An activator of GCase
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GCase Activator 3

Item No. 45307

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[(2S)-2,3-dihydro-1,4-benzodioxin-2-yl]methyl]-N-methyl-2-(3-pyridinyl)-4-quinazolinamine
CAS Number
2270984-21-7
Synonyms
  • β-Glucocerebrosidase Activator 3
Molecular Formula
C23H20N4O2
Formula Weight
384.4
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
CN(C[C@H]1COC2=CC=CC=C2O1)C3=NC(C4=CN=CC=C4)=NC5=C3C=CC=C5
InChi Code
InChI=1S/C23H20N4O2/c1-27(14-17-15-28-20-10-4-5-11-21(20)29-17)23-18-8-2-3-9-19(18)25-22(26-23)16-7-6-12-24-13-16/h2-13,17H,14-15H2,1H3/t17-/m0/s1
InChi Key
JFOVNJQCUHRYOI-KRWDZBQOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $319

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    5 mg

    $718

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    10 mg

    $957

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    Product Description

    GCase activator 3 is an activator of β-glucocerebrosidase (GCase) with a half-maximal activation concentration (AC50) value of 1.49 µM.1 It increases GCase protein levels and activity and reduces mutant GCase protein misfolding in Gaucher disease patient-derived fibroblasts expressing the reduction-in-function GBA1N370S mutation and the loss-of-function GBA184GG mutation. GCase activator 3 (5 and 15 µM) also increases GCase protein levels and activity in midbrain dopaminergic neurons derived from Parkinson’s disease patient-derived induced pluripotent stem cells (iPSCs) and GBA1N370S-expressing iPSCs, both generated from skin fibroblasts.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zheng, J., Jeon, S., Jiang, W., et al. Correction to conversion of quinazoline modulators from inhibitors to activators of β-glucocerebrosidase. J. Med. Chem. 62(5), 2850 (2019).