Celecoxib-d7
(Synonyms: 塞来昔布-D7,SC 58635-d7) 目录号 : GC47070
An internal standard for the quantification of celecoxib
Cas No.:544686-21-7
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
Celecoxib-d7 is intended for use as an internal standard for the quantification of celecoxib by GC- or LC-MS. Celecoxib is a selective inhibitor of COX-2 (IC50s = 22.9 and 0.05 μM for COX-1 and COX-2, respectively).1,2 It displays chemopreventive activity in multiple tumor types via proapoptotic effects that are independent of COX-2 inhibition.3,4,5 Formulations containing celecoxib have been used in the treatment of inflammation while circumventing the gastrointestinal toxicity associated with traditional non-sterodial anti-inflammatory drugs, however, the use of celecoxib has been tempered due to its ability to induce adverse cardiovascular events.6
1.Uddin, J.M., Rao, P.N.P., and Knaus, E.E.Design and synthesis of novel celecoxib analogues as selective cyclooxygenase-2 (COX-2) inhibitors: Replacement of the sulfonamide pharmacophore by a sulfonylazide bioisostereBioorg. Med. Chem.11(23)5273-5280(2003) 2.Mardini, I.A., and Fitzgerald, G.A.Selective inhibitors of cyclooxygenase-2: A growing class of anti-inflammatory drugsMolecular Interventions1(1)30-38(2001) 3.Jendrossek, V., Handrick, R., and Belka, C.Celecoxib activates a novel mitochondrial apoptosis signaling pathwayThe FASEB Journal171547-1549(2003) 4.Leahy, K.M., Ornberg, R.L., Wang, Y., et al.Cyclooxygenase-2 inhibition by celecoxib reduces proliferation and induces apoptosis in angiogenic endothelial cells in vivoCancer Research62625-631(2002) 5.Zhu, J., Huang, J.W., Tseng, P.H., et al.From the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitorsCancer Res.644309-4318(2004) 6.Blobaum, A.L., and Marnett, L.J.Structural and functional basis of cyclooxygenase inhibitionJ. Med. Chem.50(7)1425-1441(2007)
| Cas No. | 544686-21-7 | SDF | |
| 别名 | 塞来昔布-D7,SC 58635-d7 | ||
| Canonical SMILES | NS(C1=CC=C(N2C(C3=C([2H])C([2H])=C(C([2H])([2H])[2H])C([2H])=C3[2H])=CC(C(F)(F)F)=N2)C=C1)(=O)=O | ||
| 分子式 | C17H7D7F3N3O2S | 分子量 | 388.4 |
| 溶解度 | DMSO: 76 mg/ml,Ethanol: 33 mg/ml | 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 | 2.5747 mL | 12.8733 mL | 25.7467 mL |
| 5 mM | 0.5149 mL | 2.5747 mL | 5.1493 mL |
| 10 mM | 0.2575 mL | 1.2873 mL | 2.5747 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。
The delivery of nanoparticles improves the pharmacokinetic properties of celecoxib to open a therapeutic window for oral administration of insoluble drugs
Biomed Chromatogr 2023 Feb;37(2):e5552.PMID:36408991DOI:10.1002/bmc.5552
A sensitive and reliable LC-MS/MS method is established and validated to determine the concentration of celecoxib, in the serum of cynomolgus monkey, using Celecoxib-d7 as an internal standard. The pharmacokinetic process was investigated after giving Celebrex, celecoxib nanoparticles (CXB-NPs) and hyaluronic acid celecoxib nanoparticles (HA-CXB-NPs) by intragastric (i.g.) administration. Chromatographic separation was performed with a C18 column (2.1 × 100 mm, 2.6 μm) at 40°C with a mobile phase of 2‰ HCOOH in water and acetonitrile. The mass spectral acquisition was then performed in the multiple reaction monitoring mode, with negative ESI ion at m/z 380.0 → 316.0 and m/z 387.1 → 323.1 for celecoxib and Celecoxib-d7, respectively. Good linearity was observed over the concentration range from 3 to 2,000 ng/ml (R2 = 0.9954). The intra- and inter-day precision and accuracy, matrix effect and extraction recovery, as well as stability, all met the determination requirements of biological samples. The pharmacokinetic parameters of Celebrex, CXB-NPs and HA-CXB-NPs were determined as: area under the curve, 1,855.98 ± 346.59, 1,908.00 ± 1,130.24 and 2,164.48 ± 657.47 h·ng/ml; peak concentration, 261.08 ± 113.26, 261.12 ± 94.67 and 263.34 ± 151.78 μg/L; time to peak concentration, 2.00 ± 1.22, 4.00 ± 0.00 and 3.60 ± 0.89 h; half-life, 4.39 ± 1.26, 2.33 ± 0.94 and 4.92 ± 3.13 h; relative bioavailability, 102.80 ± 49.62 and 116.63 ± 25.55%. The validated method was successfully applied to the pharmacokinetic study of celecoxib in cynomolgus monkey, after i.g. administration. The preparation of the nanoparticles of celecoxib and the modification of hyaluronic acid on the surface of nanoparticles could improve the bioavailability and prolong the circulation of celecoxib in vivo, which could lay the foundation for further development of celecoxib nanoparticles.