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SC75741
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SC75741图片
CAS NO:913822-46-5
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)565.67
FormulaC29H23N7O2S2
CAS No.913822-46-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 35 mg/mL (61.9 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other info

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

InChi Key: QNZVBFMXWNWVKG-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H23N7O2S2/c37-24(17-4-2-1-3-5-17)19-6-7-20-22(14-19)34-29(33-20)35-27(38)23-15-40-28(32-23)18-8-11-36(12-9-18)26-25-21(10-13-39-25)30-16-31-26/h1-7,10,13-16,18H,8-9,11-12H2,(H2,33,34,35,38)

SMILES Code: O=C(C1=CSC(C2CCN(C3=C4C(C=CS4)=NC=N3)CC2)=N1)NC5=NC6=CC=C(C(C7=CC=CC=C7)=O)C=C6N5

Synonyms

SC-75741; SC 75741; SC75741;

实验参考方法
In Vitro

In vitro activity: SC75741 shows immunosuppressive activity by inhibiting human PBMC proliferation with IC50 of 2.2 μM. SC75741 inhibits replication of influenza A and B viruses by inhibiting NF-κB-mediated signalling on a transcriptional level. Moreover, SC75741 shows a high barrier for development of resistant virus variants.


Kinase Assay: The NF-κB reporter gene assay is prepared with A549-NF-κB-SEAP cell line according to manufacturer’s instructions. In short, A549 cells stably transfected with pNF-κB-SEAP reporter gene plasmid are plated and allowed to attach overnight. The cells are subsequently incubated for 5 h with described compounds at 100, 30, 10, 3, 1, 0.3, 0.1, and 0 μM and then stimulated with 10 ng/ml TNF-α for 22 h. The supernatant of the cell is analyzed for SEAP activity using a chemiluminescent SEAP reporter gene assay.


Cell Assay: Cell viability assay is prepared using a CellTiter-BluTM Cell Viability Assay. For each concentration of the compound four replicates are measured.

In VivoSC75741 (15 mg/kg i.p.) reduces virus replication and cytokine expression in mice lungs after H5N1 influenza virus infection.
Animal modelC57BL/6 mice infected with H5N1 influenza virus
Formulation & DosageDissolved in 10% DMSO, 30% Cremophor EL and 60% PBS; 15 mg/kg; i.p. injection
References

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5858-62; Cell Microbiol. 2013 Jul;15(7):1198-211.