mGluR Modulator

Troriluzole hydrochloride is a third-generation peptide precursor of Riluzole (HY-B0211) and is an orally active glutamate modulator. Troriluzole hydrochloride can reduce synaptic glutamate levels and enhance the uptake of synaptic glutamate. Troriluzole hydrochloride shows potential for treating Alzheimer's disease and Generalized Anxiety Disorder (GAD) .

BMS-955829 is an orally active and selective mGluR5 positive allosteric modulator with an EC₅₀ of 2.6 nM. BMS-955829 has no intrinsic agonist activity and a low glutamate fold shift (2.4). BMS-955829 can effectively improve cognitive and executive function deficits in rodents. BMS-955829 can be used in the research of cognitive impairment diseases such as schizophrenia.

BMS-952048 is a positive allosteric modulator of mGluR5 with an EC₅₀ of 10 nM.

mGluR2 modulator 3 (compound 1) is a potent mGluR2 positive allosteric modulator with an EC₅₀ value of 0.87 μM. mGluR2 modulator 3 has activity in psychosis disease models such as methamphetamine-induced hyperactivity and mescaline-induced scratching in mice.

VU0366248 is a mGlu5 negative allosteric modulator.

VU0359516 is a compound that modulates mGluR4 activity, obtained through structure-activity relationship analysis of mGluR4 positive allosteric modulators, with improved potency and efficacy, as well as selectivity for mGluR4.

Raseglurant hydrochloride (Standard) is the analytical standard of Raseglurant hydrochloride (HY-103574). This product is intended for research and analytical applications. Raseglurant hydrochloride is a negative allosteric modulator of mGluR5. Raseglurant hydrochloride can be used in study migraine.

MNI137 (Standard) is the analytical standard of MNI137 (HY-103572). This product is intended for research and analytical applications. MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC₅₀s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization.

NCFP is a metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulator (PAM). NCFP can be used in the study of central nervous system diseases.

GRN-529 is a negative allosteric modulator (NAM) for mGluR5. GRN-259 modulates sleep-wake activity, and exhibits anxiolytic efficacy in rats.

RO4988546 is a negative allosteric modulator (NAM) that targets metabotropic glutamate receptors 2 and 3 (mGlu2, mGlu3). RO4988546 can reduce the binding of [³h]-LY354740 at the positive binding site, while affecting the receptor's G protein coupling and intracellular signaling. RO4988546 can be used in the development of antidepressants and cognitive enhancers.

LSN2463359 (Standard) is the analytical standard of LSN2463359 (HY-110152). This product is intended for research and analytical applications. LSN2463359 is positive allosteric modulator of metabotropic glutamate 5 (mGlu5). LSN2463359 attenuates aspects of the behavioral response to administration of the competitive NMDA receptor antagonist. LSN2463359 selectively attenuates reversal learning deficits observed in the neurodevelopmental MAM E17 model. LSN2463359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

LY2389575 hydrochloride (Standard) is the analytical standard of LY2389575 (hydrochloride) (HY-107509). This product is intended for research and analytical applications. LY2389575 hydrochloride is a selective and noncompetitive mGlu3 negative allosteric modulator (NAM), with an IC₅₀ value of 190 nM. LY2389575 hydrochloride induces an increase in Mrc1 levels. LY2389575 hydrochloride also independently amplifies Amyloid beta (Aβ) toxicity and can be used in study of Alzheimer's disease.

Ro 01-6128 (Standard) is the analytical standard of Ro 01-6128 (HY-107507). This product is intended for research and analytical applications. Ro 01-6128 is a positive allosteric modulator of mGluR1.

VU0400195 (ML182) is a oral active and allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4) with the EC₅₀ of 291 nM. VU0400195 can be used for study of antiparkinsonian animal model.

(E)-PHCCC is a positive allosteric modulator (PAM) for mGluR4, that enhances the activity of the receptor's endogenous ligand (glutamate), and exhibits activity in the calcium mobilization assay in CHO cells with an EC₅₀ of 3.2 μM.

DCB (Standard) is the analytical standard of DCB (HY-103561). This product is intended for research and analytical applications. DCB (3,3′-dichlorobenzaldazine) is an neutral allosteric modulator of the metabotropic glutamate receptor metabotropic glutamate receptor subtype 5 (mGluR5). DCB blocks the positive allosteric regulation of mGluRs (mGluR5) with the help of 3,3′-difluorobenzaldazine (DFB). DCB shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB).

VU0469650 (Standard) is the analytical standard of VU0469650 (HY-110191). This product is intended for research and analytical applications. VU0469650 is a potent, selective and brain-penetrant negative allosteric modulator of mGlu1 receptor, with an IC₅₀ of 99 nM.

VU0422288 (Standard) is the analytical standard of VU0422288 (HY-110190). This product is intended for research and analytical applications. VU0422288 (ML396) is a positive allosteric modulator of group III mGluRs. VU0422288 inhibits mGluRs with EC₅₀s of 125 nM, 146 nM, and 108 nM for mGluR4, mGluR7, and mGluR8, respectively in calcium mobilization assays. VU0422288 reverses deficits in contextual fear memory, social recognition, and apneas in Rett syndrome (RTT) model mice.