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Results for "

mGlu5 negative allosteric modulator

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ERK (1) mGluR (15) Reference Standards (1)
By Research Areas:	Neurological Disease (15)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15446

Basimglurant 1 Publications Verification RG7090; RO4917523	mGluR	Neurological Disease
Basimglurant (RG7090; RO4917523) is a selective, orally active, blood-brain barrier permeable negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5), with a K_i 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 .

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-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-119765

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

HY-W565924

STX107	mGluR ERK	Neurological Disease
STX107 is a *metabotropic glutamate 5 (mGlu5) receptor* negative allosteric modulator (NAM) with a pK_i of 8.32. STX107 inhibits glutamate-induced Ca ²⁺ mobilization, IP1 accumulation, and ERK1/2 phosphorylation. STX107 also inhibits glutamate-induced mGlu5 internalization .

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-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-169345

VU6043653	mGluR	Neurological Disease
VU6043653 is a potent, selective and cross the blood-brain barrier metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC₅₀ value of 325 nM for h mGlu5 .

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-103562

DMeOB 3,3'-Dimethoxybenzaldazine	mGluR	Neurological Disease
DMeOB (3,3'-Dimethoxybenzaldazine) is a mGluR5 receptor negative allosteric modulator with an IC₅₀ of 3 μM. DMeOB displays reversible non-competitive inhibition of mGlu5-mediated responses .

HY-176122

VU6024945	mGluR	Neurological Disease
VU6024945 is an orally active negative allosteric modulator of metabotropic glutamate receptor subtype 5 (mGlu5 NAM) with an IC₅₀ value of 110 nM. VU6024945 can be used in the research of anti-anxiety, anti-depression and Parkinson's disease and other neurological diseases .

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-176420

VU6031545	mGluR	Neurological Disease
VU6031545 is a potent *mGlu 5* negative allosteric modulator with an IC₅₀ of 15 nM. VU6031545 has excellent brain penetrant and oral bioavailability in rats .

HY-114515

Basimglurant sulfate RG7090 sulfate; RO4917523 sulfate	mGluR	Neurological Disease
Basimglurant (RG7090; RO4917523) sulfate is a selective, orally active, blood-brain barrier permeable negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5), with a K_i of 1.4 nM (against [ ³H]-ABP688 (HY-110141)) and 35.6 nM (against [ ³H]-MPEP (HY-14609A)). Basimglurant sulfate 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 sulfate can be used in research on depression, fragile X syndrome, anxiety disorders, etc .

HY-15446R

Basimglurant (Standard) RG7090 (Standard); RO4917523 (Standard)	Reference Standards mGluR	Neurological Disease
Basimglurant (RG7090; RO4917523) (Standard) is the analytical standard of Basimglurant. This product is intended for research and analytical applications. Basimglurant is a selective, orally active, blood-brain barrier permeable negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5), with a K_i 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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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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mGlu5 negative allosteric modulator

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