913822-46-5
913822-46-5 structure
- Name: SC75741
- Chemical Name: N-(6-benzoyl-1H-benzimidazol-2-yl)-2-[1-(2H-thieno[3,2-d]pyrimidin-1-yl)piperidin-4-yl]-1,3-thiazole-4-carboxamide
- CAS Number: 913822-46-5
- Molecular Formula: C29H23N7O2S2
- Molecular Weight: 567.68400
- Catalog: Biochemical Inhibitor Nuclear transcription factor (NF-κB) NF-κB inhibitor
- Create Date: 2017-12-16 02:58:23
- Modify Date: 2024-01-03 14:05:59
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SC75741 is a broad and efficient NF-κB inhibitor with an IC50 of 200 nM for p65[1]. SC75741 blocks influenza viruses (IV) replication in non-toxic concentrations. SC75741 impairs DNA binding of the NF-κB subunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors. SC75741 subsequently inhibits caspase activation and blocks caspase-mediated nuclear export of viral ribonucleoproteins[2].
| Name | N-(6-benzoyl-1H-benzimidazol-2-yl)-2-[1-(2H-thieno[3,2-d]pyrimidin-1-yl)piperidin-4-yl]-1,3-thiazole-4-carboxamide |
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| Synonyms | SC75741 |
| Description | SC75741 is a broad and efficient NF-κB inhibitor with an IC50 of 200 nM for p65[1]. SC75741 blocks influenza viruses (IV) replication in non-toxic concentrations. SC75741 impairs DNA binding of the NF-κB subunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors. SC75741 subsequently inhibits caspase activation and blocks caspase-mediated nuclear export of viral ribonucleoproteins[2]. |
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| Related Catalog | |
| Target |
p65:200 nM (IC50) Caspase |
| In Vitro | SC75741 (1-10 μM; 5.5-65 hours) reduces A549 cells viability in a concentration-dependent manner indicating a cytostatic effect within a time frame of about 50 and 65 hours[2]. SC75741 (5 μM; 24 hours) strongly inhibits cleavage of the effector caspase 3 induced upon H7N7-infection[2]. Cell Viability Assay[2] Cell Line: A549 cells Concentration: 1, 2, 5 or 10 μM Incubation Time: 5.5, 29, 50, 65 hours Result: Cells viability was reduced in a concentration-dependent manner indicating a cytostatic effect. Western Blot Analysis[2] Cell Line: MDCK cells Concentration: 5 μM Incubation Time: 24 hours Result: Inhibited cleavage of the effector caspase 3 induced upon H7N7-infection. |
| In Vivo | SC75741 (intraperitoneal injection; 15 mg/kg; for 2 days) leads to a reduced propagation of the H5N1 virus in the lungs of infected mice[2]. The plasma-levels of SC74751 (intravenously of 5 mg/kg and intraperitoneally of 15 mg/kg; for 3.5 and 6 hours) after i.v. administration decreases mono-exponentially and half-life is roughly 40 min. After i.p. administration, elimination of SC75741 seems to be limited by a slow uptake from the peritoneum and a half-life of 55 min is observed[1]. Animal Model: Inbred female C57BL/6 mice at the age of 6-8 weeks[2] Dosage: 15 mg/kg Administration: Intraperitoneal injection; for 2 days Result: The amount of viral mRNA was reduced by 90%. Animal Model: Inbred female C57BL/6 mice at the age of 6-8 weeks[1] Dosage: 5 mg/kg or 15 mg/kg Administration: Intravenously of 5 mg/kg and intraperitoneally of 15 mg/kg; 3.5 and 6 hours Result: Half-life was roughly 40 min and 55 min for i.v. and i.p. administration, respectively. |
| References |
| Molecular Formula | C29H23N7O2S2 |
|---|---|
| Molecular Weight | 567.68400 |
| Exact Mass | 567.15100 |
| PSA | 166.55000 |
| LogP | 5.37770 |
| Storage condition | -20℃ |