| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Surfen targets heparan sulfate (HS) and other glycosaminoglycans (GAGs). By binding to HS, it inhibits FGF2 binding and signal transduction. It neutralizes the anticoagulant activity of heparins. Surfen also targets protein-tyrosine phosphatases (PTPs), particularly PTP1B. It binds to glycosaminoglycans and reduces tau hyperphosphorylation.
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|---|---|
| ln Vitro |
Surfen dihydrochloride is a potent HS (heparan sulfate) antagonist that binds to glycosaminoglycans. It neutralizes the anticoagulant activity of both unfractionated and low molecular weight heparins. Surfen inhibits FGF2 binding to CHO cells with an IC50 of 5 µM and FGF2-induced tube formation by primary mouse endothelial cells. It inhibits cell attachment and virus infection.
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| ln Vivo |
Surfen dihydrochloride is used in vivo as a heparan sulfate antagonist. It neutralizes the anticoagulant activity of heparins. It has antibacterial and antiviral activities. Surfen inhibits anthrax lethal factor, coagulation factor X, and lethal factor.
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| Enzyme Assay |
Surfen is a heparan sulfate antagonist, and its in vitro activity is assessed in binding and functional assays. In binding assays, the compound is incubated with heparan sulfate or other GAGs, and the binding affinity is measured. In functional assays, the inhibition of FGF2 binding and signaling is measured. The neutralization of heparin anticoagulant activity is assessed in coagulation assays.
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| Cell Assay |
Surfen dihydrochloride is dissolved in DMSO and applied to cultured cells at concentrations ranging from 1 µM to 100 µM. The effect on FGF2 binding and signaling is assessed. The effect on cell attachment and virus infection is measured.
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| ADME/Pharmacokinetics |
Surfen dihydrochloride has a molecular weight of 445.34 g/mol and a molecular formula of C21H22Cl2N6O. It is a potent heparan sulfate antagonist. The compound is typically stored as a powder at -20°C for long-term stability. Surfen dihydrochloride is also known as Aminoquinuride dihydrochloride.
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| Toxicity/Toxicokinetics |
Surfen dihydrochloride has a manageable toxicity profile. No significant toxicity has been reported in preclinical studies.
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| References | |
| Additional Infomation |
Surfen dihydrochloride is a potent heparan sulfate (HS) antagonist that binds to glycosaminoglycans. It neutralizes the anticoagulant activity of both unfractionated and low molecular weight heparins. Surfen inhibits FGF2 binding and signal transduction. It binds to glycosaminoglycans and reduces tau hyperphosphorylation. Surfen inhibits cell attachment and virus infection.
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| Molecular Formula |
C21H20N6O.HCL
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|---|---|
| Molecular Weight |
408.88404
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| Exact Mass |
408.147
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| CAS # |
5424-37-3
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| Related CAS # |
3811-56-1;
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| PubChem CID |
79472
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| Appearance |
Off-white to gray solid powder
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| Boiling Point |
587.2ºC at 760 mmHg
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| Flash Point |
308.9ºC
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| LogP |
6.318
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
30
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| Complexity |
513
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NC1=CC=C2N=C(C)C=C(N)C2=C1)NC3=CC=C4N=C(C)C=C(N)C4=C3.Cl.Cl
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| InChi Key |
GKQYGRWQCWWSHN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H20N6O.2ClH/c1-11-7-17(22)15-9-13(3-5-19(15)24-11)26-21(28)27-14-4-6-20-16(10-14)18(23)8-12(2)25-20;;/h3-10H,1-2H3,(H2,22,24)(H2,23,25)(H2,26,27,28);2*1H
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| Chemical Name |
1,3-bis(4-amino-2-methylquinolin-6-yl)urea;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 (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)
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| Solubility (In Vitro) |
H2O : ~8 mg/mL (~17.96 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.61 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 DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4457 mL | 12.2285 mL | 24.4571 mL | |
| 5 mM | 0.4891 mL | 2.4457 mL | 4.8914 mL | |
| 10 mM | 0.2446 mL | 1.2229 mL | 2.4457 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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