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Chemical Structure| 1426802-50-7 Chemical Structure| 1426802-50-7

Structure of GSK805
CAS No.: 1426802-50-7

Chemical Structure| 1426802-50-7

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GSK805 is an orally active RORγt inhibitor with central nervous system penetrance. GSK805 inhibits RORγ and Th17 cell differentiation, with pIC50 values of 8.4 and >8.2, respectively. It inhibits Th17 cell function and can be used in immunological research.

Synonyms: RORgamma-t-IN-1

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Product Details of GSK805

CAS No. :1426802-50-7
Formula : C23H18Cl2F3NO4S
M.W : 532.36
SMILES Code : O=C(NC1=CC(Cl)=C(C2=CC=CC=C2OC(F)(F)F)C(Cl)=C1)CC3=CC=C(S(=O)(CC)=O)C=C3
Synonyms :
RORgamma-t-IN-1
MDL No. :MFCD28902182
InChI Key :CEICQMBWAQAIQX-UHFFFAOYSA-N
Pubchem ID :71285927

Safety of GSK805

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

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HCC70 cells 5 μM 48 hours To evaluate the effect of GSK805 on cholesterol biosynthesis gene expression, results showed that GSK805 significantly down-regulated the expression of cholesterol biosynthesis genes. Pharmacol Res. 2022 Aug;182:106324
MDA-MB468 cells 2.5 μM 24 hours To evaluate the effect of GSK805 on cholesterol biosynthesis gene expression, results showed that GSK805 significantly down-regulated the expression of cholesterol biosynthesis genes. Pharmacol Res. 2022 Aug;182:106324

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Necrotizing enterocolitis (NEC) model Oral 10 μg/g Once daily for four days GSK805 ameliorates NEC severity by inhibiting Th17 responses Cell Biosci. 2022 Jan 4;12(1):3
Mice Mild subarachnoid hemorrhage model Oral gavage 30mg/kg Once daily for 14 days Inhibition of ROR γt decreased IL-17 production, thereby suppressing neutrophil entry into the CNS after subarachnoid hemorrhage Neurocrit Care. 2020 Aug;33(1):140-151

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.88mL

0.38mL

0.19mL

9.39mL

1.88mL

0.94mL

18.78mL

3.76mL

1.88mL

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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