SC75741

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SC75741 是一种有效的 NF-κB 抑制剂，EC50 为 200 nM。

SC75741 is a NF-kappaB inhibitor. SC75741 protects mice against highly pathogenic avian influenza A virus. SC75741 significantly protects mice against infection with highly pathogenic avian influenza A viruses of the H5N1 and H7N7 subtypes. SC75741 efficiently blocks influenza virus propagation and confers a high barrier for development of viral resistance.(In Vitro):SC75741 (5 μM; 24-96 hours) inhibits long-term A549 cells proliferation.SC75741 (1-10 μM; 5.5-65 hours) reduces A549 cells viability in a concentration-dependent manner indicating a cytostatic effect for A549 cells within a time frame of about 50 and 65?hours.SC75741 (5 μM; 24 hours) strongly inhibits 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 mRNA by 90% in the lungs of infected mice.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.

SC75741 (5 μM; 24-96 hours) inhibits long-term A549 cells proliferation.SC75741 (1-10 μM; 5.5-65 hours) reduces A549 cells viability in a concentration-dependent manner indicating a cytostatic effect for A549 cells within a time frame of about 50 and 65?hours.SC75741 (5 μM; 24 hours) strongly inhibits cleavage of the effector caspase 3 induced upon H7N7-infection. Cell Proliferation Assay Cell Line:A549 cells Concentration:5?μM Incubation Time:24, 48, 72 and 96?hours Result:Inhibited long-term cell proliferation Cell Viability Assay Cell Line:A549 cells Concentration:1, 2, 5 or 10?μM Incubation Time:5.5, 29, 50, 65 hours Result:Reduced cells viability in a concentration-dependent manner.Western Blot Analysis Cell Line:MDCK cells Concentration:5?μM Incubation Time:24 hours Result:Inhibited cleavage of the effector caspase 3 induced upon H7N7-infection.

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.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. Animal Model:Inbred female C57BL/6 mice at the age of 6-8 weeks 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 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.

SC75741 | SC-75741 | SC 75741

Cell Cycle/DNA Damage

GPR

NF-κB

Infection

——

913822-46-5

565.67

C29H23N7O2S2

>98% (HPLC)

DMSO : ≥ 125 mg/mL; 220.98 mM

O=C(NC1=NC2=CC=C(C=C2N1)C(=O)C1=CC=CC=C1)C1=CSC(=N1)C1CCN(CC1)C1=C2SC=CC2=NC=N1

N-(6-benzoyl-1H-benzimidazol-2-yl)-2-(1-thieno[3,2-d]pyrimidin-4-yl-4-piperidinyl)-4-thiazolecarboxamide

(-20℃)

With Ice Pack

≥ 2 years