Suramin hexasodium salt (Synonyms: BAY 205, Germanin, NF 060) |
Catalog No.GC16832 |
Suramin hexasodium salt(Suramin hexasodium salt)는 가역적이고 경쟁적인 protein-tyrosine phosphatase (PTPases) 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 129-46-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines |
Vero E6 and Calu-3 |
Preparation Method |
Vero E6 and Calu-3 cells were preincubated for 30 min with 2-fold serial dilutions of a starting concentration of 200 μM Suramin hexasodium salt and subsequently infected with 2 × 104 PFU of SARS-CoV-2 (MOI of 1 on Vero E6 cells) in 50 μl medium with compound. |
Reaction Conditions |
200μM for 16 hours or 21 hours |
Applications |
RT-qPCR revealed that the SARS-CoV-2 RNA levels decreased upon Suramin hexasodium salt treatment in a dose-dependent manner, showing a 3-log reduction at the highest concentration tested (200 μM) |
Animal experiment [2]: | |
Animal models |
C57BL/6JNarl (B6) mice |
Preparation Method |
Suramin hexasodium salt was diluted in normal saline, and indicated doses were administered at 4 h pre-infection, 1day post-infection or/and 3day post-infection (dpi) via the intraperitoneal (ip) route. Specifically, each dose comprised 0, 0.25, 0.5, 1 or 2 mg suramin hexasodium salt. |
Dosage form |
Intraperitoneal injection, 0, 0.25, 0.5, 1 or 2 mg |
Applications |
Viral loads in sera of mock-treated mice infected with the 0810bTw, 0611aTw and 0706aTw CHIKV strains at the 2 dpi peak were 5.8, 3 and 4.2 Log10 CCID50/ml, respectively (Fig. 2A). To parallel, viral titers of suramin hexasodium salt-treated sera after received two doses (pre 4 h and 1 dpi) were 5, 2.5 and 3.8 Log10 CCID50/ml for 0810bTw, 0611aTw and 0706aTw strains, respectively. |
References: [1]. Salgado-Benvindo, C., Thaler, M., Tas, A., Ogando, N. S., et al. Suramin inhibits SARS-CoV-2 infection in cell culture by interfering with early steps of the replication cycle. 2020. Antimicrob. Agents Chemother. 20, DOI: 10.1128/AAC.00900-20. [2]. Kuo SC, Wang YM, Ho YJ, Chang TY, Lai ZZ, Tsui PY, Wu TY, Lin CC. 2016. Suramin treatment reduces chikungunya pathogenesis in mice. Antiviral Res 134:89–96. |
Suramin hexasodium salt is a polysulfonated naphthylurea with various biological activities. Suramin hexasodium salt is a DNA topoisomerase II inhibitor with an IC50 of 5 μM [1].
Suramin hexasodium salt at 300–600 μg/ml significantly inhibited HO-8910 PM and HeLa cell growth at 24 h, in both a time-dependent and dose-dependent manner, with an IC50 of 320 μg/ml and 475 μg/ml, respectively. Suramin hexasodium salt at 300 μg/ml significantly decreased the expression of Hpa mRNA (P < 0.005) and protein (P < 0.005) in both HO-8910 PM and HeLa cells at 48 h [2]. Suramin hexasodium salt shows antiviral activity against the newly emerged virus strain SARS-CoV-2 [3,4].Solution based assays of RdRp inhibition determined that the half-maximal inhibition concentration (IC50) of suramin hexasodium salt is 0.26 µM, Cell-based experiments indicated that suramin hexasodium salt was able to inhibit SARS-CoV-2 duplication in Vero E6 cells with a half-maximal effective concentration (EC50) of roughly 2.9 µM [3].Suramin hexasodium salt treatment of infected Vero E6 cells led to a reduction in extracellular viral RNA levels of up to 3 log. The highest concentration of compound that was used proved harmless to the cells; also, cytotoxicity was observed previously only above 5 mM. Suramin hexasodium salt also displayed antiviral efficacy in a human lung epithelial cell line, and we observed a >2 log reduction in levels of infectious virus progeny in suramin hexasodium salt -treated cells (CC50/EC90 = >55) [4].
Suramin hexasodium salt has therapeutic effects on CHIKV-infected mice. Suramin hexasodium salt treatment ameliorated foot swelling and reduced inflammatory infiltration, which corresponded to reduced viremia and viral antigen expression in infected tissues. Suramin hexasodium salt induces a dose-dependent reduction in foot swelling in CHIKV 0810bTw-infected mice, and the vary degrees of decreased viremia that was detected in suramin hexasodium salt -treated mice further confirmed therapeutic effects of this drug. In the time-related assay, a single dose of 2 mg suramin hexasodium salt (at 4 h pre-infection) or double doses of 2 mg suramin hexasodium salt (at 1 dpi and 3 dpi) significantly decreased disease score and viremia compared to mock-treated mice.
References:
[1]. Bojanowski K, et al. Suramin is an inhibitor of DNA topoisomerase II in vitro and in Chinese hamster fibrosarcomacells. Proc Natl Acad Sci U S A. 1992 Apr 1;89(7):3025-9.
[2]. Li, H.; Li, H.; Qu, H.; et al. Suramin inhibits cell proliferation in ovarian and cervical cancer by downregulating heparanase expression. Cancer Cell Int. 2015, 15, 1–11
[3]. Yin, W. et al. Structural basis for inhibition of the SARS-CoV-2 RNA polymerase by suramin. Nat. Struct. Mol. Biol. 28, 319–325 (2021).
[4]. Salgado-Benvindo, C., Thaler, M., Tas, A., Ogando, N. S., et al. Suramin inhibits SARS-CoV-2 infection in cell culture by interfering with early steps of the replication cycle. 2020. Antimicrob. Agents Chemother. 20, DOI: 10.1128/AAC.00900-20
[5]. Kuo SC, Wang YM, Ho YJ, Chang TY, Lai ZZ, Tsui PY, Wu TY, Lin CC. 2016. Suramin treatment reduces chikungunya pathogenesis in mice. Antiviral Res 134:89–96.
Cas No. | 129-46-4 | SDF | |
Synonyms | BAY 205, Germanin, NF 060 | ||
Chemical Name | sodium 8,8'-((3,3'-((3,3'-(carbonylbis(azanediyl))bis(benzoyl))bis(azanediyl))bis(4-methylbenzoyl))bis(azanediyl))bis(naphthalene-1,3,5-trisulfonate) | ||
Canonical SMILES | [O-]S(=O)(C1=C(C(NC(C2=CC=C(C)C(NC(C3=CC=CC(NC(NC4=CC(C(NC5=CC(C(NC(C(C6=CC(S([O-])(=O)=O)=C7)=C7S([O-])(=O)=O)=CC=C6S([O-])(=O)=O)=O)=CC=C5C)=O)=CC=C4)=O)=C3)=O)=C2)=O)=CC=C8S([O-])(=O)=O)C8=CC(S([O-])(=O)=O)=C1)=O.[Na+].[Na+].[Na+].[Na+].[Na+].[Na+] | ||
Formula | C51H34N6Na6O23S6 | M.Wt | 1429.15 |
Solubility | > 71.45mg/mL in Water; > 50mg/mL in DMSO | Storage | 4°C, protect from light |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 0.6997 mL | 3.4986 mL | 6.9972 mL |
5 mM | 0.1399 mL | 0.6997 mL | 1.3994 mL |
10 mM | 0.07 mL | 0.3499 mL | 0.6997 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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