| CAS NO: | 64490-92-2 |
| 包装 | 价格(元) |
| 5g | 电议 |
| 10g | 电议 |
| 25g | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 315.3 |
| Cas No. | 64490-92-2 |
| Formula | C15H14NO3·Na [2H2O] |
| Solubility | ≤2mg/ml in DMSO |
| Chemical Name | 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
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