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ChemicalBook >  Product Catalog >  Biochemical Engineering >  Inhibitors >  Nuclear transcription factor (NF-κB) >  NF-κB inhibitor >  4-ThiazolecarboxaMide, N-(6-benzoyl-1H-benziMidazol-2-yl)-2-(1-thieno[3,2-d]pyriMidin-4-yl-4-piperidinyl)-

4-ThiazolecarboxaMide, N-(6-benzoyl-1H-benziMidazol-2-yl)-2-(1-thieno[3,2-d]pyriMidin-4-yl-4-piperidinyl)-

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4-ThiazolecarboxaMide, N-(6-benzoyl-1H-benziMidazol-2-yl)-2-(1-thieno[3,2-d]pyriMidin-4-yl-4-piperidinyl)- Basic information

Product Name:
4-ThiazolecarboxaMide, N-(6-benzoyl-1H-benziMidazol-2-yl)-2-(1-thieno[3,2-d]pyriMidin-4-yl-4-piperidinyl)-
Synonyms:
  • 4-ThiazolecarboxaMide, N-(6-benzoyl-1H-benziMidazol-2-yl)-2-(1-thieno[3,2-d]pyriMidin-4-yl-4-piperidinyl)-
  • SC75741
  • V 1810
  • N-(6-Benzoyl-1H-benzimidazol-2-yl)-2-(1-thieno[3,2-d]pyrimidin-4-yl-4-piperidinyl)-4-thiazolecarboxamide
  • 75741
  • CS-2697
  • 4-ThiazolecarboxaMide, N-(6-benzoyl-1H-benziMidazol-2-yl)-2-(1-thieno[3,2-d]pyriMidin-4-yl-4-piperidinyl)- USP/EP/BP
  • SC75741, 10 mM in DMSO
CAS:
913822-46-5
MF:
C29H23N7O2S2
MW:
565.67
Product Categories:
  • Inhibitors
Mol File:
913822-46-5.mol
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4-ThiazolecarboxaMide, N-(6-benzoyl-1H-benziMidazol-2-yl)-2-(1-thieno[3,2-d]pyriMidin-4-yl-4-piperidinyl)- Chemical Properties

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
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4-ThiazolecarboxaMide, N-(6-benzoyl-1H-benziMidazol-2-yl)-2-(1-thieno[3,2-d]pyriMidin-4-yl-4-piperidinyl)- Usage And Synthesis

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%.
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

4-ThiazolecarboxaMide, N-(6-benzoyl-1H-benziMidazol-2-yl)-2-(1-thieno[3,2-d]pyriMidin-4-yl-4-piperidinyl)-Supplier

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4-ThiazolecarboxaMide, N-(6-benzoyl-1H-benziMidazol-2-yl)-2-(1-thieno[3,2-d]pyriMidin-4-yl-4-piperidinyl)-(913822-46-5)Related Product Information