | -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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6008 mL | 8.0038 mL | 16.0077 mL |
| 5 mM | 0.3202 mL | 1.6008 mL | 3.2015 mL |
| 10 mM | 0.1601 mL | 0.8004 mL | 1.6008 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet