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Search Results for " desensitization "

12

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T4573	Cyclothiazide	GluR	Neuroscience
	Cyclothiazide 是AMPA 受体的正变构调节剂，可快速抑制 AMPA 受体脱敏，并缓慢增强 AMPA 电流。它可以阻断天然和异源表达的AMPA 受体脱敏。
T14989	CMPD101	ROCK; GRK; PKC	Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; GPCR/G Protein; Stem Cells
	CMPD101 是膜透性的 GRK2/3高选择性小分子抑制剂，IC50分别为 18 nM 和 5.4 nM。它针对 GRK1、GRK5 ROCK-2 和 PKCα 的选择性较小，IC50值分别为 3.1 μM，2.3 μM，1.4 μM 和 8.1 μM，可研究心衰疾病。
T4236	AR-M 1000390 hydrochloride ARM390 Hydrochloride,ARM-390 HCl	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	AR-M 1000390 hydrochloride (ARM-390 HCl) 是选择性 δ 阿片受体激动剂，EC50为 7.2±0.9 nM。
T27806	Lecozotan HCl SRA-333,SRA333,SRA 333,Lecozotan hydrochloride	5-HT Receptor	GPCR/G Protein; Neuroscience
	Lecozotan HCl (SRA-333) 是一种强效且具有选择性的 5-HT 拮抗剂。Lecozotan HCl能明显增强氯化钾刺激海马齿状回谷氨酸和乙酰胆碱的释放并具有增强认知能力的特性。在表明 5-HT(1A) 受体功能的行为模型中，长期服用Lecozotan HCl不会诱发 5-HT(1A) 受体耐受或脱敏。
T33289	Meproadifen
	Meproadifen enhances activation and desensitization of the acetylcholine receptor-ionic channel complex (AChR).
T36634	ZQ 16
	Selective medium-chain free fatty acid receptor GPR84 agonist (EC50 = 139 nM). Exhibits no response at GPR40, GPR41, GPR119 or GPR120 at 100 μM. Activates calcium mobilization, inhibits cAMP accumulation, and induces ERK1/2 phosphorylation, receptor desensitization and internalization in vitro. Liu et al (2016) Design and synthesis of 2-alkylpyrimidine-4,6-diol and 6-alkylpyridine-2,4-diol as potent GPR84 agonists. ACS Med.Chem.Lett. 7 579 PMID:27326330 \|Zhang et al (2016) Discovery and characte...
T71398	RO5126946
	RO5126946 is a Novel α7 nicotinic acetylcholine receptor-positive allosteric modulator. RO5126946 allosterically modulates α7nAChR activity. RO5126946 increased acetylcholine-evoked peak current and delayed current decay but did not affect the recovery of α7nAChRs from desensitization. In addition, RO5126946's effects were absent when nicotine-evoked currents were completely blocked by coapplication of the α7nAChR-selective antagonist methyl-lycaconitine.
T76399	PKI(5-22)amide
	PKI(5-22)amide 是环 AMP 依赖性蛋白激酶 (PKA) 抑制剂的活性片段。PKI(5-22)amide 抑制PKA 激活，但不能减弱 CRF1 受体的同源脱敏作用。
T38392	JAMI1001A
	JAMI1001A is a positive allosteric modulator of the AMPA receptor, effectively modulating the deactivation and desensitization of both flip and flop receptor isoforms.
T80503	Proadrenomedullin (N-20) (bovine, porcine) ProADM N20(bovine, porcine),PAMP-20(bovine, porcine)
	Proadrenomedullin (N-20) (bovine, porcine) 是一种来源于嗜铬细胞的、具有降压及抑制 catecholamine release 的非竞争性肽类。该化合物能显著抑制 PC12 嗜铬细胞瘤细胞的 catecholamine 分泌，显示出 350 nM 的 IC50 值。此外，Proadrenomedullin (N-20) (bovine, porcine) 作为 EC50 约为 270 nM 的阻断剂，能够有效抵抗烟碱能激动剂引起的 catecholamine release 脱敏现象和烟碱相关的信号通道 (22Na+摄取)。
T72744	(R)-PF-06256142
	(R)-PF-06256142 是 PF-06256142 的 R 型活性较差的对映异构体。PF-06256142 是一种有效的、选择性的正构D1 receptor 激动剂，可以减少相对于多巴胺和其他含儿茶酚激动剂的受体脱敏。
TP2058	Catestatin
	Non-competitive nicotinic cholinergic antagonist; selectively inhibits nicotinic-stimulated catecholamine secretion from chromaffin cells and noradrenergic neurons (IC50 ~ 200 nM). Blocks nicotinic-induced cationic signaling (IC50 ~ 200 - 250 nM) and inhi

化合物

Cat.No: T4573

Target: GluR

Cat.No: T14989

Target: ROCK, GRK, PKC

AR-M 1000390 hydrochloride

Cat.No: T4236

Synonym: ARM390 Hydrochloride,ARM-390 HCl

Target: Opioid Receptor

Cat.No: T27806

Synonym: SRA-333,SRA333,SRA 333,Lecozotan hydrochloride

Target: 5-HT Receptor

Cat.No: T33289

Cat.No: T36634

Cat.No: T71398

Cat.No: T76399

Cat.No: T38392

Proadrenomedullin (N-20) (bovine, porcine)

Cat.No: T80503

Synonym: ProADM N20(bovine, porcine),PAMP-20(bovine, porcine)

(R)-PF-06256142

Cat.No: T72744

Cat.No: TP2058

Cat. No.	Product Name	Target	Signaling Pathways
TN5580	Rediocide A
	Rediocide A, an insecticide, can inhibit calcium mobilization in Drosophila G-protein- coupled receptors (GPCR)s other than methuselah, it can induce GPCR desensitization and internalization, and such effects are mediated by the activation of conventional

天然产物

Cat.No: TN5580

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