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TLR789 inhibitor 7f

Chemical Structure : TLR789 inhibitor 7f

CAS No.: 2180127-82-4

TLR789 inhibitor 7f (BMS-615)

Catalog No.: PC-72051Not For Human Use, Lab Use Only.

TLR789 inhibitor 7f is a potent, orally bioavailable antagonist of Toll-like Receptor 7/8/9 (TLR7/8/9) with IC50 of 10/17/700 nM in NF-kB reporter assays, does not inhibit TLR3/4.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

TLR789 inhibitor 7f (BMS-615) is a potent, orally bioavailable antagonist of Toll-like Receptor 7/8/9 (TLR7/8/9) with IC50 of 10/17/700 nM in NF-kB reporter assays, does not inhibit TLR3/4.
TLR789 inhibitor 7f inhibits IL-6 prodcution via TLR7/8/9 inhibitory response in human whole blood (mWB) assays with IC50 of 5.7/5.1/320 nM, respectively.
TLR789 inhibitor 7f effectively blocks cytokine production elicited by treatment with agonists of TLR7 (gardiquimod) or TLR9 (ODN1585) in mouse pharmacodynamic (PD) models, dose-dependently decreases agonist-induced IL-6 production with plasma EC50 of 2.4 nM (TLR7) or 25 nM (TLR9).

Physicochemical Properties

M.Wt 435.612
Formula C27H37N3O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Month
Shipping
Solubility

Chemical Name/SMILES

References

1. Christopher P Mussari, et al. ACS Med Chem Lett. 2020 Jul 29;11(9):1751-1758.

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