| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 1g |
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Purity: ≥98%
Trimethobenzamide (also known as Ro 2-9578; trade names Tebamide, Tigan), a blocker of the D2 receptor, is a potent antiemetic that is used to prevent nausea and vomiting. Patients with gastroenteritis, medication-induced nausea, and other ailments are frequently prescribed it. Because it doesn't affect the histaminergic, dopaminergic, or serotonergic systems, trimethobenzamide is widely regarded as the most effective antiemetic and is less likely to have unwanted side effects. It needs a prescription in the United States. While the precise mode of action of trimethobenzamide remains unclear, it is thought to impact the medulla oblongata's chemoreceptor trigger zone (CTZ).
| Targets |
D2 receptor
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|---|---|
| ln Vitro |
Trimethobenzamide is a benzamide antiemetic (non-phenothiazine) that inhibits the medullary chemoreceptor trigger zone by blocking emetic impulses to the vomiting center. It functions by centrally inhibiting D2 receptors [1].
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| ln Vivo |
Trimethobenzamide has an oral bioavailability of 60% to 100%. After oral administration, the time to peak is approximately 45 minutes, and after intramuscular (I.M.) administration, it is approximately 30 minutes[1].
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| References |
| Molecular Formula |
C21H29CLN2O5
|
|---|---|
| Molecular Weight |
424.9184
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| Exact Mass |
424.18
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| Elemental Analysis |
C, 59.36; H, 6.88; Cl, 8.34; N, 6.59; O, 18.83
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| CAS # |
554-92-7
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| Related CAS # |
Trimethobenzamide; 138-56-7; Trimethobenzamide-d6
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| Appearance |
Solid powder
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| SMILES |
CN(C)CCOC1=CC=C(C=C1)CNC(=O)C2=CC(=C(C(=C2)OC)OC)OC.Cl
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| InChi Key |
WIIZEEPFHXAUND-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H28N2O5.ClH/c1-23(2)10-11-28-17-8-6-15(7-9-17)14-22-21(24)16-12-18(25-3)20(27-5)19(13-16)26-4;/h6-9,12-13H,10-11,14H2,1-5H3,(H,22,24);1H
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| Chemical Name |
N-[[4-[2-(dimethylamino)ethoxy]phenyl]methyl]-3,4,5-trimethoxybenzamide;hydrochloride
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| Synonyms |
Ro-2-9578; Ro-2 9578; Ro 2 9578; Tebamide; Ticon; Tigan; trimethobenzamide; trimethobenzamide monohydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 100 mg/mL (~235.3 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3534 mL | 11.7669 mL | 23.5338 mL | |
| 5 mM | 0.4707 mL | 2.3534 mL | 4.7068 mL | |
| 10 mM | 0.2353 mL | 1.1767 mL | 2.3534 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02262767 | Completed | Drug: PF-06649751 Drug: Trimethobenzamide Hydrochloride |
Healthy | Pfizer | November 2014 | Phase 1 |
| NCT01770145 | Completed | Drug: APOKYN Drug: Trimethobenzamide |
Akinesia Motor Symptoms Hypomobility |
MDD US Operations, LLC a subsidiary of Supernus Pharmaceuticals |
December 2012 | Phase 4 |
| NCT02373072 | Completed | Drug: PF-06649751 Drug: Trimethobenzamide Hydrochloride |
Idiopathic Parkinson Disease | Pfizer | March 2015 | Phase 1 |
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