SC75741 |
| Catalog No.GC10088 |
NF-κB inhibitor, potent
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 913822-46-5
Sample solution is provided at 25 µL, 10mM.
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SC75741 is a potent NF-κB inhibitor with EC50 value of 200 nM.
NF-kB is a protein complex that regulates the expression of immunoreceptors, inflammatory cytokines and chemokines and is commonly regarded as a major antiviral factor. However, it has been shown that influenza A viruses exploit this signaling pathway for efficient replication [1].
In MDCK cells, inhibitory potential of 5 uM SC75741 on virus replication is highest at later stages of infection. In the human alveolar type II epithelial cell line A549 infected with H5N1 and H7N7 viruses, SC75741 provoked an efficient reduction of virus titers in a dose-dependent way [1].
In the lung of infected mice, SC75741 reduces viral replication and H5N1-induced IL6 and IP-10 expression. In addition, SC75741 also reduced cytokine production in vivo that is involved in hypercytokinemia mediated by influenza virus infection. Importantly, SC75741 exhibits a high barrier for virus variants [1].
References:
[1]. Ehrhardt C, Rückle A, Hrincius ER, et al. The NF-κB inhibitor SC75741 efficiently blocks influenza virus propagation and confers a high barrier for development of viral resistance. Cell Microbiol, 2013, 15(7): 1198-1211.
| Cell experiment [1]: | |
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Cell lines |
Epithelial Madin–Darbycanine kidney cells (MDCK) |
|
Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
1 μM, 2 μM or 5 μM, 24 h |
|
Applications |
In Epithelial Madin–Darbycanine kidney cells (MDCK), SC75741 dose-dependently inhibited virus propagation. Treatment of MDCK cells with SC75741 (5 μM) inhibited virus replication in mono- and multicyclic infections with highest efficiency at later stages of infection replication of influenza A and B viruses. SC75741 exhibited antiviral activity on H1N1 and H3N2 influenza A virus subtype and influenza B virus replication. In the human alveolar type II epithelial cell line A549, SC75741 provoked an efficient reduction of progeny virus titres in a concentration-dependent manner. Prolonged treatment with SC75741 (55 h and 65 h) reduced cell viability in a concentration-dependent manner. SC75741 (5 μM) inhibited transcriptional activation of NF-kB-dependent genes. SC75741 (5 μM) reduced virus-induced expression of the NF-kB target genes IL-6 and TRAIL but not IFN-b or IRF-3 activity. SC75741 (5 μM) showed a high barrier for development of resistant virus variants. |
| Animal experiment [1]: | |
|
Animal models |
C57BL/6 mice |
|
Dosage form |
Intraperitoneal administration, 15 mg/kg |
|
Application |
SC75741 (15 mg/kg, i.p.) reduced virus replication and cytokine expression in mice lungs after H5N1 influenza virus infection. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Ehrhardt C, Rückle A, Hrincius E R, et al. The NF‐κB inhibitor SC75741 efficiently blocks influenza virus propagation and confers a high barrier for development of viral resistance[J]. Cellular microbiology, 2013, 15(7): 1198-1211. |
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| Cas No. | 913822-46-5 | SDF | |
| Chemical Name | (Z)-N-(6-benzoyl-1H-benzo[d]imidazol-2-yl)-2-(1-(thieno[3,2-d]pyrimidin-4-yl)piperidin-4-yl)thiazole-4-carbimidic acid | ||
| Canonical SMILES | O=C(C1=CC2=C(N=C(/N=C(O)/C3=CSC(C4CCN(C5=NC=NC6=C5SC=C6)CC4)=N3)N2)C=C1)C7=CC=CC=C7 | ||
| Formula | C29H23N7O2S2 | M.Wt | 565.67 |
| Solubility | ≥ 37.6 mg/mL in DMSO, ≥ 12.56 mg/mL in EtOH with ultrasonic and warming | Storage | Desiccate at -20°C |
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7678 mL | 8.8391 mL | 17.6782 mL |
| 5 mM | 0.3536 mL | 1.7678 mL | 3.5356 mL |
| 10 mM | 0.1768 mL | 0.8839 mL | 1.7678 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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