IA-14069 Chemical Properties

Boiling point:

487.0±45.0 °C(Predicted)

Density 

1.379±0.06 g/cm3(Predicted)

storage temp. 

Store at -20℃

solubility 

Soluble in DMSO

InChI

InChI=1S/C20H15ClF2O4/c1-20(2,3)27-19(25)16-17(24)12-6-4-10(21)8-15(12)26-18(16)13-9-11(22)5-7-14(13)23/h4-9H,1-3H3

InChIKey

FWIGHXSYEQALSL-UHFFFAOYSA-N

SMILES

C1(C2=CC(F)=CC=C2F)OC2=CC(Cl)=CC=C2C(=O)C=1C(OC(C)(C)C)=O

IA-14069 Usage And Synthesis

Uses

IA-14069 is an orally active TNF-α inhibitor for studies related to rheumatoid arthritis.

Biological Activity

IA-14069 potently inhibits both TNF-α-induced cytotoxicity (IC50 < 0.7 μM), which directly binds to TNF-α and TNF-α-triggered signaling (p-IκBα and NF-κB p65) activities. The therapeutic and preventive anti-RA effects of IA-14069 were demonstrated in TNF-α-TG and CIA models. IA-14069 and MTX had synergistic effects in the CIA therapeutic model. According to pharmacokinetic analysis, IA-14069 showed significant bioavailability. In addition, no in vivo toxicity was observed even under treatment with an excessive amount of IA-14069[1].

References

[1] Sung-Dong Park. “THU0047 IA-14069, A NOVEL SMALL-MOLECULE INHIBITOR DIRECT-TARGETING TUMOR NECROSIS FACTOR-α, ATTENUATES COLLAGEN INDUCED ARTHRITIS.” Annals of the Rheumatic Diseases 78 1 (2019): 291–291.