Amtolmetin guacil
Based on 1 Customer Validation
Amtolmetin guacil is an effective nonsteroidal anti-Inflammatory agent with pain-relieving effects. Amtolmetin guacil inhibits prostaglandin synthesis and cyclooxygenase (COX). Amtolmetin guacil can stimulate capsaicin receptors present on the gastrointestinal wall and also releases gastroprotective nitric oxide (NO). Amtolmetin guacil can be used to research knee osteoarthritis.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 87344-06-7
- Formula: C24H24N2O5
- Molecular Weight:420.46
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Storage:
Store at room temperature 3 years.
In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
51.3 μM
Compound: AMG
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Inhibition of LPS/IFNgamma-induced NO production in mouse RAW264.7 cells after 24 hrs by Griess reagent method
Inhibition of LPS/IFNgamma-induced NO production in mouse RAW264.7 cells after 24 hrs by Griess reagent method
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[PMID: 21441032] |
Amtolmetin guacil (100 μM; 0-60 min) converts to TMT (Tolmetin, HY-B1799) along with MED5 (1-methyl-5-p-methylbenzoyl-pyrrol-2-acetamido aceticacid) in rat fresh plasma and rat liver microsomal, rapidly converts to MED5 and MED5 methyl ester without yielding TMT in human fresh plasma and human liver microsomes[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats[3]
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Dosage:50 mg/kg
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Administration:p.o.; single dosage
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Result:Pharmacokinetic Parameters of Amtolmetin guacil in male Wistar rats[3].
AUC0-t (ng/mL·h) AUC0-∞ (ng/mL·h) Cmax (μg/mL) Tmax (h) Kel (h-1) t1/2,β (h) TMT following Amtolmetin guacil dosing 162 ± 21.49 164 ± 22.47 81.62 ± 5.02 0.50 ± 0.00 0.28 ± 0.00 2.41 ± 0.01
Chemical Information
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CAS No. 87344-06-7
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Appearance Solid
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Molecular Weight 420.46
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Formula C24H24N2O5
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Color White to off-white
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SMILES
O=C(C1=CC=C(C)C=C1)C2=CC=C(CC(NCC(OC3=C(C=CC=C3)OC)=O)=O)N2C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Store at room temperature 3 years
In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 100 mg/mL (237.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
[2]. Niccoli L, et al. Renal tolerability of three commonly employed non-steroidal anti-inflammatory drugs in elderly patients with osteoarthritis. Clin Exp Rheumatol. 2002 Mar-Apr;20(2):201-7. [Content Brief]
[3]. Hotha KK, et al. Species difference in the in vitro and in vivo metabolism of amtolmetin guacil. Arzneimittelforschung. 2010;60(11):667-74. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3783 mL | 11.8917 mL | 23.7835 mL | 59.4587 mL |
| 5 mM | 0.4757 mL | 2.3783 mL | 4.7567 mL | 11.8917 mL | |
| 10 mM | 0.2378 mL | 1.1892 mL | 2.3783 mL | 5.9459 mL | |
| 15 mM | 0.1586 mL | 0.7928 mL | 1.5856 mL | 3.9639 mL | |
| 20 mM | 0.1189 mL | 0.5946 mL | 1.1892 mL | 2.9729 mL | |
| 25 mM | 0.0951 mL | 0.4757 mL | 0.9513 mL | 2.3783 mL | |
| 30 mM | 0.0793 mL | 0.3964 mL | 0.7928 mL | 1.9820 mL | |
| 40 mM | 0.0595 mL | 0.2973 mL | 0.5946 mL | 1.4865 mL | |
| 50 mM | 0.0476 mL | 0.2378 mL | 0.4757 mL | 1.1892 mL | |
| 60 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9910 mL | |
| 80 mM | 0.0297 mL | 0.1486 mL | 0.2973 mL | 0.7432 mL | |
| 100 mM | 0.0238 mL | 0.1189 mL | 0.2378 mL | 0.5946 mL |