| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
Stilbamidine targets neuromuscular transmission and axonal conduction. As a diamidine compound, it is thought to interact with nucleic acids and proteins, interfering with cellular processes. Its mechanism of action as an antifungal agent is believed to involve binding to DNA and inhibiting nucleic acid synthesis. Stilbamidine also blocks neuromuscular transmission, which may contribute to its pharmacological effects. However, the precise molecular targets and mechanisms of action of Stilbamidine are not fully elucidated. It is used as a research tool to study drug distribution and neuromuscular function.
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| ln Vitro |
Propamidine inhibits the high-affinity pentamidine transporter (HAPT1), although stilamidine dihydrochloride only elicits a low affinity from it. On the other hand, ditomidine and propamidine significantly block the adenosine-sensitive pentamidine transporter (ASPT1). [3H]pentamidine (food=0.7 μM) was measured in the presence of adenosine (IC50=1.2 μM) or Melarsen oxide (IC50=0.7 μM), as well as in the presence of 250 μM adenosine and increasing concentrations of propamidine (IC50=6.1 μM). In the treatment of multiple myeloma, a condition that frequently results in elevated serum protein levels, two diamidine compounds are used: stilamidine dihydrochloride and pentamidine [2].
In vitro, Stilbamidine has been shown to have antifungal activity. Its activity is typically measured using standard antimicrobial susceptibility tests to determine the minimum inhibitory concentration (MIC) against various fungal strains. The compound also blocks neuromuscular transmission, which can be studied using isolated nerve-muscle preparations. However, specific in vitro data, such as IC50 or EC50 values, are not detailed in standard product descriptions. Stilbamidine is a research compound used to study drug distribution and neuromuscular function. |
| ln Vivo |
In vivo, Stilbamidine has been used to treat various fungal infections. It is used to study the distribution of the drug in the organs and tissues of rats following intravenous injection. The compound's ability to block neuromuscular transmission may be relevant to its pharmacological effects and toxicity. Stilbamidine has been investigated for its therapeutic potential, but its use has been limited due to toxicity concerns. It is a research compound used to study drug distribution and neuromuscular function.
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| Enzyme Assay |
In vitro assays for Stilbamidine measure its antifungal activity and its effects on neuromuscular transmission. Antifungal activity is assessed using standard broth microdilution or agar diffusion assays to determine the MIC against various fungal strains. The effects on neuromuscular transmission can be studied using isolated nerve-muscle preparations, where the compound's ability to block muscle contraction is measured. These assays confirm the compound's antifungal activity and its effects on neuromuscular function.
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| Cell Assay |
In vitro cell-based assays for Stilbamidine are used to study its effects on fungal cells and on neuromuscular function. Fungal cultures are treated with Stilbamidine, and cell viability is assessed. The compound's effects on nerve-muscle preparations can be studied using electrophysiological techniques to measure the blockade of neuromuscular transmission. These assays confirm the compound's antifungal activity and its effects on neuromuscular function.
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| Animal Protocol |
In vivo animal experiments for Stilbamidine have been conducted in rats to study the distribution of the drug in organs and tissues following intravenous injection. In a typical study, Stilbamidine is administered intravenously to rats, and the concentration of the drug in various organs and tissues is measured at different time points. These studies provide information on the compound's pharmacokinetics and tissue distribution. Stilbamidine has also been used in animal models of fungal infections to assess its efficacy.
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| ADME/Pharmacokinetics |
Stilbamidine dihydrochloride has a molecular weight of 337.25 g/mol and a molecular formula of C16H18Cl2N4. It has a CAS number of 6935-63-3 and a UNII code of 102Z61E52U. It is a solid compound with a purity of 98% by HPLC. It is soluble in DMSO. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have been studied in the context of its use as a pharmaceutical agent. Stilbamidine is typically administered intravenously.
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| Toxicity/Toxicokinetics |
Stilbamidine is a toxic compound. Its use has been associated with significant side effects, including neurotoxicity, hepatotoxicity, and nephrotoxicity. As a blocker of neuromuscular transmission, it can cause muscle weakness and respiratory depression. Due to its toxicity, its clinical use has been largely replaced by safer antifungal agents. As a research chemical, it should be handled with extreme caution using appropriate safety measures. Its use is limited to research applications.
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| References |
[1]. De Koning HP. Uptake of pentamidine in Trypanosoma brucei brucei is mediated by three distinct transporters: implications for cross-resistance with arsenicals. Mol Pharmacol. 2001 Mar;59(3):586-92.
[2]. BREWER AE.et al. Multiple myeloma treated with stilbamidine and pentamidine. Br Med J. 1948 Dec 4;2(4587):978-82. |
| Additional Infomation |
4,4'-stilbene dimethylamidine dihydrochloride is a polymer.
Stilbamidine dihydrochloride is a research compound and a pharmaceutical agent that has been investigated for its therapeutic potential. It is a diamidine compound derived from stilbene that works primarily in its isethionate salt form. Stilbamidine is a blocker of neuromuscular transmission and axonal conduction. It has been used chiefly in the treatment of various fungal infections. It is used to study the distribution of the drug in the organs and tissues of rats following intravenous injection. Stilbamidine is a research tool for studying drug distribution and neuromuscular function. |
| Molecular Formula |
C16H18CL2N4
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|---|---|
| Molecular Weight |
337.25
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| Exact Mass |
300.114
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| CAS # |
6935-63-3
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| Related CAS # |
Stilbamidine;122-06-5
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| PubChem CID |
6367036
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| Appearance |
Off-white to light yellow solid powder
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| Boiling Point |
456.4ºC at 760 mmHg
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| Flash Point |
229.8ºC
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| LogP |
4.827
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
336
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1C=CC2=CC=C(C=C2)C(=N)N)C(=N)N.Cl.Cl
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| InChi Key |
BJYYRSDXFXLJIV-SEPHDYHBSA-N
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| InChi Code |
InChI=1S/C16H16N4.2ClH/c17-15(18)13-7-3-11(4-8-13)1-2-12-5-9-14(10-6-12)16(19)20;;/h1-10H,(H3,17,18)(H3,19,20);2*1H/b2-1+;;
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| Chemical Name |
4-[(E)-2-(4-carbamimidoylphenyl)ethenyl]benzenecarboximidamide;dihydrochloride
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| Synonyms |
NCI 174 NSC 35605Stilbamidine dihydrochloride
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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) |
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 | 2.9652 mL | 14.8258 mL | 29.6516 mL | |
| 5 mM | 0.5930 mL | 2.9652 mL | 5.9303 mL | |
| 10 mM | 0.2965 mL | 1.4826 mL | 2.9652 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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