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Chemical Structure| 243984-11-4 Chemical Structure| 243984-11-4

Structure of Resatorvid
CAS No.: 243984-11-4

Chemical Structure| 243984-11-4

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TAK-242, a small-molecule-specific inhibitor of Toll-like receptor (TLR)4 signaling, inhibits the production of lipopolysaccharide-induced inflammatory mediators by binding to the intracellular domain of TLR4.

Synonyms: TAK-242; CLI-095

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Product Details of Resatorvid

CAS No. :243984-11-4
Formula : C15H17ClFNO4S
M.W : 361.82
SMILES Code : O=C(C1=CCCC[C@H]1S(=O)(NC2=CC=C(F)C=C2Cl)=O)OCC
Synonyms :
TAK-242; CLI-095
MDL No. :MFCD11046362

Safety of Resatorvid

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Resatorvid

pyroptosis
TLR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
J774A.1 cells 1 µM 6 h Inhibition of TLR4 signaling pathway, reducing CB-7-induced inflammatory response PMC9030427
RAW264.7 macrophages 100 nM 12 h To investigate the inhibitory effect of Resatorvid on LPS-induced inflammatory response in macrophages PMC7575803
Healthy donor monocytes 5 µM 1 h Inhibited TLR4 signaling pathway, reducing the conversion of monocytes into MDSC-like cells PMC11409250
HSECs 5 μM 6 h To study the effect of Resatorvid on tube formation of HSECs, the results showed that Resatorvid had a limited effect on the tube formation ability of HSECs. PMC7722740
HUVECs 5 μM 6 h To study the effect of Resatorvid on tube formation of HUVECs, the results showed that Resatorvid had a limited effect on the tube formation ability of HUVECs. PMC7722740

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice SARS-CoV-2 and MHV infection models Intraperitoneal injection 50 mg Once daily, starting from day 2 post-infection Resatorvid significantly reduced the number of aberrant neutrophils in coronavirus-infected mice, inhibited viral replication, and improved the health status of the mice. PMC7762710
Mice CCl4-induced hepatic fibrosis model Gavage 5 mg/kg Every 2 days for 8 weeks To study the effect of Resatorvid on CCl4-induced hepatic fibrosis model, the results showed that Resatorvid had a limited protective effect on hepatic fibrosis. PMC7722740
Mice SARS-CoV-2 and MHV infection models Intraperitoneal injection 50 mg Once daily, starting from day 2 post-infection Resatorvid, by inhibiting the TLR4 signaling pathway, reduced the number of aberrant neutrophils in SARS-CoV-2 and MHV infected mice and inhibited viral replication. PMC7762710
Rats Transient global cerebral ischemia model Intraperitoneal injection 3 mg/kg Single dose, 30 minutes before ischemia To evaluate the neuroprotective effects of Resatorvid after transient global cerebral ischemia, results showed that Resatorvid reduced inflammation by inhibiting the TLR-4/NF-κB pathway, decreased the expression of TLR-4, NF-κB, and TNF-α in brain tissue, and reduced neuronal necrosis and apoptosis. PMC5713316
Mice LPC-induced demyelination model Intraperitoneal injection 3 mg/kg Daily for 10 days To study the role of TLR4 in pyroptosis, inhibiting the TLR4/MyD88/NF-κB pathway, alleviating pyroptosis induced by Tregs depletion PMC9938996

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.76mL

0.55mL

0.28mL

13.82mL

2.76mL

1.38mL

27.64mL

5.53mL

2.76mL

References

 

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