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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T8552	PSEM 89S TFA	AChR	Neuroscience
	PSEM 89S TFA 是一种脑渗透性和选择性离子通道激动剂，分别对 Q79G 和 L141F 具有正交选择性。
T78025	LQVTDSGLYRCVIYHPP
	LQVTDSGLYRCVIYHPP (LP17) 为髓系细胞表达之触发受体 1 (TREM-1) 抑制性肽类化合物，能有效减轻缺血引发的梗塞及神经元损害，并可渗透大脑，阻断TREM-1。
T11434	GlyRS-IN-1	Others	Others
	GlyRS-IN-1 is an inhibitor of glycyl-tRNA synthase (GlyRS). It can inhibit the growth of bacteria.
T78026	LQVTDSGLYRCVIYHPP TFA
	LQVTDSGLYRCVIYHPP (LP17) TFA 是一种针对髓系细胞表面的触发受体1 (TREM-1) 的抑制肽。该化合物能有效减缓缺血导致的梗塞及神经元损害，并可穿透血脑屏障，阻断 TREM-1的活性。
T36811	uPSEM 817 tartrate
	Selective ultrapotent PSEM (uPSEM) agonist for α7L131G,Q139L,Y217F-GlyR (PSAM4-GlyR) and PSAM4-5-HT3 chimeric ion channel agonist (EC50 values are 0.3 and 0.5 nM, respectively). Suppresses firing of layer 2/3 cortical neurons expressing PSAM4-GlyR in brain slices. Increases contralateral rotation in mice expressing PSAM4-GlyR unilaterally in the substantia nigra reticulata (LED 0.1 mg/kg). Magnus et al (2019) Ultrapotent chemogenetics for research and potential clinical applications. Science 3...
T36810	uPSEM 792 hydrochloride
	Ultrapotent PSEM (uPSEM) agonist for PSAM4-GlyR and PSAM4-5HT3 (Ki = 0.7 nM for PSAM4-GlyR and <10 nM for PSAM4-5HT3). Exhibits >10,000-fold agonist selectivity for PSAM4-GlyR over α7-GlyR, α7-5HT3, and 5HT3-R, and 230-fold selectivity over α4β2 nAChR. Also weak partial agonist (~10 %) at α4β2 nAChR. Retains the potency of varenicline (Cat.No. 3754) for PSAM4-GlyR with enhanced chemogenetic selectivity. Does not act as a substrate for P-glycoprotein pumps. Silences neurons in vivo. Brain-penetra...
T61655	AM-1488
	AM1488 是一种有效的、具有口服活性的甘氨酸受体 (GlyR) 增效剂 (hGlyRα3EC50=0.45 μM)。
T37391	PSEM 308 hydrochloride
	PSAM (pharmacologically selective actuator module) agonist. Activates PSAML141F-GlyR chimeric ion channels. Inhibits activity of neurons expressing PSAML141F-GlyR in vivo and activates locus coeruleus noradrenergic neurons expressing PSAML141F,Y115F-5-HT3 ion channels. Recommended concentration for use in mice is 5 mg/kg or lower. Plasmid vectors for the transfection of cells with PSAML141F-GlyR and PSAML141F,Y115F-5-HT3 are available from Addgene. Lovett-Barron et al (2012) Regulation of neu...
T10618	Broflanilide	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Broflanilide 是昆虫抗狄氏剂 GABA 受体拮抗剂，可代谢为 Desmethyl-Broflanilide，抑制斜纹夜蛾 RDL GABAR，IC50值为 1.3 nM。
T16292	NFPS	Thrombin	Proteases/Proteasome
	NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion. NFPS is a selective and non-competitive glycine transporter-1 (GlyT1) inhibitor (IC50s: 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively).

化合物

LQVTDSGLYRCVIYHPP TFA

uPSEM 792 hydrochloride

PSEM 308 hydrochloride

Target: GABA Receptor

Cat. No.	Product Name	Target	Signaling Pathways
T4811	D-Alanine D-α-Alanine,Ba 2776,(R)-Alanine,D-丙氨酸,(R)-2-Aminopropionic acid	Chloride channel; Endogenous Metabolite	Membrane transporter/Ion channel; Metabolism
	D-Alanine ((R)-Alanine) 是一种GlyR 和PMBA 的弱激动剂，其对GlyR 的EC50=9 mM。
T16533	Picrotin	Chloride channel	Membrane transporter/Ion channel
	Picrotin 是甘氨酸受体的抑制剂。 Picrotin 阻断 α2 GlyR、α1 GlyR 和 α3 GlyR，可用于神经传递研究。

天然产物

D-Alanine

Cat.No: T4811

Synonym: D-α-Alanine,Ba 2776,(R)-Alanine,D-丙氨酸,(R)-2-Aminopropionic acid

Target: Chloride channel, Endogenous Metabolite

Picrotin

Cat.No: T16533

Synonym:

Target: Chloride channel

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