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| 25mg |
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Purity: ≥98%
SC75741 (SC-75741; SC 75741) is a novel, selective and potent NF-κB inhibitor with potential antiviral and anti-inflammatory activity. With an EC50 of 200 nM, it blocks NF-κB. In non-toxic concentrations, SC75741 prevents influenza viruses (IV) from replicating. Reduced expression of cytokines, chemokines, and pro-apoptotic factors is the result of SC75741's impairment of NF-κB subunit p65's DNA binding. Following this, SC75741 prevents caspase activation and obstructs the nuclear export of viral ribonucleoproteins caused by caspase. The inhibitory potential of 5 uM SC75741 on virus replication in MDCK cells is greatest later in infection. SC75741 caused an effective, dose-dependent decline in viral titers in the human alveolar type II epithelial cell line A549 that was infected with the H5N1 and H7N7 viruses.
| Targets |
NF-κB (EC50 = 200 nM)
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| ln Vitro |
SC75741 exhibits immunosuppressive activity by limiting the proliferation of human PBMCs with IC50 of 2.2 μM.[1] SC75741 inhibits transcriptional levels of NF-κB mediated signaling, which prevents the replication of influenza A and B viruses. Additionally, SC75741 exhibits a high barrier to the emergence of virus variants with resistance.[2]
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| ln Vivo |
SC75741 (15 mg/kg i.p.) reduces virus replication and cytokine expression in mice lungs after H5N1 influenza virus infection. Mice that have been exposed to SC75741 (intraperitoneal injection; 15 mg/kg; for 2 days) have 90% less H5N1 virus mRNA spread throughout their lungs.
The half-life of SC74751 is approximately 40 minutes, and its plasma levels (intravenously administered at 5 mg/kg and intraperitoneally administered at 15 mg/kg; for 3.5 and 6 hours) decrease mono-exponentially after intravenous administration. SC75741 has a half-life of 55 minutes after being administered intravenously, and it appears that this is due to a slow peritoneal uptake of the drug. |
| Enzyme Assay |
In accordance with the manufacturer's instructions, the A549-NF-κB-SEAP cell line is used to prepare the NF-κB reporter gene assay. In essence, pNF-κB-SEAP reporter gene plasmid-stably transfected A549 cells are plated and given the night to attach. The cells are then stimulated with 10 ng/ml TNF-α for 22 hours after being incubated with the aforementioned compounds at concentrations of 100, 30, 10, 3, 1, 0.3, 0.1, and 0 μM for 5 hours. Using a chemiluminescent SEAP reporter gene assay, the cell's supernatant is examined for SEAP activity.
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| Cell Assay |
Cell viability assay is prepared using a CellTiter-BluTM Cell Viability Assay. Four replicates are measured for each compound concentration.
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| Animal Protocol |
Inbred female C57BL/6 mice at the age of 6-8 weeks[2]
15 mg/kg Intraperitoneal injection; for 2 days |
| References |
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| Molecular Formula |
C29H23N7O2S2
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|---|---|---|
| Molecular Weight |
565.67
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| Exact Mass |
567.151
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| Elemental Analysis |
C, 61.58; H, 4.10; N, 17.33; O, 5.66; S, 11.34
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| CAS # |
913822-46-5
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| Related CAS # |
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| PubChem CID |
23661638
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| Appearance |
Light yellow to brown solid powder
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| LogP |
5.377
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
40
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| Complexity |
915
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=CSC(C2CCN(C3C4=C(C=CS4)N=CN=3)CC2)=N1)NC1NC2C(=CC=C(C(C3C=CC=CC=3)=O)C=2)N=1
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| InChi Key |
QNZVBFMXWNWVKG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H23N7O2S2/c37-24(17-4-2-1-3-5-17)19-6-7-20-22(14-19)34-29(33-20)35-27(38)23-15-40-28(32-23)18-8-11-36(12-9-18)26-25-21(10-13-39-25)30-16-31-26/h1-7,10,13-16,18H,8-9,11-12H2,(H2,33,34,35,38)
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| Chemical Name |
N-(6-benzoyl-1H-benzimidazol-2-yl)-2-(1-thieno[3,2-d]pyrimidin-4-ylpiperidin-4-yl)-1,3-thiazole-4-carboxamide
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.68 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 20.8 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: 2.08 mg/mL (3.68 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*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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