| Identification | Back Directory | [Name]
4-ThiazolecarboxaMide, N-(6-benzoyl-1H-benziMidazol-2-yl)-2-(1-thieno[3,2-d]pyriMidin-4-yl-4-piperidinyl)- | [CAS]
913822-46-5 | [Synonyms]
4-ThiazolecarboxaMide, N-(6-benzoyl-1H-benziMidazol-2-yl)-2-(1-thieno[3,2-d]pyriMidin-4-yl-4-piperidinyl)- | [Molecular Formula]
C29H23N7O2S2 | [MDL Number]
MFCD18206785 | [MOL File]
913822-46-5.mol | [Molecular Weight]
565.669 |
| Chemical Properties | Back Directory | [density ]
1.483±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO (Slightly), Methanol (Slightly, Heated, Sonicated) | [form ]
powder | [pka]
9.11±0.10(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Description]
SC-75741 is an inhibitor of NF-κB (EC50 = 0.1 μM in an NF-κB reporter gene assay). It inhibits replication of human, avian, and swine influenza virus strains in MDCK cells in a concentration-dependent manner. It also reversibly inhibits replication of H5N1 and H7N7 avian influenza virus strains in human A549 cells. In vivo, SC-75741 (15 mg/kg, i.p.) reduces viral mRNA and production of IL-6 and CXCL10/IP-10 in the lungs of H5N1 infected mice. SC-75741 is also protective against H5N1 and H7N7 infection in mice when administered for 7 days prior to or up to 4 days post infection. | [Uses]
SC75741 is a potent NF-κB inhibitor with EC50. | [in vivo]
SC75741 (intraperitoneal injection; 15 mg/kg; for 2 days) leads to a reduced propagation of the H5N1 virus mRNA by 90% 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: | Reduced the amount of viral mRNA by 90%.
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| 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. |
| [target]
NF-κB | [IC 50]
p65: 200 nM (IC50) | [References]
[1] JOHANN LEBAN. A novel class of potent NF-κB signaling inhibitors[J]. Bioorganic & Medicinal Chemistry Letters, 2007, 17 21: Pages 5858-5862. DOI: 10.1016/j.bmcl.2007.08.022
[2] CHRISTINA EHRHARDT. 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. DOI: 10.1111/cmi.12108
[3] EMANUEL HAASBACH . The NF-kappaB inhibitor SC75741 protects mice against highly pathogenic avian influenza A virus[J]. Antiviral research, 2013, 99 3: Pages 336-344. DOI: 10.1016/j.antiviral.2013.06.008 |
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| Company Name: |
Cool Pharm, Ltd
|
| Tel: |
021-60455363 18019463053 |
| Website: |
www.coolpharm.com |
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