GluR

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S2860	IEM 1754 2HBr	82 mg/mL	82 mg/mL	<1 mg/mL
S4716	Evans Blue	100 mg/mL	100 mg/mL	<1 mg/mL
S4774	Xanthurenic Acid	-1 mg/mL	7 mg/mL	-1 mg/mL
S1614	Riluzole	<1 mg/mL	46 mg/mL	46 mg/mL
S1245	Latrepirdine 2HCl	<1 mg/mL	24 mg/mL	13 mg/mL
S2861	CTEP (RO4956371)	<1 mg/mL	78 mg/mL	10 mg/mL
S2809	MPEP	<1 mg/mL	39 mg/mL	39 mg/mL
S6001	LY404039	<1 mg/mL	1 mg/mL	<1 mg/mL
S2690	ADX-47273	<1 mg/mL	74 mg/mL	30 mg/mL
S2795	VU 0357121	<1 mg/mL	61 mg/mL	21 mg/mL
S8035	VU 0364439	<1 mg/mL	85 mg/mL	<1 mg/mL
S5137	O-Phospho-L-serine	37 mg/mL	<1 mg/mL	-1 mg/mL
S3070	Piracetam	72 mg/mL	72 mg/mL	<1 mg/mL
S2862	VU 0364770	<1 mg/mL	47 mg/mL	47 mg/mL
S2892	VU 0361737	<1 mg/mL	53 mg/mL	<1 mg/mL
S6618	JNJ-42153605	<1 mg/mL	4 mg/mL	10 mg/mL
S1893	D-glutamine	9 mg/mL	<1 mg/mL	<1 mg/mL

亜型選択性的な製品

GluR製品

All (18) GluR阻害剤(2) GluR活性剤(1) GluR拮抗剤(4) GluR作動薬(9) GluRモジュレータ(1) GluR化学物質(1) 新GluR製品

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S2860	IEM 1754 2HBr IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.
S4716	Evans Blue Evans Blue is a potent inhibitor of the uptake of L-glutamate into synaptic vesicles, also an AMPA/kainate receptor antagonist.
S4774	Xanthurenic Acid Xanthurenic acid, a molecule arising from tryptophan metabolism by transamination of 3-hydroxykynurenine, activates mGlu2/3 Metabotropic glutamate receptors (mGlu2 and mGlu3).
S1614	Riluzole Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.	Cancer Res, 2019, 79(8):1799-1809 Neuropharmacology, 2019, 150:175-183 Int J Mol Sci, 2016, 17(3):357	Spatial memory performance. a Latency to find the hidden platform. LPS-infused controls and Aged controls were impaired (p<0.001) compared to young aCSF-infused rats. The performance of Aged rats improved across days only when treated with Ril (†t=0.035). b Distance. LPS controls swam a greater distance than aCSF controls and Aged controls (p≤0.036). c Swim Speed. Aged rats swam the most slowly (p≤0.001). d Thigmotaxis. Aged controls spent the greatest percentage of time within the pool perimeter (p<0.001).
S1245	Latrepirdine 2HCl Latrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug.
S2861	CTEP (RO4956371) CTEP (RO4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors.	EBioMedicine, 2017, 20:120-126
S2809	MPEP MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.	Mol Neurobiol, 2017, 54(7):5286-5299	The expression of mGluR5 and Homer were detected by Western blot and analysed by ImageJ. a–c Cells were treated with various concentrations of pu-erh tea for 12 h. d–f Cells were treated with 62.5 μg/mL pu-erh tea for 3, 6, 9, 12 h. g-i Cells were treated with 62.5 μg/mL pu-erh, black, or green teas for 12 h. Data were analysed using GraphPad Prism software (*p < 0.001 vs. vehicle control, p < 0.01 vs. vehicle control, n = 3)
S6001	LY404039 LY404039 is a potent agonist of recombinant human mGlu2/mGlu3 receptors with K_i of 149 nM/92 nM, shows >100-fold selectivity over ionotropic glutamate receptors, glutamate transporters, and other receptors. Phase 3.	Synapse, 2015, 70:45–48 Neuropharm, 2012, 62(7):2184-91 PLoS One, 2011, 6(7):e22235	LY404039 avoids reduction in phospho-Akt levels caused by DETA/NO. Total cellular proteins were extracted as described in Materials and Methods from astrocytes exposed to 1 mM DETA/NO6100 mM LY40403961 mM db-cAMP for 30 min, and 50 mg of protein extracts were assayed for phospho-Akt by western-blot. (A) Specificity of the western-blot was analyzed by incubating astrocytes with the PI3K/Akt pathway inhibitor, 20 mM LY294002, which completely prevented LY404039-induced Akt phosphorylation, and LPS/IFNc was used as positive control of Akt activation. Membranes were stripped and incubated with anti-total Akt antibody, which was considered loading control. (B) Data were expressed as phospho-Akt/ total Akt ratio and related to control group. Bars represent the mean 6 SEM of 4 independent experiments. p,0.05, **p,0.001 versus control, ‘‘p,0.01 versus LY404039.
S6266^新	(S)-Glutamic acid (S)-Glutamic acid (L-Glutamic acid) is an endogenous, non-selective glutamate receptor agonist.
S2690	ADX-47273 ADX47273 is a potent and specific mGlu5 positive allosteric modulator(PAM) with EC50 of 0.17 μM, showing no activity at other mGlu subtypes.
S2795	VU 0357121 VU0357121 is a novel positive allosteric modulator (PAM) of mGlu5 with EC50 of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes.
S8035	VU 0364439 VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.	Antioxidants (Basel), 2018, 10.3390/antiox7110150
S5137	O-Phospho-L-serine O-Phospho-L-serine, a molecule that mimics the phosphatidylserine head group and partially blocks microglial phagocytosis of apoptotic cells, is a specific group III metabotropic glutamate receptor (mGluR) agonist.
S3070	Piracetam Piracetam is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
S2862	VU 0364770 VU 0364770 is a positive allosteric modulator(PAM) of mGlu4 with EC50 of 1.1 μM, exhibits insignificant activity at 68 other receptors, including other mGlu subtypes.
S2892	VU 0361737 VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors, can penetrate into CNS.
S6618^新	JNJ-42153605 JNJ-42153605 is a potent and selective mGlu2 receptor positive allosteric modulator with an EC50 of 17 nM.
S1893	D-glutamine D-glutamine is a D type stereoisomer of glutamine which is one of the 20 amino acids encoded by the standard genetic code.

製品コード

製品説明

文献中Selleckの製品使用例

お客様のフィードバック

S2860

IEM 1754 2HBr

IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.

S4716

Evans Blue

Evans Blue is a potent inhibitor of the uptake of L-glutamate into synaptic vesicles, also an AMPA/kainate receptor antagonist.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S4774	Xanthurenic Acid Xanthurenic acid, a molecule arising from tryptophan metabolism by transamination of 3-hydroxykynurenine, activates mGlu2/3 Metabotropic glutamate receptors (mGlu2 and mGlu3).

製品コード

製品説明

文献中Selleckの製品使用例

お客様のフィードバック

S4774

Xanthurenic Acid

Xanthurenic acid, a molecule arising from tryptophan metabolism by transamination of 3-hydroxykynurenine, activates mGlu2/3 Metabotropic glutamate receptors (mGlu2 and mGlu3).

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1614	Riluzole Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.	Cancer Res, 2019, 79(8):1799-1809 Neuropharmacology, 2019, 150:175-183 Int J Mol Sci, 2016, 17(3):357	Spatial memory performance. a Latency to find the hidden platform. LPS-infused controls and Aged controls were impaired (p<0.001) compared to young aCSF-infused rats. The performance of Aged rats improved across days only when treated with Ril (†t=0.035). b Distance. LPS controls swam a greater distance than aCSF controls and Aged controls (p≤0.036). c Swim Speed. Aged rats swam the most slowly (p≤0.001). d Thigmotaxis. Aged controls spent the greatest percentage of time within the pool perimeter (p<0.001).
S1245	Latrepirdine 2HCl Latrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug.
S2861	CTEP (RO4956371) CTEP (RO4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors.	EBioMedicine, 2017, 20:120-126
S2809	MPEP MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.	Mol Neurobiol, 2017, 54(7):5286-5299	The expression of mGluR5 and Homer were detected by Western blot and analysed by ImageJ. a–c Cells were treated with various concentrations of pu-erh tea for 12 h. d–f Cells were treated with 62.5 μg/mL pu-erh tea for 3, 6, 9, 12 h. g-i Cells were treated with 62.5 μg/mL pu-erh, black, or green teas for 12 h. Data were analysed using GraphPad Prism software (*p < 0.001 vs. vehicle control, p < 0.01 vs. vehicle control, n = 3)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S6001	LY404039 LY404039 is a potent agonist of recombinant human mGlu2/mGlu3 receptors with K_i of 149 nM/92 nM, shows >100-fold selectivity over ionotropic glutamate receptors, glutamate transporters, and other receptors. Phase 3.	Synapse, 2015, 70:45–48 Neuropharm, 2012, 62(7):2184-91 PLoS One, 2011, 6(7):e22235	LY404039 avoids reduction in phospho-Akt levels caused by DETA/NO. Total cellular proteins were extracted as described in Materials and Methods from astrocytes exposed to 1 mM DETA/NO6100 mM LY40403961 mM db-cAMP for 30 min, and 50 mg of protein extracts were assayed for phospho-Akt by western-blot. (A) Specificity of the western-blot was analyzed by incubating astrocytes with the PI3K/Akt pathway inhibitor, 20 mM LY294002, which completely prevented LY404039-induced Akt phosphorylation, and LPS/IFNc was used as positive control of Akt activation. Membranes were stripped and incubated with anti-total Akt antibody, which was considered loading control. (B) Data were expressed as phospho-Akt/ total Akt ratio and related to control group. Bars represent the mean 6 SEM of 4 independent experiments. p,0.05, **p,0.001 versus control, ‘‘p,0.01 versus LY404039.
S6266^新	(S)-Glutamic acid (S)-Glutamic acid (L-Glutamic acid) is an endogenous, non-selective glutamate receptor agonist.
S2690	ADX-47273 ADX47273 is a potent and specific mGlu5 positive allosteric modulator(PAM) with EC50 of 0.17 μM, showing no activity at other mGlu subtypes.
S2795	VU 0357121 VU0357121 is a novel positive allosteric modulator (PAM) of mGlu5 with EC50 of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes.
S8035	VU 0364439 VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.	Antioxidants (Basel), 2018, 10.3390/antiox7110150
S5137	O-Phospho-L-serine O-Phospho-L-serine, a molecule that mimics the phosphatidylserine head group and partially blocks microglial phagocytosis of apoptotic cells, is a specific group III metabotropic glutamate receptor (mGluR) agonist.
S3070	Piracetam Piracetam is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
S2862	VU 0364770 VU 0364770 is a positive allosteric modulator(PAM) of mGlu4 with EC50 of 1.1 μM, exhibits insignificant activity at 68 other receptors, including other mGlu subtypes.
S2892	VU 0361737 VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors, can penetrate into CNS.