2. Immunology/Inflammation
  3. COX
  4. Tolmetin sodium dihydrate

Tolmetin sodium dihydrate 

Cat. No.: HY-B1489 Purity: 99.89%
COA Handling Instructions

Tolmetin sodium dihydrate is an orally active and potent COX inhibitor with IC50s of 0.35 μM and 0.82 μM human COX-1 and COX-2, respectively. Tolmetin sodium dihydrate is a non-steroidal anti-inflammatory drug (NSAID).

For research use only. We do not sell to patients.

Tolmetin sodium dihydrate Chemical Structure

Tolmetin sodium dihydrate Chemical Structure

CAS No. : 64490-92-2

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10 mM * 1 mL in DMSO USD 66 In-stock
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Other Forms of Tolmetin sodium dihydrate:

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

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Description

Tolmetin sodium dihydrate is an orally active and potent COX inhibitor with IC50s of 0.35 μM and 0.82 μM human COX-1 and COX-2, respectively. Tolmetin sodium dihydrate is a non-steroidal anti-inflammatory drug (NSAID)[1][2].

IC50 & Target[1]

Human COX-1

0.35 μM (IC50)

Human COX-2

0.82 μM (IC50)

In Vitro

Tolmetin sodium dihydrate (0.25 mM) does not attenuate lipid peroxidation in rat brain homogenate. Tolmetin (0.25, 0.5, 0.75, 1 mM) shows radical scavenging properties but without superoxide anion generation in rat brain homogenat[3].
Tolmetin sodium dihydrate (0.001-100 μM) shows anticancer activity againts HT-29 colon cancer cell line in a dose-dependent manner[4].
Tolmetin sodium dihydrate (0-100 μM) shows no effect on osteoblast growth[5].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

Tolmetin sodium dihydrate (30,100 mg/kg; gavage; single dose or twice daily for 3 and 14 days) shows maximal ulcerogenic effect 4 h after the single dose, while potently decreases after 3 and 14 days of repeated administration in male Wistar rats weighing 180-200 g. Tolmetin causes gastric lesions in 100 mg/kg[2].
Tolmetin sodium dihydrate (5 mg/kg twice a day for 5 days) pre-treatment considerably attenuates quinolinic acid (QA)-induced neurotoxicity[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

315.30

Appearance

Solid

Formula

C15H18NNaO5
CAS No.
SMILES

O=C(O[Na])CC1=CC=C(C(C2=CC=C(C)C=C2)=O)N1C.O.O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL (317.16 mM)

DMSO : 12.5 mg/mL (39.64 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  PBS

    Solubility: 25 mg/mL (79.29 mM); Clear solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.25 mg/mL (3.96 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.25 mg/mL (3.96 mM); Clear solution

  • 4.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (3.96 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Tolmetin sodium dihydrate64490-92-2COXCyclooxygenasenon-steroidalanti-inflammatoryNSAIDanticancerneurotoxicityInhibitorinhibitorinhibit

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