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Isoforms Recommended:	mGluR5

Results for "

mGlu5

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) iGluR (2) mGluR (43) PERK (1)
By Research Areas:	Cancer (2) Neurological Disease (45)

Inhibitors & Agonists

Peptides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-W062697

HTL14242 HTL0014242	mGluR	Neurological Disease
HTL14242 (HTL0014242) is an advanced and orally active mGlu5 NAM with a pK_i and a pIC₅₀ of 9.3 and 9.2, respectively . HTL14242 can be used for the research of parkinson’s disease .

HY-119765

VU0366248	mGluR	Neurological Disease
VU0366248 is a mGlu5 negative allosteric modulator .

HY-107504

VU0360172 hydrochloride	mGluR	Neurological Disease
VU0360172 hydrochloride is a potent and selective mGlu5 receptor positive allosteric modulator (PAM) with an EC₅₀ value of 16 nM and a K_i of 195 nM, respectively. VU0360172 hydrochloride stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice .

HY-12371

VU0431316	mGluR	Neurological Disease
VU0431316 is a potent and selective non-competitive antagonist of *mGlu5* with an IC₅₀ value of 24 nM .

HY-19623

VU0092273	mGluR	Neurological Disease
VU0092273 is a potent *mGlu5* positive allosteric modulator (PAM) that also binds to the MPEP site, with an EC₅₀ of 0.27 μM .

HY-123667

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

HY-118238

Remeglurant MRZ-8456	mGluR	Neurological Disease
Remeglurant (MRZ-8456) acts as a selective, orally active and allosteric antagonist of the *mGlu5* receptor, with an IC₅₀ of 13 nM. Remeglurant (MRZ-8456) can be used in the research for dyskinesia in Parkinson’s disease (PD) .

HY-118256

LSN2814617	mGluR	Neurological Disease
LSN2814617 is an orally active, potent, brain-penetrant, and selective *mGlu₅* (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC₅₀ values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). LSN2814617 shows wake-promoting effect. LSN2814617 can be used for schizophrenia research .

HY-117697

Lu AF11205	Others	Others
Lu AF11205 is a mGlu5 receptor positive allosteric modulator with activity modulating mGlu5 receptor activity. Optimization of Lu AF11205 resulted in a series of potent fused thiazole analogs whose structures and activities were influenced by substituents and which could affect receptor function in cell lines expressing mGlu5 receptors.

HY-120527

VU0463841	mGluR	Neurological Disease
VU0463841 is a potent, selective and brain-penetrant *mGlu5* negative allosteric modulator (NAM) with an IC₅₀ of 13 nM. VU0463841 is ineffective against mGlu1-4 and mGlu7-8. VU0463841 has the potential for the Cocaine addiction research .

HY-114589

VU0240382	Others	Others
VU0240382 is a metabotropic glutamate receptor subtype 5 modulator whose activity differs depending on whether it has allosteric agonist activity. VU0240382 with allosteric agonist activity can activate mGlu(5) receptors in cell lines, but has no agonist activity in natural systems and has similar efficacy to mGlu(5) modulators without allosteric agonist activity in animal models.

HY-12510

Methoxy-PEPy	mGluR	Neurological Disease
Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM.

HY-19559

JNJ-46778212 VU 0409551	mGluR	Neurological Disease
JNJ-46778212 (VU 0409551) is an *mGlu5* positive allosteric modulator with an EC₅₀ of 260 nM.

HY-119941

VU0652835	mGluR	Neurological Disease
VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC₅₀ of 81 nM .

HY-102095

SIB-1757	mGluR	Neurological Disease
SIB-1757 is a highly selective and noncompetitive antagonist of mGlu5 receptor with an IC₅₀ of 0.4 μM .

HY-16654

ML254	mGluR	Neurological Disease
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.

HY-120589

VU0360172	mGluR	Neurological Disease
VU0360172 is a potent and selective mGlu5 receptor positive allosteric modulator with an EC₅₀ value of 16 nM and a K_i of 195 nM, respectively. VU0360172 stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice . VU0360172 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-16617

Auglurant VU0424238	mGluR	Neurological Disease
Auglurant (VU0424238) is a novel and selective *mGlu5* antagonist with an IC₅₀ value of 11 nM (rat) and an IC₅₀ value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration .

HY-110141

ABP688	mGluR	Others
ABP688 is a high affinity human mGluR5 antagonist with anK_i of 1.7 nM. Radioisotope-labeled ABP688 can be used as a PET tracer for clinical imaging of the mGlu5 receptor .

HY-124984

ML353	mGluR	Neurological Disease
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-14866

Raseglurant ADX-10059	mGluR	Neurological Disease
Raseglurant (ADX-10059) is a mGlu5 receptor negative allosteric modulator. Raseglurant is effective against migraine. Raseglurant reduces the Haloperidol (HY-14538)-induced catalepsy in mice .

HY-110180

VU0409106	mGluR	Neurological Disease
VU0409106 is a potent and selective *mGlu₅* negative allosteric modulator (NAM) with an IC₅₀ of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB) .

HY-15257A

Mavoglurant racemate AFQ-056 racemate	mGluR	Neurological Disease
Mavoglurant racemate (AFQ-056 racemate) is the racemate of Mavoglurant. Mavoglurant is a novel, non-competitive mGlu5 receptor antagonist . Mavoglurant (racemate) 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-15446

Basimglurant 1 Publications Verification RG7090; CTEP Derivative	mGluR	Neurological Disease
Basimglurant (RG7090) is a potent, selective and orally available *mGlu5* negative allosteric modulator with a K_d of 1.1 nM . Basimglurant 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-14611

3,3'-Difluorobenzaldazine DFB	mGluR	Neurological Disease
3,3'-Difluorobenzaldazine (DFB) is a selective positive allosteric modulator of *mGluR5. 3,3'-Difluorobenzaldazine potentiates 3- to 6-fold action for mGlu5* agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC₅₀s in the 2 to 5 μM range .

HY-114978

VU0424465	mGluR PERK	Neurological Disease
VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for *mGlu₅* mediated iCa ²⁺ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a K_i value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons .

HY-120727

VU0364289	mGluR	Neurological Disease
VU0364289 is a highly selective *mGlu5* positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC₅₀ of 1.6 µM. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research .

HY-131019

JF-NP-26	mGluR	Neurological Disease
JF-NP-26, an inactive photocaged derivative of raseglurant, is the first caged mGlu5 receptor negative allosteric modulator. Uncaging of JF-NP-26 is elicited with light pulses in the visible spectrum (405 nm). JF-NP-26 induces light-dependent analgesia in models of inflammatory and neuropathic pain in freely behaving animals .

HY-15445

CTEP 2 Publications Verification RO 4956371; mGluR5 inhibitor	mGluR	Neurological Disease
CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC₅₀ of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors. CTEP 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-14609

MPEP Hydrochloride 3 Publications Verification	mGluR	Neurological Disease
MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC₅₀ of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride has anxiolytic-or antidepressant-like effects . MPEP (Hydrochloride) 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-14609A

MPEP 3 Publications Verification	mGluR	Neurological Disease
MPEP is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC₅₀ of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP has anxiolytic-or antidepressant-like effects . MPEP 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-103550

A-841720	mGluR	Neurological Disease
A-841720 is a potent, non-competitive and selective mGlu1 receptor antagonist with an IC₅₀ of 10 nM for human mGlu1 receptor. A-841720 displays 34-fold selectivity over mGlu5 (IC₅₀ of 342 nM), and no significant activity at a range of other neurotransmitter receptors, ion channels, and transporters. A-841720 has the potential for chronic pain research .

HY-107508

VU-29	mGluR	Neurological Disease
VU-29 is a positive allosteric modulator of *metabotropic glutamate 5 (mGlu5) receptor* (EC₅₀=9 nM and K_i=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC₅₀: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM) .

HY-101478

Fenobam	mGluR Apoptosis	Neurological Disease Cancer
Fenobam is a selective and orally active *mGluR5* antagonist (IC₅₀=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the K_d values of 54 nM and 31 nM on rat and human recombinant *mGlu5* receptors, respectively. Fenobam has anxiolytic activity, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. Fenobam can be used for research on neurological diseases, cancer and drug addiction .

HY-101478A

Fenobam hydrate	mGluR Apoptosis	Neurological Disease Cancer
Fenobam hydrate is a selective and orally active *mGluR5* antagonist (IC₅₀=84 nM) that can penetrate the blood-brain barrier. Fenobam hydrate shows the K_d values of 54 nM and 31 nM on rat and human recombinant *mGlu5* receptors, respectively. Fenobam hydrate has anxiolytic activity, inhibits self-administration behavior in rat, and induces apoptosis in cancer cells. Fenobam hydrate can be used for research on neurological diseases, cancer and drug addiction .

HY-19630

ML289 VU0463597	mGluR	Neurological Disease
ML289 (VU0463597) is a potent, selective, and CNS-penetrant *mGlu3* (IC₅₀=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5 . ML289 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-110152

LSN2463359	mGluR	Neurological Disease
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-100588

VU0364770	mGluR	Neurological Disease
VU0364770 is a selective and potent positive allosteric modulator (PAM) of *mGlu4. VU0346770 exhibits EC₅₀s of 290 nM and 1.1 μM at rat mGlu4* and *human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5* with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with K_i values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .

HY-100588A

VU0364770 hydrochloride	mGluR	Neurological Disease
VU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of *mGlu4. VU0346770 hydrochloride exhibits EC₅₀s of 290 nM and 1.1 μM at rat mGlu4* and *human mGlu4 receptor, respectively. VU0364770 hydrochloride exhibits antagonist activity at mGlu5* with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 hydrochloride also possesses activity at MAO with K_i values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .

HY-P1195

PDZ1 Domain inhibitor peptide	iGluR	Neurological Disease
PDZ1 Domain inhibitor peptide, a cyclic peptide, incorporates a β-Ala lactam side chain linker and targets the PDZ1 domains of the postsynaptic density protein 95 (PSD-95). PDZ1 Domain inhibitor peptide disrupts the GluR6/PSD-95 interaction and is very efficient in competing against the C terminus of GluR6 for the PDZ1 domain .

HY-P1195A

PDZ1 Domain inhibitor peptide TFA	iGluR	Neurological Disease
PDZ1 Domain inhibitor peptide TFA, a cyclic peptide, incorporates a β-Ala lactam side chain linker and targets the PDZ1 domains of the postsynaptic density protein 95 (PSD-95). PDZ1 Domain inhibitor peptide TFA disrupts the GluR6/PSD-95 interaction and is very efficient in competing against the C terminus of GluR6 for the PDZ1 domain .

HY-103559

HexylHIBO	mGluR	Neurological Disease
HexylHIBO is a potent group I mGluR antagonist with Kbs of 140 and 110 μM at mGlu_1a and mGlu_5a receptors, respectively. HexylHIBO decreased sEPSC in rat .

HY-15393

VU 0357121	mGluR	Neurological Disease
VU 0357121 is a positive and highly selective *mGlu5R* allosteric modulator (PAM) with an EC₅₀ of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes .

HY-135464

(±)-LY367385	mGluR	Neurological Disease
(±)-LY367385 is the racemate of LY367385. LY367385 is a highly potent and selective mGluR1a antagonist. LY367385 has an IC₅₀ of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with > 100 μM for mGlu5a .

HY-107515

LY367385 2 Publications Verification	mGluR	Neurological Disease
LY367385 is a highly selective and potent mGluR1a antagonist. LY367385 has an IC₅₀ of 8.8 μM for inhibiting of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects .

HY-107515A

LY367385 hydrochloride 2 Publications Verification	mGluR	Neurological Disease
LY367385 hydrochloride is a highly selective and potent mGluR1a antagonist. LY367385 hydrochloride has an IC₅₀ of 8.8 μM for inhibiting of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 hydrochloride has neuroprotective, anticonvulsant and antiepileptic effects .

HY-70059

LY341495 Maximum Cited Publications 9 Publications Verification	mGluR	Neurological Disease
LY341495 is a metabotropic glutamate receptor (mGluR) antagonist with IC₅₀s of 21 nM, 14 nM, 7.8 μM, 8.2 μM, 170 nM, 990 nM, 22 μM for mGlu2, mGlu3, mGlu1a, mGlu5a, mGlu8, mGlu7, and mGlu4 receptors, respectively ^[5].

HY-70059A

(Rac)-LY341495	Others	Neurological Disease
(Rac)-LY341495 is the isomer of LY341495 (HY-70059), and can be used as an experimental control. LY341495 is a metabotropic glutamate receptor (mGluR) antagonist with IC₅₀s of 21 nM, 14 nM, 7.8 μM, 8.2 μM, 170 nM, 990 nM, 22 μM for mGlu2, mGlu3, mGlu1a, mGlu5a, mGlu8, mGlu7, and mGlu4 receptors, respectively ^[5].

Cat. No.	Product Name	Target	Research Area

HY-P1195

PDZ1 Domain inhibitor peptide	iGluR	Neurological Disease
PDZ1 Domain inhibitor peptide, a cyclic peptide, incorporates a β-Ala lactam side chain linker and targets the PDZ1 domains of the postsynaptic density protein 95 (PSD-95). PDZ1 Domain inhibitor peptide disrupts the GluR6/PSD-95 interaction and is very efficient in competing against the C terminus of GluR6 for the PDZ1 domain .

HY-P1195A

PDZ1 Domain inhibitor peptide TFA	iGluR	Neurological Disease
PDZ1 Domain inhibitor peptide TFA, a cyclic peptide, incorporates a β-Ala lactam side chain linker and targets the PDZ1 domains of the postsynaptic density protein 95 (PSD-95). PDZ1 Domain inhibitor peptide TFA disrupts the GluR6/PSD-95 interaction and is very efficient in competing against the C terminus of GluR6 for the PDZ1 domain .

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