Carebastine-d5
(Synonyms: 卡依巴司丁 d5) 目录号 : GC47040
An internal standard for the quantification of carebastine
Cas No.:1189661-02-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Carebastine-d5 is intended for use as an internal standard for the quantification of carebastine by GC- or LC-MS. Carebastine is an active metabolite of ebastine .1,2 Ebastine undergoes extensive first-pass metabolism by the hepatic cytochrome P450 (CYP) isomer CYP3A4 into carebastine, which acts as an antagonist at histamine H1 receptors (IC50 = 45 nM).2,3 Carebastine decreases production of RANTES/CCL5 and monocyte chemoattractant protein 1 (MCP-1/CCL2) in human nasal epithelial cells (HNECs) isolated from patients with nasal allergies.4
1.Vincent, J., Liminana, R., Meredith, P.A., et al.The pharmacokinetics, antihistamine and concentration-effect relationship of ebastine in healthy subjectsBr. J. Clin. Pharmacol.26(5)497-502(1988) 2.Liu, K.-H., Kim, M.-G., Lee, D.-J., et al.Characterization of ebastine, hydroxyebastine, and carebastine metabolism by human liver microsomes and expressed cytochrome P450 enzymes: Major roles for CYP2J2 and CYP3ADrug. Metab. Dispos.34(11)1793-1797(2006) 3.Abou-Gharbia, M., Moyer, J.A., Nielsen, S.T., et al.New antihistamines: Substituted piperazine and piperidine derivatives as novel H1-antagonistsJ. Med. Chem.38(20)4026-4032(1995) 4.Yamauchi, Y., Fujikura, T., and Shimosawa, T.The effect of H1 antagonists carebastine and olopatadine on histamine induced expression of CC chemokines in cultured human nasal epithelial cellsAllergol. Int.56(2)171-177(2007)
| Cas No. | 1189661-02-6 | SDF | |
| 别名 | 卡依巴司丁 d5 | ||
| Canonical SMILES | O=C(C1=CC=C(C(C)(C)C(O)=O)C=C1)CCCN(CC2)CCC2OC(C3=CC=CC=C3)C4=C([2H])C([2H])=C([2H])C([2H])=C4[2H] | ||
| 分子式 | C32H32D5NO4 | 分子量 | 504.7 |
| 溶解度 | Chloroform: slightly soluble,Ethyl Acetate: slightly soluble | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9814 mL | 9.9069 mL | 19.8138 mL |
| 5 mM | 0.3963 mL | 1.9814 mL | 3.9628 mL |
| 10 mM | 0.1981 mL | 0.9907 mL | 1.9814 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。