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Isoforms Recommended: mGluR5
Results for "

mGlu5

" in MedChemExpress (MCE) Product Catalog:

41

Inhibitors & Agonists

2

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 pKi and a pIC50 of 9.3 and 9.2, respectively . HTL14242 can be used for the research of parkinson’s disease .
    HTL14242
  • HY-12510
    Methoxy-PEPy

    		mGluR Neurological Disease
    Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM.
    Methoxy-PEPy
  • HY-119765
    VU0366248

    		mGluR Neurological Disease
    VU0366248 is a mGlu5 negative allosteric modulator .
    VU0366248
  • 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 Ki of 195 nM, respectively. VU0360172 hydrochloride stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice .
    VU0360172 hydrochloride
  • 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 .
    LSN2814617
  • 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.
    JNJ-46778212
  • HY-119941
    VU0652835

    		mGluR Neurological Disease
    VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 of 81 nM .
    VU0652835
  • 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 .
    SIB-1757
  • 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.
    ML254
  • 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 Ki 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.
    VU0360172
  • 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 .
    Auglurant
  • HY-110141
    ABP688

    		mGluR Others
    ABP688 is a high affinity human mGluR5 antagonist with anKi of 1.7 nM. Radioisotope-labeled ABP688 can be used as a PET tracer for clinical imaging of the mGlu5 receptor .
    ABP688
  • HY-124984
    ML353

    		mGluR Neurological Disease
    ML353 is a selective ligand of mGlu5 silent allosteric modulator (SAM) with an Ki 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.
    ML353
  • 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) .
    VU0409106
  • 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.
    Mavoglurant racemate
  • HY-156331
    VU6004909

    		mGluR Neurological Disease
    VU6004909 is a mGlu5 receptor positive allosteric modulator (pEC50: 7.59). VU6004909 shows antipsychotic-like effects. VU6004909 can reverse MK801-induced cortical hyperactivity and cognitive deficits .
    VU6004909
  • 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 Kd 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.
    Basimglurant
  • 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 .
    3,3'-Difluorobenzaldazine
  • 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 Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons .
    VU0424465
  • 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 .
    VU0364289
  • 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 .
    JF-NP-26
  • 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.
    CTEP
  • 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.
    MPEP Hydrochloride
  • 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.
    MPEP
  • 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 .
    A-841720
  • HY-107508
    VU-29

    		mGluR Neurological Disease
    VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM and Ki=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) .
    VU-29
  • 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 Kd 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 .
    Fenobam
  • 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 Kd 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 .
    Fenobam hydrate
  • 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.
    ML289
  • 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.
    LSN2463359
  • 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 Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .
    VU0364770
  • 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 Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .
    VU0364770 hydrochloride
  • 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 .
    PDZ1 Domain inhibitor peptide
  • 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 .
    PDZ1 Domain inhibitor peptide TFA
  • HY-103559
    HexylHIBO

    		mGluR Neurological Disease
    HexylHIBO is a potent group I mGluR antagonist with Kbs of 140 and 110 μM at mGlu1a and mGlu5a receptors, respectively. HexylHIBO decreased sEPSC in rat .
    HexylHIBO
  • 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 .
    VU 0357121
  • 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 .
    (±)-LY367385
  • HY-107515
    LY367385
    1 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 .
    LY367385
  • HY-107515A
    LY367385 hydrochloride
    1 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 .
    LY367385 hydrochloride
  • HY-70059
    LY341495
    Maximum Cited Publications
    7 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].
    LY341495
  • 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].
    (Rac)-LY341495

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