mGluR Modulator

mGluR Modulators (44):

Cat. No.	Product Name	Effect	Purity

HY-15129

O-Phospho-L-serine	Modulator	≥98.0%
O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.

HY-14569

CDPPB	Modulator	99.32%
CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC₅₀ of 27 nM in Chinese hamster ovary cells expressing human mGluR5. CDPPB may provide an approach for development of antipsychotic agents.

HY-114403

VU6012962	Modulator	99.92%
VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu₇ NAM) with an IC₅₀ of 347 nM.

HY-122559

BMS-984923	Modulator	99.94%
BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (K_i = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling.

HY-107507

Ro 01-6128	Modulator	99.87%
Ro 01-6128 is a positive allosteric modulator of mGluR1.

HY-18162

JNJ-42153605	Modulator	99.24%
JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC₅₀ of 17 nM.

HY-16766

Decoglurant	Modulator	98.78%
Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant.

HY-110190

VU0422288	Modulator	99.88%
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.

HY-16636

ML337	Modulator	99.13%
ML337 is a selective and brain-penetrant negative allosteric modulator of mGlu3, with an IC₅₀ of 593 nM. ML337 possesses a favorable dystrophia myotonica protein kinase (DMPK) and ancillary pharmacology profile. ML337 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-124984

ML353	Modulator	98.07%
ML353 is a selective ligand of mGlu5 silent allosteric modulator (SAM) with an K_i value of 18.2 nM. ML353 improves the affinity of common allosteric sites, 20-fold higher than the previous mGlu5 SAM tool compound 5mpep. ML353 has potential applications in solving the intrinsic activity of SAM in vivo or as a agent blocker. ML353 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-119078

VU0080241	Modulator	99.69%
VU0080241 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 4 (mGluR4), with an EC₅₀ of 4.6 μM.

HY-13058B

(R)-ADX-47273	Modulator	99.00%
(R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC₅₀ of 168 nM for potentiation .

HY-100605

VU0483605	Modulator
VU0483605 is a potent and brain-penetrated mGlu₁ receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu₁ PAM activity at both human and rat, with EC₅₀ values of 390 and 356 nM, respectively.

HY-110122

AZ 12216052	Modulator	98.73%
AZ 12216052 is a mGluR8 positive allosteric modulator, and helps mGluR8 modulate signaling inputing to retinal ganglion cells. AZ 12216052 exhibits antianxiety effect.

HY-110152

LSN2463359	Modulator	99.16%
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.

HY-14612

CPPHA	Modulator	98.04%
CPPHA is potent and selective positive allosteric modulator (PAM) of the mGluR5 and mGluR1 (metabotropic glutamate receptor). CPPHA can potentiate responses of mGluR5 and mGluR1 to activation of these receptors. CPPHA is developed for the research of central nervous system disorders.

HY-122647

Valiglurax	Modulator	98.96%
Valiglurax (VU0652957) is a potent, orally active and selective mGlu4 positive allosteric modulator with EC₅₀ values of 64.6 nM and 197 nM for hmGlu₄/Gqi5 and rmGlu₄ GIRK, respectively. Valiglurax is a central nervous system (CNS) penetrant. Valiglurax can be used in research of Parkinson's disease.

HY-107509

LY2389575 hydrochloride	Modulator	99.93%
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.

HY-103572

MNI137	Modulator
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.

HY-16654

ML254	Modulator
ML254 is a potent mGlu₅ potentiator, with EC₅₀ and pEC₅₀ of 9.3 nM and 8.03 nM for rat mGlu₅, respectively. ML254 can be used for researching schizophrenia. ML254 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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