| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
Soluflazine targets equilibrative nucleoside transporters (ENTs), a class of proteins responsible for the bidirectional flux of endogenous nucleosides like adenosine across cell membranes. By inhibiting adenosine transport, soluflazine increases extracellular adenosine levels, which contributes to its anticonvulsant and vasodilatory effects.
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| ln Vitro |
Soluflazine is a nucleoside transport inhibitor with anticonvulsant action. It enhances peripheral blood flow by modulating calcium influx and inhibiting platelet aggregation. The compound's ability to inhibit adenosine transport leads to increased extracellular adenosine, which has neuroprotective and vasodilatory effects.
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| ln Vivo |
Soluflazine has anticonvulsant effects in vivo and can be used as an antiepileptic agent. It has also been investigated for its vasodilatory and antiplatelet properties. Specific animal model data and dosing regimens are not extensively detailed in standard reference sources.
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| Enzyme Assay |
Soluflazine's inhibition of nucleoside transport can be assessed using in vitro uptake assays with cells expressing equilibrative nucleoside transporters. Cells are incubated with a radiolabeled nucleoside (e.g., [³H]adenosine) in the presence of varying concentrations of soluflazine. The amount of intracellular radiolabeled nucleoside is measured by scintillation counting. Inhibition of adenosine uptake is calculated, and IC50 values are determined from dose-response curves.
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| Cell Assay |
The cellular activity of soluflazine is evaluated in neuronal cell cultures or cell lines expressing ENTs. Cells are treated with increasing concentrations of soluflazine, and adenosine uptake is measured using radiolabeled adenosine or fluorescent adenosine analogs. Extracellular adenosine levels are measured by HPLC or ELISA. The effect of soluflazine on neuronal excitability or platelet aggregation can also be assessed.
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| Animal Protocol |
Soluflazine is administered orally or intraperitoneally in animal models of epilepsy. In rodent seizure models (e.g., maximal electroshock or pentylenetetrazol-induced seizures), soluflazine is given at various doses. Seizure latency, severity, and incidence are monitored to assess anticonvulsant efficacy.
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| ADME/Pharmacokinetics |
Soluflazine has a molecular formula of C28H30Cl2FN5O3 and a molecular weight of 574.48 g/mol. Its IUPAC name is 4-[2-(2,6-dichloroanilino)-2-oxoethyl]-1-[4-(4-fluorophenyl)-4-pyridin-3-ylbutyl]piperazine-2-carboxamide. Specific pharmacokinetic parameters are not extensively detailed.
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| Toxicity/Toxicokinetics |
The toxicity profile of soluflazine is not extensively documented. As a nucleoside transport inhibitor, potential adverse effects may include those related to increased adenosine levels, such as vasodilation and sedation. Specific LD50 values and organ-specific toxicity data are not readily available.
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| Additional Infomation |
Soluflazine (CAS# 112415-83-5) is also known as R 64719 and R-64719. It is a nucleoside transport inhibitor with anticonvulsant action that can be used as an antiepileptic agent. Soluflazine has also been investigated for its vasodilatory and antiplatelet properties.
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| Molecular Formula |
C28H32CL4FN5O2
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|---|---|
| Molecular Weight |
631.39
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| Exact Mass |
629.129
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| CAS # |
112415-83-5
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| Related CAS # |
734499-99-1;112415-83-5 (HCl);
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| PubChem CID |
163885
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
788.2ºC at 760mmHg
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| Flash Point |
430.5ºC
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| Vapour Pressure |
8.19E-25mmHg at 25°C
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| LogP |
7.828
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
40
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| Complexity |
762
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C([H])=C([H])C([H])=C(C=1N([H])C(C([H])([H])N1C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])C([H])([H])C([H])(C2=C([H])N=C([H])C([H])=C2[H])C2C([H])=C([H])C(=C([H])C=2[H])F)C([H])(C(N([H])[H])=O)C1([H])[H])=O)Cl.Cl[H].Cl[H]
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| InChi Key |
KQZLAOQGNIIITJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H30Cl2FN5O2.2ClH/c29-23-6-1-7-24(30)27(23)34-26(37)18-35-14-15-36(25(17-35)28(32)38)13-3-5-22(20-4-2-12-33-16-20)19-8-10-21(31)11-9-19;;/h1-2,4,6-12,16,22,25H,3,5,13-15,17-18H2,(H2,32,38)(H,34,37);2*1H
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| Chemical Name |
4-[2-(2,6-dichloroanilino)-2-oxoethyl]-1-[4-(4-fluorophenyl)-4-pyridin-3-ylbutyl]piperazine-2-carboxamide;dihydrochloride
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| Synonyms |
R-64719; R 64719; Soluflazine
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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) |
DMSO : ~125 mg/mL (~197.97 mM)
H2O : ~83.33 mg/mL (~131.98 mM) |
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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 | 1.5838 mL | 7.9190 mL | 15.8381 mL | |
| 5 mM | 0.3168 mL | 1.5838 mL | 3.1676 mL | |
| 10 mM | 0.1584 mL | 0.7919 mL | 1.5838 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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