| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Thiambutosine targets Mycobacterium leprae and mushroom tyrosinase. It exhibits inhibitory activity against Mycobacterium leprae, the causative agent of leprosy, and against mushroom tyrosinase. The compound's mechanism of action against M. leprae is not fully understood, but it is thought to involve inhibition of essential metabolic pathways.
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|---|---|
| ln Vitro |
In vitro, Thiambutosine exhibits inhibitory activity against Mycobacterium leprae and mushroom tyrosinase. It has an EC50 of 11 µg/mL against mycobacteria. The compound's in vitro activity is well-characterized and forms the basis for its use in leprosy research.
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| ln Vivo |
In vivo, Thiambutosine can inhibit leprosy infection in animal experiments when administered by intramuscular injection. Oral activity is low, making parenteral administration necessary for in vivo efficacy. The compound's in vivo efficacy is attributed to its inhibitory activity against M. leprae.
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| Enzyme Assay |
Cell-free assays for Thiambutosine are performed using M. leprae cultures or mycobacterial strains. Minimum inhibitory concentrations (MICs) are determined using broth microdilution methods. Tyrosinase inhibition is assessed using enzymatic activity assays with L-DOPA as substrate. These cell-free assays are essential for characterizing the potency of Thiambutosine as an inhibitor of M. leprae and tyrosinase.
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| Cell Assay |
In cellular assays, mycobacterial cultures are treated with Thiambutosine at varying concentrations. Bacterial growth is assessed by measuring optical density or colony-forming units. Inhibition of M. leprae growth is evaluated. These cellular assays are crucial for understanding the functional consequences of Thiambutosine treatment and for validating its activity as an antileprotic agent.
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| Animal Protocol |
In vivo efficacy of Thiambutosine is evaluated in animal models of leprosy infection. The compound is administered by intramuscular injection. Bacterial load in tissues and clinical signs of infection are monitored to assess therapeutic efficacy. These in vivo studies are essential for confirming the compound's efficacy in a physiologically relevant context.
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| ADME/Pharmacokinetics |
Thiambutosine has low oral bioavailability. Following intramuscular injection, the compound is absorbed and distributed to tissues. Pharmacokinetic parameters are determined in animal studies. The compound's low oral activity necessitates parenteral administration for in vivo efficacy.
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| Toxicity/Toxicokinetics |
Toxicological evaluation includes assessment of local and systemic toxicity following intramuscular injection. Standard toxicology studies in animals evaluate organ toxicity, hematological parameters, and safety margins. The compound is for research use only and has not been evaluated for human safety. Standard safety precautions should be followed when handling Thiambutosine, including the use of appropriate personal protective equipment and adherence to institutional safety guidelines.
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| References |
Smith TC, Richardus JH. Relapse rates in patients treated with dapsone monotherapy and combinations of dapsone and thiambutosine, thiacetazone, isoniazid and streptomycin in the pre-MDT era. Int J Lepr Other Mycobact Dis. 1994 Sep;62(3):353-8. PubMed PMID: 7525795.
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| Additional Infomation |
Thiambutosine (CAS 500-89-0) is a research compound for laboratory use only. It is an inhibitor of Mycobacterium leprae used in leprosy research. The compound has low oral activity and is administered by intramuscular injection in animal experiments. It is not approved for human therapeutic use and is intended for research purposes only. The compound should be stored according to the manufacturer's recommendations, typically at -20°C, to ensure stability. When handling Thiambutosine, researchers should follow standard safety protocols for handling chemical reagents, including the use of appropriate personal protective equipment and working in a well-ventilated area.
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| Molecular Formula |
C19H25N3OS
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|---|---|
| Molecular Weight |
343.489
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| Exact Mass |
343.172
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| CAS # |
500-89-0
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| Related CAS # |
500-89-0;
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| PubChem CID |
3002003
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.187g/cm3
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| Boiling Point |
478.9ºC at 760mmHg
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| Flash Point |
243.4ºC
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| Index of Refraction |
1.663
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| LogP |
4.886
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
24
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| Complexity |
362
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S=C(N([H])C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])N([H])C1C([H])=C([H])C(=C([H])C=1[H])N(C([H])([H])[H])C([H])([H])[H]
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| InChi Key |
JYCBKPOKWDDOOV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H25N3OS/c1-4-5-14-23-18-12-8-16(9-13-18)21-19(24)20-15-6-10-17(11-7-15)22(2)3/h6-13H,4-5,14H2,1-3H3,(H2,20,21,24)
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| Chemical Name |
1-(p-Butoxyphenyl)-3-(p-dimethylaminophenyl)-2-thiourea
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| Synonyms |
Thiambutosine SC 682 SC682 SC-682 SU-1906 SU1906 SU 1906 Summit 1906 Ciba 1906
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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 |
| 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) |
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
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| 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 | 2.9113 mL | 14.5565 mL | 29.1129 mL | |
| 5 mM | 0.5823 mL | 2.9113 mL | 5.8226 mL | |
| 10 mM | 0.2911 mL | 1.4556 mL | 2.9113 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.
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