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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
37 Results for "
mGluR5 modulator
" in MedChemExpress (MCE) Product Catalog:
Products (37)
37 Results for "mGluR5 modulator" in MCE Product Catalog:
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1 Cited Publications
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CDPPB is a selective, orally active and brain-penetrant mGluR5 allosteric modulator. CDPPB increases AKT and ERK1/2 activation and augments the BDNF mRNA. CDPPB inhibits caspase-3 activation and mitochondrial dysfunction. CDPPB improves cognitive impairment, depression, and Huntington's disease .
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1 Cited Publications
Synonyms: RG7090; RO4917523
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Basimglurant (RG7090; RO4917523) is a selective, orally active, blood-brain barrier permeable negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5), with a Ki of 1.4 nM (against [ 3H]-ABP688 (HY-110141)) and 35.6 nM (against [ 3H]-MPEP (HY-14609A)). Basimglurant inhibits mGlu5-mediated signaling pathways and receptor constitutive activity, regulates dopamine levels in the nucleus accumbens, exerts anxiolytic, antidepressant-like, analgesic and arousal-promoting effects, and alters δ-wave power during non-rapid eye movement sleep. Basimglurant can be used in research on depression, fragile X syndrome, anxiety disorders, etc .
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1 Cited Publications
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ADX-47273 is a potent, selective and brain-penetrant mGluR5 positive allosteric modulator (PAM), with an EC50 of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities .
Synonyms: ADX48621
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Dipraglurant (ADX48621) is a potent, selective, orally active and brain penetrant mGluR5 negative allosteric modulator (NAM), with an IC50 of 21 nM. Dipraglurant can reduce Levodopa-induced dyskinesia (LID) in vivo . Dipraglurant 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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BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 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 .
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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 .
Cat. No.: HY-141832
CAS No.: 1261171-52-1
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mGluR5 modulator 1 is a mGluR5 positive allosteric modulator. mGluR5 modulator 1 can be used for the research of the schizophrenia and cognitive impairments .
Cat. No.: HY-103571
CAS No.: 327056-22-4
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VU0285683 is a selective mGluR5 positive allosteric modulator (PAM). VU0285683 has anxiolytic-like activity in rodent models for anxiety .
Cat. No.: HY-129636
CAS No.: 1611483-29-4
Synonyms: (E)-GABAB receptor antagonist 1
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CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
Cat. No.: HY-103574
CAS No.: 757949-98-7
Synonyms: ADX-10059 hydrochloride
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Raseglurant hydrochloride is a negative allosteric modulator of mGluR5. Raseglurant hydrochloride can be used in study migraine .
Cat. No.: HY-107508
CAS No.: 890764-36-0
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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) .
Cat. No.: HY-119282
CAS No.: 453566-30-8
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AZD6538 is a potent, selective and brain penetrant mGluR5 negative allosteric modulator. AZD6538 inhibits DHPG (HY-12598A)-stimulated intracellular Ca2+ release in HEK cells expressing rat or human mGluR5, with IC50 values of 3.2 and 13.4 nM for rat mGluR5 and human mGluR5, respectively. AZD6538 can be used for the research of neuropathic pain .
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BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.
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(S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923. (S,S)-BMS-984923 shows an EC50 >1μM for mGluR5 receptor . BMS-984923 is a potent mGluR5 silent allosteric modulator . (S,S)-BMS-984923 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cat. No.: HY-123874
CAS No.: 1375751-32-8
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BMS-952048 is a positive allosteric modulator of mGluR5 with an EC50 of 10 nM .
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MFZ 10-7 is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki of 0.67 nM for rat mGluR5 . MFZ 10-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cat. No.: HY-124393
CAS No.: 1253291-12-1
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GRN-529 is a negative allosteric modulator (NAM) for mGluR5. GRN-259 modulates sleep-wake activity, and exhibits anxiolytic efficacy in rats .
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DCB (3,3′-dichlorobenzaldazine) is an neutral allosteric modulator of themetabotropic 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) .
Cat. No.: HY-16951
CAS No.: 890764-63-3
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VU-1545 is a metabotropic glutamate receptor 5 positive allosteric modulator (mGluR5 PAM) with a Ki of 156 nM and an EC50 of 9.6 nM .
Cat. No.: HY-115483
CAS No.: 1946021-40-4
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VU0477573 is a brain-penetrant partial negative allosteric modulator of metabotropic glutamate receptor subtype 5 (mGluR5). VU0477573 exhibits neuroprotective and anxiolytic effects. VU0477573 can be used for the research of neurological disease, such as Parkinson disease .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
