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Results for "

mglur5 (human)

" in TargetMol Product Catalog
  • Inhibitors & Agonists
    12
    TargetMol | Inhibitors_Agonists
Fenobam
T1527557653-26-6
Fenobam shows inverse agonist activity which blocks the mGlu5 receptor basal activity(IC50: 84 nM). Fenobam has anxiolytic activity. Fenobam is a selective and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively).
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AZD 9272
T14389327056-26-8In house
AZD 9272 is a brain-permeable mGluR5 antagonist for the study of gastroesophageal reflux.
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6-8 weeks
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CDPPB
T22641781652-57-1
CDPPB is a modulator of mGluR5 positive allosteric(with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5).
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VU-29
VU 29
T23515890764-36-0
VU-29 is a positive allosteric mGlu5 receptor modulator with an EC50 of 9 nM and a Ki of 244 nM for rmGluR5. It is selective for mGluR5 relative to other mGluR subtypes [EC50: rmGluR1 rmGluR2=557 nM 1.5 μM; hmGluR4=154 nM].
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ABP688
ABP-688, ABP 688
T26520924298-51-1
ABP688 is a non-competitive and selective mGluR5 antagonist(Ki = 1.7 nM). ABP688 can be used as a PET tracer for clinical imaging.
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6-8 weeks
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Auglurant
VU0424238
T172411396337-04-4
Auglurant is a novel and selective mGlu5 antagonist (IC50: 11 nM (rat) and an IC50: 14 nM (human)). Auglurant has an acceptable CNS penetration.
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6-8 weeks
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VU6043653
T2017073032791-06-0
VU6043653 is an effective, selective, and blood-brain barrier-permeable negative allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGlu5), with an IC50 value of 325 nM against h mGlu5.
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10-14 weeks
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a 841720
T21848869802-58-4
A-841720 is a potent, selective, and non-competitive antagonist of the mGlu1 receptor, exhibiting an IC 50 value of 10 nM specifically for the human mGlu1 receptor. It demonstrates a 34-fold greater selectivity for mGlu1 over mGlu5 (IC 50 of 342 nM), with negligible activity across a spectrum of other neurotransmitter receptors, ion channels, and transporters. Additionally, A-841720 possesses analgesic potential within a certain dose range [1] [2].
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6-8 weeks
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azd6538
AZD-6538, AZD 6538
T26719453566-30-8
AZD6538 is an mGluR5 negative allosteric modulator used in the study of CNS-related diseases such as Alzheimer's disease.
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6-8 weeks
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lsn2814617
LSN-2814617, LSN 2814617
T278551313498-17-7
LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu 5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC 50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). In vivo EEG studies demonstrated that LSN2463359 has marked wake-promoting properties with minimal rebound hypersomnolence, and it can be used for schizophrenia research [1].
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6-8 weeks
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FTIDC
T3483873551-53-2
FTIDC is a highly potent and selective allosteric antagonist of mGluR1 receptors and shows very weak potency against human and rat mGluR5 receptors. The inhibition of FTIDC for mGluR1 receptors is shown to be in noncompetitive manner and displays IC50 val
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fenobam hydrate
T6895963540-28-3
Fenobam hydrate is a noncompetitive antagonist and inverse agonist of metabotropic glutamate receptor 5 (mGluR5). It inhibits intracellular calcium mobilization induced by the glutamate analog quisqualate and inhibits basal activity of mGluR5. Fenobam reduces stress-induced hyperthermia, exhibits anxiolytic-like activity, and may induce analgesia.
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1-2 weeks
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