| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
| ln Vivo |
Intravenous tolonidine decreases peripheral vascular resistance, lowers aortic blood flow, and decreases the amplitude of ventricular contractions in dogs under anesthesia [1]. Tolonidine raises blood pressure persistently without producing secondary hypotension in doubly denervated rats, indicating that it may have peripheral sympathomimetic effects [1].
|
|---|---|
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
After oral administration, bioavailability is close to 100% and is unaffected by food. Metabolism/Metabolites First-pass hepatic degradation is negligible. No active metabolites were identified. Biological Half-Life The mean plasma half-life in patients is approximately 15 hours. In patients with severe renal impairment (creatinine clearance less than 30 ml/min per 1.73 m² body surface area), the half-life can be prolonged to 35 hours. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Tocarbide was withdrawn from the US market in 2003 due to its potential to cause serious and even fatal hematologic adverse reactions. Limited data suggest that a significant amount of tocarbide is excreted into breast milk. Due to a lack of data on breastfeeding during maternal treatment with tocarbide and its potential toxicity, tocarbide should be avoided during lactation. ◉ Effects on Breastfed Infants No published information found as of the revision date. ◉ Effects on Lactation and Breast Milk No published information found as of the revision date. Protein Binding Approximately 10% is bound to plasma proteins. |
| References |
|
| Additional Infomation |
Tocainide is a monocarboxylic acid amide composed of an amide bond formed by the combination of 2,6-dimethylaniline and isobutyric acid; it is used as a local anesthetic. It has local anesthetic, antiarrhythmic, and sodium channel blocking effects. It is an antiarrhythmic drug that produces potential- and rate-dependent blocking effects on sodium channels. It is an antiarrhythmic drug that produces potential- and rate-dependent blocking effects on sodium channels. Indications It is used to treat confirmed ventricular arrhythmias, such as sustained ventricular tachycardia, that are deemed life-threatening by a physician. Mechanism of Action Tocainide acts on sodium channels on the neuronal cell membrane, limiting the spread of epileptic activity and reducing the propagation of seizures. Tocainide preferentially binds to the inactive state of sodium channels. Its antiarrhythmic effect is achieved by affecting sodium channels in Purkinje fibers.
Pharmacodynamics Toccanib is a primary amine analogue of lidocaine, possessing antiarrhythmic properties and used to treat ventricular arrhythmias. Similar to lidocaine, tropicib dose-dependently reduces sodium and potassium conductance, thereby decreasing the excitability of cardiomyocytes. In animal models, the dose-dependent inhibition of sodium current in ischemic tissue is more significant than in normal tissue. Tocainib belongs to class I antiarrhythmic drugs, and its electrophysiological properties in humans are similar to lidocaine, but different from quinidine, procainamide, and disopyramide. |
| Molecular Formula |
C11H16N2O
|
|---|---|
| Molecular Weight |
192.25754
|
| Exact Mass |
192.126
|
| CAS # |
41708-72-9
|
| Related CAS # |
Tocainide hydrochloride;71395-14-7
|
| PubChem CID |
38945
|
| Appearance |
White to off-white solid powder
|
| Melting Point |
246-266 °C
246 - 266 °C |
| LogP |
2.362
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
14
|
| Complexity |
196
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
BUJAGSGYPOAWEI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C11H16N2O/c1-7-5-4-6-8(2)10(7)13-11(14)9(3)12/h4-6,9H,12H2,1-3H3,(H,13,14)
|
| Chemical Name |
2-amino-N-(2,6-dimethylphenyl)propanamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~650.16 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.2013 mL | 26.0064 mL | 52.0129 mL | |
| 5 mM | 1.0403 mL | 5.2013 mL | 10.4026 mL | |
| 10 mM | 0.5201 mL | 2.6006 mL | 5.2013 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
