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
S6906	Capric acid	34 mg/mL	34 mg/mL	34 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 (PK 26124)	<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
S9686	NBQX (FG9202)	<1 mg/mL	67 mg/mL	<1 mg/mL
S2645	SIB 1757	<1 mg/mL	22 mg/mL	9 mg/mL
S6001	pomaglumetad (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
S0165	Ampalex (CX-516)	48 mg/mL	48 mg/mL	48 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
S6803	1-BCP	6 mg/mL	47 mg/mL	47 mg/mL
S5222	Coluracetam	<1 mg/mL	68 mg/mL	23 mg/mL
S4721	L-Glutamic acid monosodium salt	33 mg/mL	<1 mg/mL	<1 mg/mL
S6804	CX546	<1 mg/mL	49 mg/mL	49 mg/mL
S6618	JNJ-42153605	<1 mg/mL	4 mg/mL	10 mg/mL
S2434	IDRA-21	<1 mg/mL	47 mg/mL	14 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 (27) GluR阻害剤(3) GluR活性剤(1) GluR拮抗剤(6) GluR作動薬(13) GluRモジュレータ(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
S2860	IEM 1754 2HBr IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.
S6906	Capric acid Capric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes to seizure control through direct AMPA receptor inhibition. Capric acid is also a modulating ligand for PPARs. Due to its specific melting range the product may be solid, liquid, a solidified melt or a supercooled melt.
S4716	Evans Blue Evans Blue (Direct Blue 53) is a potent inhibitor of the uptake of L-glutamate into synaptic vesicles, also an AMPA/kainate receptor antagonist.
S4774	Xanthurenic Acid Xanthurenic acid (xanthurenate, 8-Hydroxykynurenic acid, 4,8-Dihydroxyquinaldic acid), a molecule arising from tryptophan metabolism by transamination of 3-hydroxykynurenine, activates mGlu2/3 Metabotropic glutamate receptors (mGlu2 and mGlu3).
S1614	Riluzole (PK 26124) Riluzole (PK 26124, RP-54274) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.	Mol Genet Metab, 2021, S1096-7192(21)00826-X Cancer Res, 2019, 79(8):1799-1809 Neuropharmacology, 2019, 150:175-183	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 themost 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)
S9686	NBQX (FG9202) NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect.
S2645	SIB 1757 SIB 1757 is a highly selective, noncompetitive antagonist of metabotropic glutamate receptor type 5 (mGluR5) with IC50 of 0.4 μM at hmGluR5 compared with >30 µM at hmGluR1b, hmGluR2, hmGluR4, hmGluR6, hmGluR7 and hmGluR8.
S6001	pomaglumetad (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.	Schizophr Bull, 2021, sbab047 Neuropsychopharmacology, 2020, 10.1038/s41386-020-0764-2 Sci Rep, 2019, 9(1):14247	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.
S2690	ADX-47273 ADX47273 (BA 94673139) is a potent and specific mGlu5 positive allosteric modulator(PAM) with EC50 of 0.17 μM, showing no activity at other mGlu subtypes.	J Biol Chem, 2014, 289(41):28460-77
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 (Dexfosfoserine), 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 (UCB 6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
S6266	(S)-Glutamic acid (S)-Glutamic acid (L-Glutamic acid) is an endogenous, non-selective glutamate receptor agonist.	CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
S0165	Ampalex (CX-516) Ampalex (CX-516, Ampakine CX 516, BDP-12, SPD 420) is a positive allosteric modulator of AMPA receptor. Ampalex exhibits potential treatment for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).
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.
S6803	1-BCP 1-BCP (Piperonylic acid piperidide) is a memory-enhancing agent that enhances AMPA-induced currents.
S5222	Coluracetam Coluracetam (BCI-540, MKC-231) is a nootropic belonging to the racetam family of drugs with cognitive enhancing and neuroprotective effects.
S4721	L-Glutamic acid monosodium salt L-Glutamic acid monosodium salt (Monosodium glutamate, MSG) is the sodium salt of glutamic acid, found naturally in tomatoes, cheese and other foods.
S6804	CX546 CX546, a prototypical ampakine agent, is a selective positive AMPA receptor modulator.
S6618	JNJ-42153605 JNJ-42153605 is a potent and selective mGlu2 receptor positive allosteric modulator with an EC50 of 17 nM.
S2434	IDRA-21 IDRA-21 is a partial allosteric modulator of AMPA receptor desensitization. IDRA-21 is a potent cognition-enhancing drug virtually devoid of neurotoxic liability.
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.

S6906

Capric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes to seizure control through direct AMPA receptor inhibition. Capric acid is also a modulating ligand for PPARs. Due to its specific melting range the product may be solid, liquid, a solidified melt or a supercooled melt.

S4716

Evans Blue

Evans Blue (Direct Blue 53) 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 (xanthurenate, 8-Hydroxykynurenic acid, 4,8-Dihydroxyquinaldic 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 (xanthurenate, 8-Hydroxykynurenic acid, 4,8-Dihydroxyquinaldic 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 (PK 26124) Riluzole (PK 26124, RP-54274) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.	Mol Genet Metab, 2021, S1096-7192(21)00826-X Cancer Res, 2019, 79(8):1799-1809 Neuropharmacology, 2019, 150:175-183	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 themost 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)
S9686	NBQX (FG9202) NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect.
S2645	SIB 1757 SIB 1757 is a highly selective, noncompetitive antagonist of metabotropic glutamate receptor type 5 (mGluR5) with IC50 of 0.4 μM at hmGluR5 compared with >30 µM at hmGluR1b, hmGluR2, hmGluR4, hmGluR6, hmGluR7 and hmGluR8.

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	pomaglumetad (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.	Schizophr Bull, 2021, sbab047 Neuropsychopharmacology, 2020, 10.1038/s41386-020-0764-2 Sci Rep, 2019, 9(1):14247	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.
S2690	ADX-47273 ADX47273 (BA 94673139) is a potent and specific mGlu5 positive allosteric modulator(PAM) with EC50 of 0.17 μM, showing no activity at other mGlu subtypes.	J Biol Chem, 2014, 289(41):28460-77
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 (Dexfosfoserine), 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 (UCB 6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
S6266	(S)-Glutamic acid (S)-Glutamic acid (L-Glutamic acid) is an endogenous, non-selective glutamate receptor agonist.	CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
S0165	Ampalex (CX-516) Ampalex (CX-516, Ampakine CX 516, BDP-12, SPD 420) is a positive allosteric modulator of AMPA receptor. Ampalex exhibits potential treatment for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).
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.
S6803	1-BCP 1-BCP (Piperonylic acid piperidide) is a memory-enhancing agent that enhances AMPA-induced currents.
S5222	Coluracetam Coluracetam (BCI-540, MKC-231) is a nootropic belonging to the racetam family of drugs with cognitive enhancing and neuroprotective effects.
S4721	L-Glutamic acid monosodium salt L-Glutamic acid monosodium salt (Monosodium glutamate, MSG) is the sodium salt of glutamic acid, found naturally in tomatoes, cheese and other foods.

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
S6804	CX546 CX546, a prototypical ampakine agent, is a selective positive AMPA receptor modulator.
S6618	JNJ-42153605 JNJ-42153605 is a potent and selective mGlu2 receptor positive allosteric modulator with an EC50 of 17 nM.
S2434	IDRA-21 IDRA-21 is a partial allosteric modulator of AMPA receptor desensitization. IDRA-21 is a potent cognition-enhancing drug virtually devoid of neurotoxic liability.

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

S6804