RO5459072 |CAS:1252637-35-6 Probechem Biochemicals

Chemical Structure : RO5459072

RO5459072 (RG7625, Petesicatib)

Catalog No.: PC-60528Not For Human Use, Lab Use Only.

RO5459072 (Petesicatib, RG7625) is a potent, selective cathepsin S (Cat-S) inhibitor, inhibits human Cat-S with apparent IC50 of 0.1 nM and murine Cat-S of 0.3 nM.

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Biological Activity

RO5459072 (Petesicatib, RG7625) is a potent, selective cathepsin S (Cat-S) inhibitor, inhibits human Cat-S with apparent IC50 of 0.1 nM and murine Cat-S of 0.3 nM.

RO5459072 displats no sub-micro molar inhibition on any other of the tested cathepsins (Cat L, B, K, and F) with the exception of Cat V with apparent IC50 of 700 nM.

RO5459072 also shows ≤30% inhibition on a diversity panel consisting of nearly 100 receptor binding and enzymatic assays at 10 µM。

RO5459072 inhibits Cat-S in cells in the lip10 accumulation assays in human purified B-cells from whole blood and a potent induction of lip10 with EC50 of 15.8 nM.

RO5459072 attenuates systemic autoimmunity in MRL-(Fas)lpr mice, RO5459072 is more potent than MMF in suppressing kidney pathology.

RO5459072 effectively suppresses hypergammaglobulinemia and anti-dsDNA production, albuminuria, and lupus nephritis disease activity.

Physicochemical Properties

M.Wt	603.54
Formula	C25H23F6N5O4S
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(2S,4R)-N-(1-cyanocyclopropyl)-4-((4-(1-methyl-1H-pyrazol-4-yl)-2-(trifluoromethyl)phenyl)sulfonyl)-1-(1-(trifluoromethyl)cyclopropane-1-carbonyl)pyrrolidine-2-carboxamide

References

1. Tato M, et al. Sci Rep. 2017 Jun 5;7(1):2775.
2. Theron M, et al. Front Immunol. 2017 Jul 17;8:806.
3. Kratochwil NA, et al. Br J Clin Pharmacol. 2021 Sep;87(9):3550-3560.

RO5459072 (RG7625, Petesicatib)

Biological Activity

Physicochemical Properties

References

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