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)- Property

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 and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

H400Very toxic to aquatic life

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P273Avoid release to the environment.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P391Collect spillage. Hazardous to the aquatic environment

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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

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

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