| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
Compared to CQ, the intrinsic antimalarial characteristics of the calcium channel blockers VIZ and Fantofarone (SR) are evidently weaker, and they both seem to be marginally more effective against CQ-resistant parasites than against CQ-sensitive parasites. Strength. Interestingly, Fantofarone was approx. Ten times as powerful than elavil. When it comes to two strains of P. fdciparum, fantofarone (SR) is ten times more effective than the phenylalkylamine verapamil (VR). Both calcium channel blockers, with verapamil being two to three times more powerful than Fantofarone, increased the CQ-sensitive activity of CQ-resistant P. fufcipurum strains, as demonstrated by isobolograms. Additionally, when taken with identical IC50 subinhibitory fractions, VR reduces CQ resistance 2–3 times more effectively than Fantofarone [1].
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| ln Vivo |
Treatment with ventofalone (50 mg/kg, intravenous) or isosorbide dinitrate (0.3 mg/kg, intravenous) decreased the incidence and severity of vasospasm, while verapamil (0.2 mg/kg, intravenous injection) is far less effective. Isosorbide dinitrate largely prevented distal AIV, but it had no discernible effect on proximal diameter reduction. Fantofarone was found to be the most efficient drug in reducing both proximal and distal vasospasm. Throughout the experiment, this compound greatly decreased AIV. There is no discernible decrease in AIV with verapamil[2].
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| References |
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| Molecular Formula |
C31H38N2O5S
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|---|---|
| Molecular Weight |
550.714
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| Exact Mass |
550.25
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| CAS # |
114432-13-2
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| PubChem CID |
119349
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.16g/cm3
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| Index of Refraction |
1.573
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| LogP |
6.936
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
39
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| Complexity |
825
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ITAMRBIZWGDOHW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H38N2O5S/c1-23(2)27-22-33-18-7-6-9-28(33)31(27)39(34,35)26-13-11-25(12-14-26)38-20-8-17-32(3)19-16-24-10-15-29(36-4)30(21-24)37-5/h6-7,9-15,18,21-23H,8,16-17,19-20H2,1-5H3
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| Chemical Name |
N-[2-(3,4-dimethoxyphenyl)ethyl]-N-methyl-3-[4-(2-propan-2-ylindolizin-1-yl)sulfonylphenoxy]propan-1-amine
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| Synonyms |
SR33557; SR-33557; SR 33557
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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 : ~100 mg/mL (~181.58 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8158 mL | 9.0792 mL | 18.1584 mL | |
| 5 mM | 0.3632 mL | 1.8158 mL | 3.6317 mL | |
| 10 mM | 0.1816 mL | 0.9079 mL | 1.8158 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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