A positive allosteric modulator of mGluR4
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ADX-88178 (trifluoroacetate salt)

Item No. 43178

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-methyl-N-(4-methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine, trifluoroacetate salt
Molecular Formula
C12H12N6S • CF3COOH
Formula Weight
386.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
CC1=NC(NC2=NC(C3=CNN=C3)=C(C)S2)=NC=C1.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C12H12N6S.C2HF3O2/c1-7-3-4-13-11(16-7)18-12-17-10(8(2)19-12)9-5-14-15-6-9;3-2(4,5)1(6)7/h3-6H,1-2H3,(H,14,15)(H,13,16,17,18);(H,6,7)
InChi Key
XEUMDGWKSIMLGJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $72

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    10 mg

    $137

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    50 mg

    $394

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    100 mg

    $501

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    Product Description

    ADX-88178 is a positive allosteric modulator (PAM) of metabotropic glutamate receptor 4 (mGluR4).1 It enhances glutamate-induced intracellular calcium mobilization in HEK293 cells expressing human or rat mGluR4 (EC50s = 3.5 and 9.1 nM, respectively). ADX-88178 is selective for mGluR4 over mGluR1, mGluR2, mGluR3, mGluR5, mGluR7, and the GABAB receptor at 30 µM, mGluR6 at 10 µM, and mGluR8 (EC50 = 2.2 µM). It is also selective for mGluR4 over a panel of 71 receptors, transporters, enzymes, and ion channels at 10 µM. ADX-88178 (10 mg/kg) reverses catalepsy induced by haloperidol (Item No. 12014) in rats. It enhances L-DOPA-induced decreases in motor impairments in 6-OHDA-lesioned rats in a dose-dependent manner. However, it does not reverse L-DOPA- and benserazide-induced dyskinesia in 6-OHDA-lesioned rats.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Le Poul, E., Boléa, C., Girard, F., et al. A potent and selective metabotropic glutamate receptor 4 positive allosteric modulator improves movement in rodent models of Parkinson’s disease. J. Pharmacol. Exp. Ther. 343(1), 167-177 (2012).

    2. Finlay, C.J., Jackson, M.J., Fisher, R., et al. Metabotropic glutamate receptor 4 (mGlu4) positive allosteric modulators lack efficacy in rat and marmoset models of L-DOPA-induced dyskinesia. J. Parkinsons Dis. 14(2), 245-259 (2024).