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Chemical Structure| 1334294-76-6 Chemical Structure| 1334294-76-6

Structure of GSK682753A
CAS No.: 1334294-76-6

Chemical Structure| 1334294-76-6

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GSK682753A is an inverse agonist of EB virus-induced receptor 2 (EBI2) with an IC50 value of 53.6 nM. This compound has potential research applications in regulating immune responses and understanding viral infection mechanisms.

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Product Details of GSK682753A

CAS No. :1334294-76-6
Formula : C23H21Cl3N2O3
M.W : 479.78
SMILES Code : O=C1OC2(CCN(C(/C=C/C3=CC=C(Cl)C=C3)=O)CC2)CN1CC4=CC=C(Cl)C(Cl)=C4
MDL No. :MFCD30738004
InChI Key :RDDLWMWIRXGSJM-XBXARRHUSA-N
Pubchem ID :126843232

Safety of GSK682753A

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of GSK682753A

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
B cells 7 pM 5 hours GSK682753A inhibits 7α,25-OHC-induced B cell migration FEBS Open Bio. 2013 Feb 19;3:156-60
HEK293 cells 0.35 μM 60 minutes To determine the inhibitory activity of GSK682753A on EBI2, the results showed an IC50 of 0.35 μM. Structure. 2022 Jul 7;30(7):1016-1024. e5
HEK293 cell membranes 2.6 nM 30 minutes Inhibition of GTPγS binding to EBI2 J Biol Chem. 2011 Aug 19;286(33):29292-29302
HEK293 cells 10.9 nM 24 hours Inhibition of EBI2-mediated cAMP accumulation J Biol Chem. 2011 Aug 19;286(33):29292-29302
HEK293 cells 53.6 nM 24 hours Inhibition of constitutive activity of EBI2 J Biol Chem. 2011 Aug 19;286(33):29292-29302
CHO cells 0.2 μM 30 minutes GSK682753A inhibits 7α,25-OHC-induced G protein activation FEBS Open Bio. 2013 Feb 19;3:156-60
CHO-K1 EA-arrestin cells 40 nM 90 minutes GSK682753A inhibits 7α,25-OHC-induced β-arrestin recruitment FEBS Open Bio. 2013 Feb 19;3:156-60

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice WT and EBI2-overexpressing mice In vitro culture 1.3 μM 48 hours Inhibition of antibody-induced B cell proliferation J Biol Chem. 2011 Aug 19;286(33):29292-29302

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.42mL

2.08mL

1.04mL

20.84mL

4.17mL

2.08mL

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
 

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