Rexaceract (GT-02287) | GCase PAM, GCase GCase activator

Chemical Structure : Rexaceract

Rexaceract (GT-02287, GT02287)

Catalog No.: PC-26353Not For Human Use, Lab Use Only.

Rexaceract (GT-02287) is a potent, selective positive allosteric modulator (PAM) of beta-glucocerebrosidase (β-glucocerebrosidase, β-glucosidase, or GCase) with KD of 17-24 uM at pH 7.4, enhances the function of lysosomal GCase.

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Biological Activity

Rexaceract (GT-02287) is a potent, selective positive allosteric modulator (PAM) of beta-glucocerebrosidase (β-glucocerebrosidase, β-glucosidase, or GCase) with KD of 17-24 uM at pH 7.4, enhances the function of lysosomal GCase.

Rexaceract (GT-02287) enhances GCase activity and facilitates its transport to lysosomes.

Rexaceract (GT-02287) increases GCase activity in fibroblast lysates by binding to a site distinct from the active site.

Rexaceract (GT-02287) (1.56-12.5 uM) effectively reduced GlcCer levels in patient fibroblasts.

Rexaceract (GT-02287) promotes lysosomal delivery of the ER-retained variant GCaseLeu444Pro, promotes CNX release and prevent proteasomal degradation of GCaseLeu444Pro.

Rexaceract (GT-02287) alleviates UPR in p.N370S/ins and p.L444P/p.L444P patient fibroblasts.

Physicochemical Properties

M.Wt	362.41
Formula	C21H19FN4O
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	4-amino-N-(2,3-dihydro-1H-inden-2-yl)-6-((2-fluorophenyl)amino)picolinamide

References

1. Patent WO2021105908 A1 2021-06-03. 2. Fregno I, et al. Int J Mol Sci. 2025 May 6;26(9):4392.

Rexaceract (GT-02287, GT02287)

Biological Activity

Physicochemical Properties

References

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