| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
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| Other Sizes |
|
| Targets |
Nucleic acids (specifically binds to guanine-rich regions without intercalation, acting as a conformational probe) [2]
Lysosomes (stabilizes lysosomal membranes and exhibits anti-proteolytic activity) [1] |
|---|---|
| ln Vitro |
Research has indicated that following polyribosome release using Nonidet P-40 (NP-40), the trypanocidal dye Hydroxystilbamidine bis(methanesulfonate) can repair mRNA. The sucrose gradient examination of detergent-lysed postnuclear supernatants was utilized to examine the size distribution of NP-40-released polyribosomes. Polyribosomes can be seen in the heparin gradient, but a significant peak of very heavy polyribosomes can be seen in the hydroxystilmidine bis(methanesulfonate) gradient. If hydroxystilamidine bis(methanesulfonate) is present prior to adding NP-40, this peak can be consistently obtained[3].
Hydroxystilbamidine demonstrated significant immunosuppressive effects by inhibiting the release of lysosomal enzymes from macrophages. Treatment with 10 μg/mL reduced β-glucuronidase release by 50% in cultured mouse peritoneal macrophages, indicating lysosomal stabilization and suppression of inflammatory responses. [1] The drug exhibited antifungal activity against Blastomyces dermatitidis at concentrations of 1–5 μg/mL, disrupting fungal cell integrity through lysosome-mediated mechanisms. [1] In nucleic acid binding studies, Hydroxystilbamidine selectively bound to double-stranded RNA and guanine-rich DNA regions via minor groove interactions, altering nucleic acid conformation without intercalation. This was confirmed by spectral shifts (absorption peak at 335 nm) and fluorescence quenching assays. [2] |
| ln Vivo |
When given before stimulating sheep red blood cells (SRBC), hydroxystilmidine bis(methanesulfonate) is a highly effective inhibitor of the plaque-forming cell (PFC) response. In treated mice, hydroxystilbamidine bis(methanesulfonate) suppresses the plaque response. Throughout the trial, mice treated with hydroxystilmidine bis(methanesulfonate) showed reduced PFC; however, this reduction in inhibition was not sustained over time. PFC levels in normal and hydroxystilamidine bis(methanesulfonate)-treated animals were nearly at baseline by day 14 [1].
Intraperitoneal administration of 10 mg/kg Hydroxystilbamidine in mice suppressed delayed-type hypersensitivity (DTH) responses to sheep red blood cells by 70%, attributed to lysosome stabilization and reduced protease release from immune cells. [1] |
| Enzyme Assay |
Nucleic acids (specifically binds to guanine-rich regions without intercalation, acting as a conformational probe) [2]
; Lysosomes (stabilizes lysosomal membranes and exhibits anti-proteolytic activity) [1] |
| Cell Assay |
Mouse peritoneal macrophages were harvested, cultured in medium, and pre-treated with Hydroxystilbamidine (1–10 μg/mL) for 30 min. Cells were then stimulated with zymosan particles (1 mg/mL) for 60 min. β-glucuronidase release in supernatants was measured to evaluate lysosomal membrane stability. [1]
For antifungal testing, Blastomyces dermatitidis was incubated with Hydroxystilbamidine (0.1–10 μg/mL) in broth culture at 37°C for 48 hours. Growth inhibition was determined by turbidity measurements at 600 nm. [1] |
| References |
|
| Additional Infomation |
Hydroxystilbamidine acts as a lysosome-stabilizing agent that inhibits proteolytic enzyme release, thereby suppressing immune cell activation and inflammation. This mechanism underlies its immunosuppressive and antifungal effects. [1]
The drug serves as a unique nonintercalating nucleic acid probe due to its selective binding to guanine bases via hydrogen bonding and electrostatic interactions, inducing conformational changes in double-stranded RNA and GC-rich DNA regions. [2] |
| Molecular Formula |
C16H16N4O.2[CH4O3S]
|
|---|---|
| Molecular Weight |
472.53576
|
| Exact Mass |
472.108
|
| Elemental Analysis |
C, 45.75; H, 5.12; N, 11.86; O, 23.70; S, 13.57
|
| CAS # |
223769-64-0
|
| Related CAS # |
495-99-8
|
| PubChem CID |
135818273
|
| Appearance |
Light yellow to yellow solid powder
|
| Hydrogen Bond Donor Count |
7
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
31
|
| Complexity |
505
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CS(=O)(=O)O.CS(=O)(=O)O.C1=CC(=CC=C1/C=C/C2=C(C=C(C=C2)C(=N)N)O)C(=N)N
|
| InChi Key |
YGNSQKCULHSJDC-HFPMQDOPSA-N
|
| InChi Code |
InChI=1S/C16H16N4O.2CH4O3S/c17-15(18)12-5-2-10(3-6-12)1-4-11-7-8-13(16(19)20)9-14(11)21;2*1-5(2,3)4/h1-9,21H,(H3,17,18)(H3,19,20);2*1H3,(H,2,3,4)/b4-1+;;
|
| Chemical Name |
4-[(E)-2-(4-carbamimidoylphenyl)ethenyl]-3-hydroxybenzenecarboximidamide;methanesulfonic acid
|
| Synonyms |
223769-64-0; Hydroxystilbamidine bis(methanesulfonate); HydroxystilbaMidine bis(Methanesulfonate) [Know as FluoroGold(TM), TM of FluorochroMe]; 4-[(E)-2-(4-carbamimidoylphenyl)ethenyl]-3-hydroxybenzenecarboximidamide;methanesulfonic acid; 2-Hydroxystilbene-4,4'-dicarboxamidine bis(methanesulfonate); NCGC00166289-01; DTXSID7046592; Hydroxystilbamidine Dimesylate;
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~50 mg/mL (~105.81 mM)
H2O : ~50 mg/mL (~105.81 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 | 2.1162 mL | 10.5811 mL | 21.1622 mL | |
| 5 mM | 0.4232 mL | 2.1162 mL | 4.2324 mL | |
| 10 mM | 0.2116 mL | 1.0581 mL | 2.1162 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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