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Search Results for " kainate "

39

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
T8458	CNQX disodium	iGluR	Membrane transporter/Ion channel; Neuroscience
	CNQX disodium 是一种有效的、竞争性的 AMPA /海藻酸酯受体 (AMPA/kainate receptor) 拮抗剂，IC50分别为 0.3 μM 和 1.5 μM。它能够阻止大鼠恐惧增强的表达，是一种竞争性的非 NMDA 受体拮抗剂。
T7178	CNQX FG9065,6-氰基-7-硝基喹喔啉-2,3-二酮	GluR; iGluR	Membrane transporter/Ion channel; Neuroscience
	CNQX (FG9065) 是一种竞争性、非 NMDA 谷氨酸受体拮抗剂，对 AMPA 和红藻氨酸受体的IC50分别为 0.3 和 1.5 μM。
T21584	CP 465022	iGluR	Membrane transporter/Ion channel; Neuroscience
	CP 465022 hydrochloride 是强效的、选择性的AMPA 受体非竞争性拮抗剂，具有抗惊厥活性。CP 465022 hydrochloride 在大鼠皮层神经元中抑制Kainate 诱导的反应 (IC50= 25 nM)。
T16963	SYM 2081	iGluR	Membrane transporter/Ion channel; Neuroscience
	SYM 2081 是一种特异性红藻氨酸受体激动剂，对 [3H]-红藻氨酸结合的 IC50 值为 35 nM。 SYM 2081 使肌肉去极化并降低 EPSP 振幅。
T6134	IEM 1754 2HBr IEM 1754 dihydrobromide	GluR	Neuroscience
	IEM 1754 2HBr (IEM 1754 dihydrobromide) 是一种选择性 AMPA/红藻氨酸受体阻滞剂，作用于 GluR1 和 GluR3，IC50 为 6 μM。
T31208	Dasolampanel NGX-426,NGX 426,NGX426	GluR; iGluR	Membrane transporter/Ion channel; Neuroscience
	Dasolampanel (NGX-426) 是一种可口服的离子型谷氨酸受体 AMPA 和 Kainate 受体拮抗剂，可用于研究慢性疼痛疾病，包括神经性疼痛和偏头痛。
T20571	cis-PDA 哌啶-2,3-二羧酸,cis PDA	GluR; NMDAR; iGluR	Membrane transporter/Ion channel; Neuroscience
	cis-PDA (cis PDA) 是一种通用的离子型受体拮抗剂。 cis-PDA 通过阻断 NMDA、AMPA 和红藻氨酸介导的反应发挥作用。
T7304	DNQX 二硝基喹酮,FG 9041	GluR; iGluR	Membrane transporter/Ion channel; Neuroscience
	DNQX (FG 9041) 是喹恶啉衍生物，是一种选择性和强竞争性的非 NMDA 谷氨酸受体拮抗剂，对 AMPA、kainate 和 NMDA 受体的IC50分别为 0.5、2 和 40 μM。
T27949	LY382884 LY-382884,LY 382884	GluR	Neuroscience
	LY382884 是一种具有选择性和有效性的 GLU(K5)受体拮抗剂，具有抗焦虑活性。LY382884可阻断阻断苔藓纤维LTP的诱导。
T0313	Evans blue Direct Blue 53,C.I. 23860,伊文思蓝	GluR	Neuroscience
	Evans blue (C.I. 23860) 是一种突触泡谷氨酸吸收的有效抑制剂，同时也是一种AMPA/kainate 受体拮抗剂。
T8459	DNQX disodium salt DNQX Disodium	NMDAR; iGluR	Membrane transporter/Ion channel; Neuroscience
	DNQX disodium salt 是一种选择性、强竞争性的非 NMDA 谷氨酸受体 (non-NMDA glutamate receptor) 拮抗剂 (对 AMPA、kainate 和 NMDA 受体的 IC50分别为 0.5、2 和 40 μM)，是一种喹恶啉衍生物。
T0675	Topiramate RWJ 17021,McN 4853,托吡酯	Potassium Channel; Calcium Channel; GABA Receptor; Sodium Channel; GluR; Carbonic Anhydrase; iGluR	Membrane transporter/Ion channel; Metabolism; Neuroscience
	Topiramate (RWJ 17021) 是一种GluR5受体拮抗剂，可通过增强GABAergic 活性，抑制kainate/AMPA 受体，抑制钠和钙通道的电压敏感，增加钾电导并抑制碳酸酐酶来产生抗癫痫作用，用于治疗部分性和全身性癫痫发作。
T23489	UBP301 UBP 301	Others	Others
	kainate receptor antagonist
T23215	(R)-3,4-DCPG	Others	Others
	AMPA receptor antagonist with weak activity at NMDA receptors and little activity at kainate receptors
T22546	UBP316 ACET	Others	Others
	GluR5-containing kainate receptor antagonist
T11522	GYKI 52466 dihydrochloride	Others	Others
	GYKI 52466 dihydrochloride is orally active and non-competitive kainate- and AMPA-activated currents antagonist (IC50s: 7.5 μM and 11 μM). It is inactive against NMDA or γ-aminobutyric acid responses. It is a muscle relaxant and anticonvulsant agent and h
T23488	UBP 296	Others	Others
	GluR5-subunit containing kainate receptor antagonist
T23295	(S)-(-)-5-Iodowillardiine	Others	Others
	hGluR5 kainate receptor agonist
T23088	NS 3763	Others	Others
	kainate receptor antagonist
T23216	(R)-3C4HPG	Others	Others
	NMDA and AMPA/kainate receptor antagonist
T17193	UBP 302	Others	Others
	UBP 302 is an effective and selective GLUK5-subunit-containing kainate receptor antagonist (apparent Kd=402 nM) and displays very little affinity on GluK2 kainate receptors.
T23487	UBP-282	Others	Others
	AMPA and kainate receptor antagonist
T27947	LY339434 LY 339434,LY-339434
	LY339434 is a potent and selective agonist of the kainate receptor GluK1, GluR5.
T23490	UBP310 UBP 310	Others; iGluR	Membrane transporter/Ion channel; Neuroscience; Others
	UBP310 (UBP 310) 是选择性GluR5拮抗剂，Kd 值为 130 nM。
T13405	Fanapanel hydrate MPQX hydrate,ZK200775 (hydrate)	Others	Others
	Fanapanel hydrate is a highly selective antagonist of AMPA/kainate with little activity against NMDA(Ki of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively).
T13405L	Fanapanel MPQX,ZK200775	Others	Others
	Fanapanel is a highly selective AMPA/kainate antagonist with little activity against NMDA. It also has Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.
T38779	NS-102
	NS-102 is a powerful and selective antagonist of the kainate receptor (GluK2), as well as a potent antagonist of the GluR6/7 receptor.
T26037	RAD-140-Q RAD 140,RAD-140Q,RAD-140 Q,RAD140,RAD-140
	RAD-140-Q (RAD-140) is a selective androgen receptor modulator that inhibits the Growth of Androgen/Estrogen Receptor-Positive Breast Cancer Models with a Distinct Mechanism of Action. RAD-140-Q is neuroprotective in cultured neurons and kainate-lesioned
T38192	Unifiram	Others	Others
	Unifiram 是一种认知增强剂。 Unifiram 诱导大鼠海马 CA1 区场兴奋性突触后电位 (fEPSP) 幅度的持久增加 (EC50= 27 nM) 并增加大鼠大脑皮层中乙酰胆碱 (ACh) 的释放。
T21449	GYKI-52466 GYKI 52,466,GYKI-5,2466,GYKI52,466
	GYKI-52466 is a selective non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >50 μM for AMPA-, kainate- and NMDA-induced responses, respectively) used as a Skeletal muscle relaxant, orally active anticonvulsant, neuroprotective and
T8435	YM90K YM90K hydrochloride,6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-,1,4-二氢-6-(1H-咪唑-1-基)-7-硝基-2,3-喹喔啉二酮单盐酸盐	GluR; iGluR	Membrane transporter/Ion channel; Neuroscience
	YM90K (6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-) hydrochloride 是一种选择性的、有效的AMPA 受体拮抗剂，Ki=84 nM。YM90K 抑制海藻酸酯 (Ki 为 2.2 μM) 和 NMDA (Ki 为 37 μM) 受体的效力较低，并具有神经保护活性。
T61145	Topiramate lithium
	Topiramate lithium (McN 4853) is a wide-ranging antiepileptic compound with GluR5 receptor antagonistic properties. Its mechanism of action involves enhancing GABAergic activity, inhibiting kainate/AMPA receptors, voltage-sensitive sodium and calcium channels, and increasing potassium conductance. Additionally, this compound inhibits carbonic anhydrase. [1][2][3]
T21875	CP-465022 (maleate)
	CP-465022 Maleate is a potent, selective, noncompetitive AMPA receptor antagonist with anticonvulsant activity. It effectively counters the Kainate-induced response in rat cortical neurons, exhibiting an IC 50 of 25 nM. As such, CP-465022 Maleate presents a valuable instrument for studying the involvement of AMPA receptors in various physiological and pathophysiological processes [1] [2].
T39565	L-Glutamic acid-15N
	L-Glutamic acid-15N is the 15N-labeled version of L-Glutamic acid, an excitatory neurotransmitter and an agonist at metabotropic, kainate, NMDA, and AMPA glutamate receptor subtypes. It directly activates the release of dopamine (DA) from dopaminergic terminals.
T39207	L-803087 TFA
	L-803087 TFA is a highly potent and selective agonist of the somatostatin sst4 receptor, exhibiting a Ki value of 0.7 nM. It displays a remarkable selectivity, being over 280-fold more preferential for the sst4 receptor compared to other somatostatin receptors. Furthermore, L-803087 TFA promotes AMPA-mediated synaptic responses in hippocampal preparations and enhances kainate-induced seizures in mice.
T69202	NBQX sodium
	NBQX, also known as FG9202, is an AMPA receptor antagonist. NBQX blocks AMPA receptors in micromolar concentrations (~10–20 µM) and also blocks kainate receptors. In experiments, it is used to counter glutamate excitotoxicity. NBQX was found to have anticonvulsant activity in rodent seizure models. As the disodium salt, NBQX is soluble in water at high concentrations (at least up to 100 mM).
T37671	CAY10608 CAY10608
	N-Methyl-D-aspartate (NMDA) receptors are Ca2+ permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. CAY10608 is a propanolamine that potently, selectively, and non-competitively antagonizes the NR2B subunit of NMDA receptors (IC50 = 50 nM). It does not inhibit NR1, NR2A, NR2C, and NR2D subunits and has no significant effects on α-amino-3-hydroxy-5-methyl-4-isoxazolepropioinic acid (AMPA) or kainate receptors. CAY...
T70063	GYKI 52466 HCl
	GYKI 52466 is an allosteric AMPA receptor antagonist. It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of general...
T69806	EGIS-8332
	EGIS-8332 is a potent and selective non-competitive AMPA receptor antagonist. EGIS-8332 inhibits AMPA/kainate ion channels and cell death. EGIS-8332 inhibited AMPA currents in rat cerebellar Purkinje cells and inhibited the AMPA- and quisqualate-induced excitotoxicity in primary cultures of telencephalon neurons (IC(50)=5.1-9.0 microM), in vitro. EGIS-8332 seems suitable for further development for the treatment of epilepsy, ischaemia and stroke based on its efficacy in a variety of experimenta...

化合物

Cat.No: T8458

Target: iGluR

Cat.No: T7178

Synonym: FG9065,6-氰基-7-硝基喹喔啉-2,3-二酮

Target: GluR, iGluR

Cat.No: T21584

Target: iGluR

Cat.No: T16963

Target: iGluR

Cat.No: T6134

Synonym: IEM 1754 dihydrobromide

Target: GluR

Cat.No: T31208

Synonym: NGX-426,NGX 426,NGX426

Target: GluR, iGluR

Cat.No: T20571

Synonym: 哌啶-2,3-二羧酸,cis PDA

Target: GluR, NMDAR, iGluR

Cat.No: T7304

Synonym: 二硝基喹酮,FG 9041

Target: GluR, iGluR

Cat.No: T27949

Synonym: LY-382884,LY 382884

Target: GluR

Cat.No: T0313

Synonym: Direct Blue 53,C.I. 23860,伊文思蓝

Target: GluR

DNQX disodium salt

Cat.No: T8459

Synonym: DNQX Disodium

Target: NMDAR, iGluR

Cat.No: T0675

Synonym: RWJ 17021,McN 4853,托吡酯

Target: Potassium Channel, Calcium Channel, GABA Receptor, Sodium Channel, GluR, Carbonic Anhydrase, iGluR

Cat.No: T23489

Synonym: UBP 301

Target: Others

Cat.No: T23215

Target: Others

Cat.No: T22546

Synonym: ACET

Target: Others

GYKI 52466 dihydrochloride

Cat.No: T11522

Target: Others

Cat.No: T23488

Target: Others

(S)-(-)-5-Iodowillardiine

Cat.No: T23295

Target: Others

Cat.No: T23088

Target: Others

Cat.No: T23216

Target: Others

Cat.No: T17193

Target: Others

Cat.No: T23487

Target: Others

Cat.No: T27947

Synonym: LY 339434,LY-339434

Cat.No: T23490

Synonym: UBP 310

Target: Others, iGluR

Fanapanel hydrate

Cat.No: T13405

Synonym: MPQX hydrate,ZK200775 (hydrate)

Target: Others

Cat.No: T13405L

Synonym: MPQX,ZK200775

Target: Others

Cat.No: T38779

Cat.No: T26037

Synonym: RAD 140,RAD-140Q,RAD-140 Q,RAD140,RAD-140

Cat.No: T38192

Target: Others

Cat.No: T21449

Synonym: GYKI 52,466,GYKI-5,2466,GYKI52,466

Cat.No: T8435

Synonym: YM90K hydrochloride,6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-,1,4-二氢-6-(1H-咪唑-1-基)-7-硝基-2,3-喹喔啉二酮单盐酸盐

Target: GluR, iGluR

Topiramate lithium

Cat.No: T61145

CP-465022 (maleate)

Cat.No: T21875

L-Glutamic acid-15N

Cat.No: T39565

Cat.No: T39207

Cat.No: T69202

Cat.No: T37671

Synonym: CAY10608

Cat.No: T70063

Cat.No: T69806

Cat. No.	Product Name	Target	Signaling Pathways
T13456	(S)-Willardiine (-)-Willardiine,L-willardiine,Willardiine	iGluR	Membrane transporter/Ion channel; Neuroscience
	(S)-Willardiine (L-willardiine) 存在于金合欢和含羞草的种子中。 (S)-Willardiine 是一种 AMPA/红藻氨酸受体激动剂 (EC50 = 44.8 μM)。

天然产物

(S)-Willardiine

Cat.No: T13456

Synonym: (-)-Willardiine,L-willardiine,Willardiine

Target: iGluR

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