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Chemical Structure| 1216744-19-2 Chemical Structure| 1216744-19-2

Structure of GSK4112
CAS No.: 1216744-19-2

Chemical Structure| 1216744-19-2

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GSK4112 is an agonist of Rev-erbα with EC50 of 0.4 μM and it can be designed to mimic the action of heme.

Synonyms: SR6452

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Product Details of GSK4112

CAS No. :1216744-19-2
Formula : C18H21ClN2O4S
M.W : 396.89
SMILES Code : ClC1=CC=C(CN(CC2=CC=C([N+]([O-])=O)S2)CC(OC(C)(C)C)=O)C=C1
Synonyms :
SR6452
MDL No. :MFCD12912412
InChI Key :WYSLOKHVFKLWOU-UHFFFAOYSA-N
Pubchem ID :50905018

Safety of GSK4112

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

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
J774.1 macrophages 50 μg/mL 24 hours PGE2 pre-treatment enhanced TsV-induced IL-1β expression, while EP2 and EP4 antagonists abrogated IL-1β production. PMC4766425
Bone marrow-derived macrophages (BMDMs) 50 μg/mL 24 hours TsV alone induces significant production of IL-1β, demonstrating that the venom itself delivers signals necessary for inflammasome activation in BMDMs. PMC4766425

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Tityus serrulatus venom (TsV)-induced inflammation model Intraperitoneal injection 120 μg/kg (sublethal dose) and 180 μg/kg(lethal dose) Single injection, monitored for 24 hours TsV activates the NLRP3 inflammasome, resulting in the production of IL-1β, LTB4, and PGE2, leading to lung edema, neutrophil recruitment, and animal mortality. IL-1Ra or caspase-1/11-deficient mice significantly reduced these effects. PMC4766425
Humanized mice HTLV-1 infection model Intraperitoneal injection 5 nmol per mouse Three times a week for six weeks To evaluate the effect of MK886 treatment on LTB4 plasma levels and viral load in HTLV-1-infected mice. Results showed that MK886 treatment significantly reduced LTB4 plasma levels and viral load. PMC5489682
Mice Zymosan-induced peritonitis Intraperitoneal injection 1 mg/kg Single dose, 30 minutes prior Evaluate the effect of MK886 on reducing LTB4 levels, showing more significant effects in female mice PMC5531400
Rats Chronic hypoxic pulmonary hypertension model Intraperitoneal injection 30 mg/kg Once daily for 28 days MK-886 inhibited the development of chronic hypoxic pulmonary hypertension, reducing pulmonary artery pressure and right ventricular hypertrophy PMC507334

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.60mL

2.52mL

1.26mL

25.20mL

5.04mL

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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