Apremilast-d5
(Synonyms: 阿普斯特-D5,CC-10004-d5) 目录号 : GC46867
An internal standard for the quantification of apremilast
Cas No.:1258597-47-5
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
Apremilast-d5 is intended for use as an internal standard for the quantification of apremilast by GC- or LC-MS. Apremilast is an inhibitor of phosphodiesterase 4 (PDE4) with an IC50 value of 74 nM when tested in U937 cell lysates with 1 mM cAMP.1,2 It is orally active, significantly decreasing epidermal thickness and the epithelial cell proliferation index in a mouse model of psoriasis.2 Apremilast reduces both TNF-α and matrix metalloproteinase-3 production in gut lamina propria mononuclear cells from patients with inflammatory bowel disease.3 It also blocks spontaneous production of TNF-α from human rheumatoid synovial cells and improves the clinical score in mouse models of arthritis.4
1.Man, H.W., Schafer, P., Wong, L.M., et al.Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitorJournal of Medicinal Chemistry52(6)1522-1524(2009) 2.Schafer, P.H., Parton, A., Gandhi, A.K., et al.Apremilast, a cAMP phosphodiesterase-4 inhibitor, demonstrates anti-inflammatory activity in vitro and in a model of psoriasisBritish Journal of Pharmacology159(4)842-855(2010) 3.Gordon, J.C., Prothero, J.D., Thornton, C.A., et al.CC-10004 but not thalidomide or lenalidomide inhibits lamina propria mononuclear cell TNF-α and MMP-3 production in patients with inflammatory bowel diseaseJ.Crohns.Colitis.3(3)175-182(2009) 4.McCann, F.E., Palfreeman, A.C., Andrews, M., et al.Apremilast, a novel PDE4 inhibitor, inhibits spontaneous production of tumour necrosis factor-alpha from human rheumatoid synovial cells and ameliorates experimental arthritisArthritis Research & Therapy12(3)(2010)
| Cas No. | 1258597-47-5 | SDF | |
| 别名 | 阿普斯特-D5,CC-10004-d5 | ||
| Canonical SMILES | O=C1N([C@H](CS(C)(=O)=O)C2=CC(OC([2H])([2H])C([2H])([2H])[2H])=C(OC)C=C2)C(C3=C(NC(C)=O)C=CC=C31)=O | ||
| 分子式 | C22H19D5N2O7S | 分子量 | 465.5 |
| 溶解度 | DMSO : 100 mg/mL (214.81 mM; Need ultrasonic); DMSO : 44 mg/mL (94.52 mM; Need ultrasonic) | 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 | 2.1482 mL | 10.7411 mL | 21.4823 mL |
| 5 mM | 0.4296 mL | 2.1482 mL | 4.2965 mL |
| 10 mM | 0.2148 mL | 1.0741 mL | 2.1482 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。