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LB42708
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。
LB42708图片
CAS NO:226929-39-1
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
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)555.46
FormulaC30H27BrN4O2
CAS No.226929-39-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (180.0 mM)
Water: <1 mg/mL
Ethanol: 86 mg/mL warmed (154.8 mM)
Other info

Chemical Name: (1-((1-(4-bromobenzyl)-1H-imidazol-5-yl)methyl)-4-(naphthalen-1-yl)-1H-pyrrol-3-yl)(morpholino)methanone

InChi Key: GUUIRIMAQGOLHT-UHFFFAOYSA-N

InChi Code: InChI=1S/C30H27BrN4O2/c31-24-10-8-22(9-11-24)17-35-21-32-16-25(35)18-33-19-28(27-7-3-5-23-4-1-2-6-26(23)27)29(20-33)30(36)34-12-14-37-15-13-34/h1-11,16,19-21H,12-15,17-18H2

SMILES Code: O=C(C1=CN(CC2=CN=CN2CC3=CC=C(Br)C=C3)C=C1C4=C5C=CC=CC5=CC=C4)N6CCOCC6

SynonymsLB-42708; LB 42708; LB42708;
实验参考方法
In Vitro

In vitro activity: LB42708 potently inhibits the processing of the cellular farnesylated protein p21ras induced by LPS + IFN-γ in murine macrophage cell line RAW264.7 cells. LB42708 inhibits NF-κB activation and iNOS promoter activity through the inhibition of IKK activity. Moreover, LB42708 suppresses the expression of inducible NO synthase, cyclooxygenase-2, TNF-alpha, and IL-1beta and the production of NO and PGE(2) in immune-activated macrophages and osteoblasts. LB42708 irreversibly inhibits growth and induces apoptosis in H-ras and K-ras-transformed rat intestinal epithelial cells. LB42708 inhibits of VEGF-induced tumor angiogenesis by blocking Ras-dependent MAPK and PI3K/Akt pathways in tumor-associated endothelial cells.


Cell Assay: Cell growth is measured by MTT. Briefly, cells were seeded at 2 × 103 cells per well in 96-well culture plates in triplicate. After the addition of various concentrations of drugs, cells are incubated for 72 h. At the end of culture, the plates are washed twice with PBS, and cells are incubated with 200 μl of RPMI 1640 containing 10% FCS and 0.25 mg/ml of MTT at 37 °C for 3 h. The absorbance of each well is measured with Titer-Tech 96-well multiscanner at 570 nm. The viable cell number is proportional to the absorbance.

In VivoLB42708 (12.5 mg/kg i.p.) inhibits production of NO, PGE2, TNF-α, and IL-1β in LPS-injected mice, and also prevents the development of CIA. LB42708 (20 mg/kg/day i.p.) also inhibits tumor growth and angiogenesis in both Ras wild-type and mutated tumors.
Animal modelMice collagen-induced arthritis model.
Formulation & DosageDissolved in Saline; 10 mg/kg; i.p. injection
References

J Immunol. 2004 Jul 15;173(2):1276-83; Toxicol Appl Pharmacol. 2006 Sep 15;215(3):317-29; Mol Pharmacol. 2010 Jul;78(1):142-50.