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Tolmetin (sodium salt hydrate) Sale

(Synonyms: 痛灭定) 目录号 : GC16428

A non-selective NSAID

Tolmetin (sodium salt hydrate) Chemical Structure

Cas No.:64490-92-2

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5g
¥693.00
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10g
¥1,313.00
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25g
¥2,520.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

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.
[2]. Etcheverry SB, et al. Three new vanadyl(IV) complexes with non-steroidal anti-inflammatory drugs (Ibuprofen, Naproxen and Tolmetin). Bioactivity on osteoblast-like cells in culture. J Inorg Biochem. 2002 Jan 1;88(1):94-100.
[3]. Dairam A, et al. Non-steroidal anti-inflammatory agents, tolmetin and sulindac, attenuate oxidative stress in rat brain homogenate and reduce quinolinic acid-induced neurodegeneration in rat hippocampal neurons. Metab Brain Dis. 2006 Sep;21(2-3):221-33.

产品描述

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.

Chemical Properties

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
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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。
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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
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