| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
EthA (mycobacterial flavin monooxygenase, activation); InhA (enoyl-ACP reductase, inhibition of mycolic acid synthesis).
|
|---|---|
| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
Prothionamide shows activity against Mycobacterium tuberculosis in vitro with MIC values typically in the range of 0.5–2 µg/mL for susceptible strains. Resistance is associated with mutations in the ethA gene. The drug is also active against Mycobacterium leprae. In enzyme assays, the activated metabolite inhibits InhA with IC50 values in the submicromolar range, although precise values depend on the activation system used. |
| ln Vivo |
In vivo, prothionamide is effective in murine models of tuberculosis when administered orally at doses of 25–100 mg/kg/day, reducing bacterial burden in lungs and spleen. It is also used in combination regimens to prevent resistance. The deuterated form is used for pharmacokinetic profiling.
|
| Enzyme Assay |
For in vitro susceptibility testing, M. tuberculosis strains are grown in Middlebrook 7H9 broth, and MICs are determined by the broth microdilution method or the proportion method on 7H10 agar. For EthA activation assays, recombinant EthA is incubated with prothionamide and NADPH, and metabolite formation is monitored by HPLC. InhA inhibition is measured using a spectrophotometric assay with 2-trans-enoyl-CoA substrates.
|
| Cell Assay |
In vitro cell experiments use M. tuberculosis cultures or macrophage infection models. THP-1 or primary macrophages are infected with M. tuberculosis and treated with prothionamide (0.1–10 µg/mL). Intracellular bacterial survival is assessed by CFU counting. Cytotoxicity is evaluated in HepG2 or Vero cells to determine selectivity indices.
|
| Animal Protocol |
Mouse models of tuberculosis (e.g., BALB/c or C57BL/6) are infected by aerosol or intravenous routes and treated with prothionamide by oral gavage at 25–100 mg/kg/day for 4–8 weeks. Bacterial burden in lungs and spleen is quantified by CFU. Pharmacokinetic studies use the deuterated internal standard for LC-MS/MS quantification of prothionamide in plasma and tissues.
|
| References |
|
| Molecular Formula |
C9H12N2S
|
|---|---|
| Molecular Weight |
185.300788879395
|
| CAS # |
1330261-26-1
|
| Related CAS # |
Prothionamide;14222-60-7
|
| Appearance |
Typically exists as solid at room temperature
|
| SMILES |
S=C(C1=CC(CC([2H])([2H])C([2H])([2H])[2H])=NC=C1)N
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 5.3967 mL | 26.9833 mL | 53.9665 mL | |
| 5 mM | 1.0793 mL | 5.3967 mL | 10.7933 mL | |
| 10 mM | 0.5397 mL | 2.6983 mL | 5.3967 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
