Tolmetin (sodium salt hydrate)
(Synonyms: 痛灭定) 目录号 : GC16428
A non-selective NSAID
Cas No.:64490-92-2
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');)
;)
Tolmetin is a non-steroidal anti-inflammatory drug that non-selectively inhibits human COX-1 and -2 [1].
The cyclooxygenase (COX) is a therapeutic target for preventing cancer. Two isoforms of COX have been identified: COX 1 and COX 2. COX 1 has been constitutively expressed in most tissues and involved in mediating production of prostaglandins that control normal physiological functions, such as maintenance of the gastric mucosa and regulation of renal blood flow. COX 2 is undetectable in most normal tissues [2].
In vitro: Tolmetin inhibited the activity of human COX-1 and -2 with IC50 values of 0.35 and 0.82 μM, respectively [1]. Tolmetin was a competitive and reversible inhibitor of prostaglandin synthetase [3].
In vivo: In rats, pretreatment with tolmetin reduced prostaglandin synthesis by minces of renal medulla. Incubation of medullary tissue with tolmetin decreased prostagland production. In anesthetized dogs, Tolmetin reduced renal blood flow and shifted the distribution of renal cortical flow from the inner cortex toward the outer cortex [4].
References:
[1] Warner T D, Giuliano F, Vojnovic I, et al. Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis[J]. Proceedings of the National Academy of Sciences, 1999, 96(13): 7563-7568.
[2] Dannenberg A J, Altorki N K, Boyle J O, et al. Cyclo-oxygenase 2: a pharmacological target for the prevention of cancer[J]. The lancet oncology, 2001, 2(9): 544-551.
[3] Taylor R J, Salata J J. Inhibition of prostaglandin synthetase by tolmetin (Tolectin, McN-2559), a new non-steroidal anti-inflammatory agent[J]. Biochemical pharmacology, 1976, 25(22): 2479-2484.
[4] Noordewier B, Stygles V G, Hook J B, et al. Effect of tolmetin on renal function and prostaglandin metabolism[J]. Journal of Pharmacology and Experimental Therapeutics, 1978, 204(2): 461-468.
|
Animal experiment: |
Rats[1]After 2 weeks of acclimatization, rats are randomized to different groups and given the non-selective COX inhibitors, amtolmetin guacyl (AMG) (50 and 150 mg/kg) and Tolmetin (30 and 100 mg/kg) as well as the selective COX-2 inhibitor, celecoxib (CXIB; 20 and 60 mg/kg). The compounds are suspended in 1% carboxymethylcellulose (CMC) immediately before use and administered by gavage in a 10-mL/kg volume. Control groups receive CMC in the same volume. Rats from each group are divided into 3 subgroups, consisting each of at least 10 animals. Subgroups are dosed either with a single dose (acute treatment group) or twice daily for 3 and 14 days (chronic treatment groups). To ensure that all groups are dosed for the same period of time, those receiving less than 14 days of NSAIDs are given CMC until they are due to start the assigned treatment. Rats are killed by cervical dislocation 4 h after the last administration. Stomachs are immediately removed, opened along the lesser curvature and gently rinsed[1]. |
|
References: [1]. Morini G, et al. Morphological features of rat gastric mucosa after acute and chronic treatment with amtolmetin guacyl: comparison with non-selective and COX-2-selective NSAIDs. Digestion. 2003;68(2-3):124-32. Epub 2003 Nov 7. |
|
| Cas No. | 64490-92-2 | SDF | |
| 别名 | 痛灭定 | ||
| 化学名 | 1-methyl-5-(4-methylbenzoyl)-1H-pyrrole-2-acetic acid, monosodium, dihydrate | ||
| Canonical SMILES | CC1=CC=C(C(C2=CC=C(CC([O-])=O)N2C)=O)C=C1.[Na+].O.O | ||
| 分子式 | C15H18NNaO5 | 分子量 | 315.3 |
| 溶解度 | ≤2mg/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 | 3.1716 mL | 15.8579 mL | 31.7158 mL |
| 5 mM | 0.6343 mL | 3.1716 mL | 6.3432 mL |
| 10 mM | 0.3172 mL | 1.5858 mL | 3.1716 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet