Sodium tolmetin dihydrate
Sodium tolmetin dihydrate Basic information
- Product Name:
- Sodium tolmetin dihydrate
- Synonyms:
-
- sodiumtolmetindihydrate
- tolmetinsodiumdihydrate
- 1-methyl-5-(p-toluoyl)pyrrole-2-acetic acid sodium-potassium salt dihydrate
- TOLMELINSODIUM
- Tolmetinsodiumsaltdihydratecrystalline
- 1-Methyl-5-(4-methylbenzoyl)-1H-pyrrole-2-acetic Acid Sodium Dihydrate
- 1-Methyl-5-p-toluoylpyrrole-2-acetic Acid Sodium Dihydrate
- 5-[(p-Tolyl)carbonyl]-1-methylpyrrole-2-acetic Acid Sodium Dihydrate
- CAS:
- 64490-92-2
- MF:
- C15H14NO3.Na.2H2O
- MW:
- 315.3
- EINECS:
- 626-708-5
- Product Categories:
-
- Aromatics
- Heterocycles
- API intermediates
- Intermediates & Fine Chemicals
- Pharmaceuticals
- BETAGAN
- Mol File:
- 64490-92-2.mol
Sodium tolmetin dihydrate Chemical Properties
- Melting point:
- 155-157 (dec.)
- storage temp.
- -20°C Freezer
- solubility
- Methanol (Slightly), Water (Slightly)
- form
- Solid
- color
- White to Beige
- Water Solubility
- Soluble in water
- InChIKey
- QQILXENAYPUNEA-UHFFFAOYSA-M
- CAS DataBase Reference
- 64490-92-2(CAS DataBase Reference)
MSDS
- Language:English Provider:SigmaAldrich
Sodium tolmetin dihydrate Usage And Synthesis
Chemical Properties
Crystalline Solid
Uses
beta-adrenergic blocker
Uses
Anti-inflammatory.
Definition
ChEBI: An organic sodium salt that is the dihydrate form of tolmetin sodium. Used as a nonselective nonsteroidal anti-inflammatory drug.
Biological Activity
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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Sodium tolmetin dihydrate(64490-92-2)Related Product Information
- Phenylmethylsulfonyl fluoride
- Sodium phenylacetate
- 1-Methylpyrrolidine
- Sodium bicarbonate
- Sodium chloride
- Trisodium phosphate
- Diclofenac sodium
- Methyl acrylate
- Sodium acetate
- Methyl cellulose
- Tolmetin sodium
- Methylparaben
- Sodium hydroxide
- Pyrrole
- Phenoxyacetic acid sodium salt
- N-Methyl-2-pyrrolidone
- Sodium citrate
- Amtolmetin guacil