Basic information Safety Supplier Related

GSK547

Basic information Safety Supplier Related

GSK547 Basic information

Product Name:
GSK547
Synonyms:
  • GSK547
  • RIP1 inhibitor 547
  • RIP1I
  • CPD3508
  • (S)-6-(4-(5-(3,5-Difluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbonyl)piperidin-1-yl)pyrimidine-4-carbonitrile
  • RIP1 inhibitor GSK547
  • 4-Pyrimidinecarbonitrile, 6-[4-[[(5S)-5-(3,5-difluorophenyl)-4,5-dihydro-1H-pyrazol-1-yl]carbonyl]-1-piperidinyl]-
  • Inhibitor,RIP kinase,inhibit,GSK-547,GSK547,Receptor-interacting protein kinases,RIPK,GSK 547
CAS:
2226735-55-1
MF:
C20H18F2N6O
MW:
396.39
Mol File:
2226735-55-1.mol
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GSK547 Chemical Properties

Boiling point:
578.3±60.0 °C(Predicted)
Density 
1.43±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:65.0(Max Conc. mg/mL);163.98(Max Conc. mM)
form 
Solid
pka
1.93±0.28(Predicted)
color 
White to off-white
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GSK547 Usage And Synthesis

Biological Activity

GSK'547 is a highly selective and potent inhibitor of RIP1 (RIPK1) with a 400-fold increase in oral exposure compared to GSK'963 in mouse pharmacokinetic studies.

in vitro

In vitro, treatment with GSK'547 directed bone marrow-derived macrophages to develop an immunogenic phenotype, with up-regulation of MHC-II, TNFa and IFNg expression, and decreased CD206, IL- 10 and TGFb expression. In addition, it also up-regulated STAT1 signaling and decreased STAT3, STAT5 and STAT6 signaling in bone marrow-derived macrophages. Macrophages treated with GSK'547 had stronger ability to capture antigens.

in vivo

Mice were given GSK'547 through food, the concentration of GSK'547 in vivo was stable within 24 hours, which was higher than the IC50 value in L929 cells. GSK'547 maintained high concentrations in vivo during the 6-week administration. GSK'547 was well tolerated with no obvious pathological features. In mice with in situ pancreatic ductal adenocarcinoma, It reduced tumor burden and prolonged survival compared to control and Nec-1s-treated groups. GSK'547 prevents established tumors and liver metastases.

target

GSK547Supplier

Fujian boshi pharmaceutical technology co. LTD Gold
Tel
0595-22008920; 18120708884
Email
393612455@qq.com
ShangHai Caerulum Pharma Discovery Co., Ltd. Gold
Tel
18149758185 18149758185
Email
sales-cpd@caerulumpharma.com
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
Shanghai Balmxy Pharmaceutical Co., Ltd
Tel
021-24206007 13764915196
Email
sales@balmxy.com
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
TargetValue
RIP1
()