mGluR Inhibitor

mGluR Inhibitors (36):

Cat. No.	Product Name	Effect	Purity

HY-15446

Basimglurant	Inhibitor	99.56%
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-P1077A

CALP1 TFA	Inhibitor	98.15%
CALP1 TFA is a calmodulin (CaM) agonist (K_d of 88 µM) with binding to the CaM EF-hand/Ca²⁺-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC₅₀ of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity.

HY-120717

VU6001966	Inhibitor	99.89%
VU6001966 is a brain-penetrant and selective mGlu2 receptor inhibitor. VU6001966 blocks mGlu2 receptor activity, counteracts LY379268 (HY-103558)-mediated blood-brain barrier protection and inflammatory cytokine dampening in microglia under inflammatory conditions. VU6001966 enhances antidepressant effects when combined with Scopolamine (HY-N0296). VU6001966 can be used for the research of major depressive disorder.

HY-101845

FITM	Inhibitor	98.00%
FITM is a negative allosteric modulator of mGlu1 receptor with a K_i of 2.5 nM.

HY-W062697

HTL14242	Inhibitor	98.06%
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-122255

LY487379	Inhibitor	98.92%
LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [³⁵S]GTPγS binding with EC₅₀ values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research.

HY-120530

JNJ-46281222	Inhibitor	98.77%
JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator) with nanomolar affinity (K_d = 1.7 nM) and a high modulatory potency (pEC₅₀ = 7.71).

HY-19630

ML289	Inhibitor	98.29%
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-100405

FTIDC	Inhibitor	99.34%
FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC₅₀ of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1.

HY-169345

VU6043653	Inhibitor	99.97%
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-119282

AZD6538	Inhibitor
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.

HY-16617

Auglurant	Inhibitor	99.34%
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-110180

VU0409106	Inhibitor	99.76%
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-108011

Naftazone	Inhibitor	99.0%
Naftazone is a naphthoquinone derivative, it can be used for the research of venous insufciency. Naftazone protects blood vessels, increases venous tonicity and capillary resistance, and improves lymphatic and venous circulation.

HY-P1077

CALP1	Inhibitor	98.44%
CALP1 is a calmodulin (CaM) agonist (K_d of 88 µM) with binding to the CaM EF-hand/Ca²⁺-binding site. CALP1 blocks calcium influx and apoptosis (IC₅₀ of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity.

HY-100728

BMT-145027	Inhibitor
BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC₅₀ of 47 nM.

HY-132219

N,N-Dipropyldopamine hydrobromide	Inhibitor	98.22%
N. N-dipropyrldopamine is a potent inhibitor of glutamate release and has anticancer activity. The increase of glutamate secretion leads to cancer-induced bone pain (CIBP). N. N-dipropyrldopamine plays an analgesic role in CIBP.

HY-110254

AZD 9272	Inhibitor	99.87%
AZD 9272 is a selective, orally active and brain penetrant mGluR5 antagonist with IC₅₀s of 2.6 nM and 7.6 nM for rat and human receptors, respectively. AZD 9272 shows >3900-fold selectivity over other mGlu receptors^2].

HY-100404

DFMTI	Inhibitor	99.04%
DFMTI can completely block the rmGlu1 L757V glutamate response.

HY-119941

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

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