An inhibitor of UDP-glucose ceramide glucosyltransferase
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TP-060

Item No. 41127

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-fluoro-2-(2,2,2-trifluoroethoxy)phenyl]-2,3-dihydro-2-[4-(1-hydroxy-1-methylethyl)phenyl]-1H-pyrrolo[3,4-c]pyridin-1-one
CAS Number
2601393-20-6
Synonyms
  • T-036
Molecular Formula
C24H20F4N2O3
Formula Weight
460.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C1C2=C(CN1C3=CC=C(C(C)(C)O)C=C3)C(C4=C(OCC(F)(F)F)C=C(F)C=C4)=NC=C2
InChi Code
InChI=1S/C24H20F4N2O3/c1-23(2,32)14-3-6-16(7-4-14)30-12-19-17(22(30)31)9-10-29-21(19)18-8-5-15(25)11-20(18)33-13-24(26,27)28/h3-11,32H,12-13H2,1-2H3
InChi Key
OAZAPIKYVGRNCO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $109

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    5 mg

    $191

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    Product Description

    TP-060 is an inhibitor of UDP-glucose ceramide glucosyltransferase (IC50 = 0.031 µM).1 It is selective for UDP-glucose ceramide glucosyltransferase over human ether-a-go-go (hERG) at 10 µM but also inhibits serotonin receptors (5-HT; IC50 = 0.31 µM). In vivo, TP-060 (30 mg/kg per day) decreases the cerebral cortex and serum levels of glucosylceramide and glucosylsphingosine in a Gba D409V transgenic mouse model of Gaucher disease.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tanaka, Y., Seto, M., Kakegawa, K., et al. Discovery of brain-penetrant glucosylceramide synthase inhibitors with a novel pharmacophore. J. Med. Chem. 65(5), 4270-4290 (2022).

    2. Fujii, T., Tanaka, Y., Oki, H., et al. A new brain-penetrant glucosylceramide synthase inhibitor as potential Therapeutics for Gaucher disease. J. Neurochem. 159(3), 543-553 (2021).