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Chemical Structure| 2226735-55-1 Chemical Structure| 2226735-55-1

Structure of GSK547
CAS No.: 2226735-55-1

Chemical Structure| 2226735-55-1

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GSK'547 is a highly selective and potent RIP1 inhibitor with improved oral bioavailability.

Synonyms: GSK'547

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Product Details of GSK547

CAS No. :2226735-55-1
Formula : C20H18F2N6O
M.W : 396.39
SMILES Code : N#CC1=NC=NC(N2CCC(C(N3N=CC[C@H]3C4=CC(F)=CC(F)=C4)=O)CC2)=C1
Synonyms :
GSK'547
MDL No. :MFCD32062767

Safety of GSK547

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of GSK547

pyroptosis

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
L929 cells 10 μM 24 hours Pretreatment with RIP1i inhibited TNFα and caspase inhibitor QVD-Oph-induced cell death. Cancer Cell. 2018 Nov 12;34(5):757-774. e7
bone marrow-derived macrophages (BMDM) 50 nM 18 hours RIP1i treatment directed BMDM towards an immunogenic M1-like phenotype, upregulating MHCII, TNFα, and IFNγ, while downregulating CD206, IL-10, and TGF-β. Cancer Cell. 2018 Nov 12;34(5):757-774. e7
Peritoneal macrophages 50 ng/ml 3 hours To evaluate the effect of GSK547 on oxLDL-induced foam cell formation, results showed GSK547 promoted foam cell formation. Front Cardiovasc Med. 2021 Oct 25;8:715337

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
ApoESA/SA mice Atherosclerosis model induced by hypercholesterolemia and hypertension Oral 10 mg/kg/day Once daily for 2 or 4 weeks To evaluate the effect of GSK547 on atherosclerotic plaque formation, results showed short-term treatment reduced plaque area, while long-term treatment exacerbated plaque formation. Front Cardiovasc Med. 2021 Oct 25;8:715337

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.61mL

2.52mL

1.26mL

25.23mL

5.05mL

2.52mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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