Diclofenac Sodium
(Synonyms: 双氯芬酸钠; GP 45840) 目录号 : GC14261
An NSAID and a COX inhibitor
Cas No.:15307-79-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rats[1]Male Sprague-Dawley rats (150 ± 200 g) are dosed orally with Diclofenac either once (acute dosing) or twice daily for 5 days (chronic dosing). A plasma sample is obtained 1 h after the morning dose on day 4 for measurement of Diclofenac concentration. Immediately after the administration of the last dose on day 5, the rats are injected via a tail vein with 0.5 mL of 51Cr-labelled red blood cells from a donor rat after incubation with sodium 51chromate. The rats are placed individually in metabolism cages with food and water ad libitum. Faeces are collected for a 48 h period and 51Cr faecal excretion is calculated as a % of total injected dose (20 mCi per animal)[1]. Squirrel monkeys[1]Squirrel monkeys (Saimiri sciureus; 0.8 ± 1.4 kg) are dosed orally with Diclofenac twice daily for 1 ± 5 days. One hour after administration of the last dose, 51CrCl3 in sterile saline (1 mL/kg, 4 ± 5 mCi per animal) is injected via a saphenous vein and plasma samples are obtained for measurement of Diclofenac concentration. The monkeys are then housed individually in metabolism cages. Faeces are collected for a 24 h period and 51Cr faecal excretion is calculated as a % of total injected dose[1]. |
References: [1]. Riendeau D, et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17. | |
Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 nM, 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1, 0.84 μM for ovine COX-1 and COX-2, respectively.
Diclofenac Sodium (GP 45840) is a potent COX inhibitor, with IC50s of 4 nM and 1.3 nM for human COX-1 and COX-2 in the CHO cells, respectively. Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC50 of 7 ± 3 nM[1]. Diclofenac Sodium exihibits inhibition on COX-1 and COX-2 enzyme with IC50s of 5.1 and 0.84 μM, respectively[2].
Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly increases faecal 51Cr excretion in rats, and such effect is also observed in squirrel monkeys after administrated of 1 mg/kg twice daily for 4 days[1]. Diclofenac (10 mg/kg) shows anti-inflammatory activity in mice[2]. Diclofenac (10 mg/kg) decreases oxidized low-densitylipoprotein (Ox-LDL), but shows no effects on the kinetics parameters of catalase and glutathione peroxidase via intramuscularly injection into rats[3].
Reference:
[1]. Riendeau D, et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17.
[2]. Labib MB, et al. Design, synthesis of novel isoindoline hybrids as COX-2 inhibitors: Anti-inflammatory, analgesic activities and docking study. Bioorg Chem. 2018 Oct;80:70-80.
[3]. Curcelli EC, et al. Beneficial effects of diclofenac therapy on serum lipids, oxidized low-density lipoprotein and antioxidant defenses in rats. Life Sci. 2008 Apr 9;82(15-16):892-8.
| Cas No. | 15307-79-6 | SDF | |
| 别名 | 双氯芬酸钠; GP 45840 | ||
| 化学名 | sodium;2-[2-(2,6-dichloroanilino)phenyl]acetate | ||
| Canonical SMILES | C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+] | ||
| 分子式 | C14H10Cl2NNaO2 | 分子量 | 318.13 |
| 溶解度 | ≥ 15.91mg/mL 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。 |
||
| 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 | 3.1434 mL | 15.7168 mL | 31.4337 mL |
| 5 mM | 0.6287 mL | 3.1434 mL | 6.2867 mL |
| 10 mM | 0.3143 mL | 1.5717 mL | 3.1434 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。