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26

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9232	Mitochondrial fusion promoter M1	Mitochondrial Metabolism	Metabolism
	Mitochondrial fusion promoter M1 是一种线粒体动态调节剂，能够保持线粒体功能并促进细胞呼吸，减轻心肌缺血/再灌注大鼠的心脏损伤和大脑损伤。
T21793	CGP 35348	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	CGP 35348 是 GABAB 受体的选择性拮抗剂 (EC50 = 34 μM)。 CGP 35348 可用于研究白化新生小鼠脑损伤后的神经肌肉协调和空间学习。
T9776	TRPM4 inhibitor 8	TRP/TRPV Channel	Membrane transporter/Ion channel
	TRPM4 inhibitor 8 是瞬态受体电位 melastatin 4 (TRPM4) 的抑制剂，它有助于活力、迁移、细胞周期转变和粘附。
T70470L	isomer-CM 352 isomer-1542205-83-3	MMP	Proteases/Proteasome
	isomer-CM 352 是一种金属酶抑制剂，可用于减缓脑损伤。
T70470	CM-352	MMP	Proteases/Proteasome
	CM-352是一种金属蛋白酶抑制剂，可减少脑损伤并改善脑出血大鼠模型的功能恢复。
T28607	Rocepafant LAU 8080,LAU8080,BN 50730,LAU-8080,BN50730,BN-50730	Platelet aggregation	Others
	Rocepafant (LAU8080) 是一种血小板活化因子(PAF)拮抗剂，可减轻新生大鼠缺氧缺血性脑损伤。Rocepafant 抑制肿瘤坏死因子-Afa 介导的小鼠 L929 肿瘤细胞的细胞毒性。
T32098L	Homocarnosine acetate	GABA Receptor; Endogenous Metabolite	Membrane transporter/Ion channel; Metabolism; Neuroscience
	Homocarnosine acetate 是大脑特有的二肽，由 γ-氨基丁酸 (GABA) 和组氨酸组成。它具有抗氧化和抗炎作用、预防 DNA 损伤和抑制晚期糖基化终产物形成
T73599	TSPO ligand-1	Autophagy	Autophagy
	TSPO ligand-1 对外周和中枢苯二氮卓受体有亲和力。TSPO ligand-1 是一种线粒体外膜跨膜结构域上与 AUTAC4 结合的蛋白，可诱导线粒体自噬 (autophagy) 促进胞内线粒体更新。TSPO ligand-1 参与胆固醇在胞内的转运，可作为脑损伤和神经变性的生物标志物。
T72662	NMDAR/TRPM4-IN-2	ERK; TRP/TRPV Channel; NMDAR; iGluR	MAPK; Membrane transporter/Ion channel; Neuroscience
	NMDAR/TRPM4-IN-2 是一种有效的 NMDAR/TRPM4 相互作用界面抑制剂。NMDAR/TRPM4-IN-2 保护小鼠免受 MCAO 诱导的脑损伤和 NMDA 诱导的视网膜神经节细胞丢失。NMDAR/TRPM4-IN-2 具有神经保护活性，可预防 NMDA 诱导的海马神经元细胞死亡和线粒体功能障碍，其 IC50 值为 2.1 μM。
T38063	N-Acetyl lysyltyrosylcysteine amide	Glutathione Peroxidase	Metabolism
	N-Acetyl lysyltyrosylcysteine amide 是一种无毒的髓过氧化物酶 (MPO) 三肽抑制剂，具有有效性，可逆性和特异性。N-Acetyl lysyltyrosylcysteine amide 在体内可有效抑制 MPO 产生。N-Acetyl lysyltyrosylcysteine amide 减轻中风后大脑的神经元损伤，并保留脑组织和神经功能。N-Acetyl lysyltyrosylcysteine amide 抑制MPO依赖性次氯酸 (HOCl) 的生成，蛋白质硝化和 LDL 氧化。N-Acetyl lysyltyrosylcysteine amide 可用于研究支气管发育不良。
T61268	Vutiglabridin HSG4112	Phosphatase	Metabolism
	Vutiglabridin (HSG4112) 是一种新型且安全的PON2调节剂，是一个外消旋化合物。Vutiglabridin 是Glabridin 的优化结构类似物，比Glabridin 在减重效果和化学稳定性方面更加优越。Vutiglabridin 通过靶向线粒体对氧磷酶-2改善mptp 诱导的帕金森病小鼠的神经变性。Vutiglabridin 是一种治疗肥胖的临床2期药物，在PD 模型中对对线粒体PON2具有治疗作用。Vutiglabridin 渗透到大脑，结合PON2，恢复1-甲基-4-苯基吡啶(MPP*)诱导的SH-SY5Y 神经母细胞瘤细胞线粒体功能障碍。Vutiglabridin 在小鼠实验中显著减轻了1-甲基-4苯基-1,2,3,6-四氢吡啶(MPTP)诱导的PD 模型小鼠的运动障碍和多巴胺能神经元损伤。
T25722	Lifarizine methanesulfonate
	Lifarizine methanesulfonate is a modulator of sodium-calcium channel that reduces ischemic brain damage.
T27959	LY503430 LY-503430,LY 503430
	LY503430 is a AMPA receptor potentiator with oral activity. LY503430 has both nootropic and neuroprotective effects, reducing brain damage caused by 6-hydroxydopamine or MPTP.
T70838	RO27-3225 TFA
	RO27-3225, also known as RO273225 is a melanocortin type 4 receptor agonist with EC50 = 1 nM. It may alleviate intestinal dysfuntion and brain damage. It has been investigated for an anti-obesity medication. Ro 27-3225 shows some activity at the MC1 receptor. Ro 27-3225 reverses hemorrhagic shock, reduces multiple organ damage, and improves survival.
T26627	Anatibant LF16-0687,LF-16-0687,LF 160687,LF 16-0687,LF-160687
	Anatibant 是一种有效的非肽缓激肽B2受体拮抗剂。Anatibant 降低实验性外伤性脑损伤后颅内高压和组织病理学损伤。
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。
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。
T73508	FLDP-5
	FLDP-5 为一种可透过血脑屏障的姜黄素类似物，能够诱导活性氧（ROS）产生、DNA损伤及细胞周期S期阻滞。此外，FLDP-5 在抑制LN-18细胞增殖和迁移方面表现出显著的抗肿瘤活性。
T78071	3-Methylglutaconic acid β-Methylglutaconic acid	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	3-Methylglutaconic acid 是MGTA (3-甲基戊二酸尿症) 的主要积累代谢物，能够诱发脂质和蛋白质的氧化损伤，减弱大脑皮层上清液的非酶促抗氧化防御，导致氧化应激。此化合物适用于研究大脑损伤相关疾病。
T62062	MAO-B-IN-7
	MAO-B-IN-7 是有效的、具有血脑屏障渗透性的MAO-B 和AChE 抑制剂。MAO-B-IN-7抑制人 AChE、电鳗 AChE 和 MAO-B 的IC50分别为 41 nM、87 nM 和 0.3 μM。MAO-B-IN-7 可以有效缓解氧化应激和神经炎症损伤。
T73818	Homocarnosine TFA
	Homocarnosine TFA, 作为一种大脑特定的γ-氨基丁酸(GABA)与组氨酸的二肽, 具备抑制性神经调节功能。它在神经元内由GABA合成，既显示出抗惊厥效应，也表现抗氧化、抗炎作用，能防止DNA损伤并抑制晚期糖基化终产物的形成。
T81573	Pabinafusp alfa JR-141
	Pabinafusp alfa (JR-141) 是由Iduronate 2-sulfatase和抗人转铁蛋白受体抗体结合而成的转铁蛋白受体靶向抗体。它具备穿透血脑屏障的能力，可防止粘多糖病II型(MPS II)小鼠中枢神经系统中硫酸肝素(HS)的积累。此外，Pabinafusp alfa能够促进小鼠的学习能力，并抑制中枢神经系统神经元的损伤。
T73989	Tirilazad
	Tirilazad是一种21-氨基类固醇非糖皮质激素，具有抑制脂质过氧化的能力。它对于脑或脊髓中因创伤、中风、缺血再灌注损伤所致的损害有减轻作用。此外，Tirilazad还展现出针对新型肺炎病毒的抗病毒活性，并在缺血性中风中提供神经保护，适用于蛛网膜下腔出血研究场景。
T36701	Phosphoramide mustard (cyclohexanamine)
	Phosphoramide mustard cyclohexanamine is the major metabolite for Cyclophosphamide , with anticancer activitiy. Phosphoramide mustard cyclohexanamine induces DNA adduct formation in ovarian granulosa cells, induces DNA damage and elicits the ovarian DNA repair response[1][2]. Phosphoramide mustard cyclohexanamine causes cytotoxicity through forming cross-linked DNA adducts which inhibit DNA strand separation during replication[1].Phosphoramide mustard cyclohexanamine destroys rapidly dividing ce...
T37898	UDP-α-D-Glucose (sodium salt hydrate)
	UDP-α-D-Glucose is an endogenous nucleotide sugar involved in glycosyltransferase reactions in metabolism. It has been shown to bind the P2Y14receptor (EC50= 0.35 μM), an atypical P2Y receptor involved in the activation of dendritic cells and glial cells.1It can also bind to and activate GPR17, inducing oligodendrocyte differentiation at a maximal concentration of 100 μM.2 1.Jacobson, K.A., Ivanov, A.A., de Castro, S., et al.Development of selective agonists and antagonists of P2Y receptorsPurin...
T36947	Pyrithiamine (hydrobromide)
	Pyrithiamine is the pyridine analog of thiamine that prevents growth of organisms that require intact thiamine. [1] It inhibits the growth of bacterial and fungal species at a pyrithiamine:thiamine ratio of 10:1 in growth media and induces symptoms of thiamine deficiency in mice at a dietary ratio of 3:1. These effects are reversible with addition of sufficient thiamine in all species. Pyrithiamine inhibits the formation of cocarboxylase from thiamine in chicken blood in a dose-dependent manner....

化合物

Mitochondrial fusion promoter M1

Cat.No: T9232

Target: Mitochondrial Metabolism

Cat.No: T21793

Target: GABA Receptor

TRPM4 inhibitor 8

Cat.No: T9776

Target: TRP/TRPV Channel

Cat.No: T70470L

Synonym: isomer-1542205-83-3

Target: MMP

Cat.No: T70470

Target: MMP

Cat.No: T28607

Synonym: LAU 8080,LAU8080,BN 50730,LAU-8080,BN50730,BN-50730

Target: Platelet aggregation

Homocarnosine acetate

Cat.No: T32098L

Target: GABA Receptor, Endogenous Metabolite

Cat.No: T73599

Target: Autophagy

NMDAR/TRPM4-IN-2

Cat.No: T72662

Target: ERK, TRP/TRPV Channel, NMDAR, iGluR

N-Acetyl lysyltyrosylcysteine amide

Cat.No: T38063

Target: Glutathione Peroxidase

Cat.No: T61268

Synonym: HSG4112

Target: Phosphatase

Lifarizine methanesulfonate

Cat.No: T25722

Cat.No: T27959

Synonym: LY-503430,LY 503430

Cat.No: T70838

Cat.No: T26627

Synonym: LF16-0687,LF-16-0687,LF 160687,LF 16-0687,LF-160687

LQVTDSGLYRCVIYHPP

Cat.No: T78025

LQVTDSGLYRCVIYHPP TFA

Cat.No: T78026

Cat.No: T73508

3-Methylglutaconic acid

Cat.No: T78071

Synonym: β-Methylglutaconic acid

Target: GABA Receptor

Cat.No: T62062

Homocarnosine TFA

Cat.No: T73818

Pabinafusp alfa

Cat.No: T81573

Synonym: JR-141

Cat.No: T73989

Phosphoramide mustard (cyclohexanamine)

Cat.No: T36701

UDP-α-D-Glucose (sodium salt hydrate)

Cat.No: T37898

Pyrithiamine (hydrobromide)

Cat.No: T36947

Cat. No.	Product Name	Target	Signaling Pathways
T4S1725	Galanthamine Galantamine,加兰他敏	Apoptosis; AChE	Apoptosis; Neuroscience
	Galanthamine (Galantamine) 是一种乙酰胆碱酯酶抑制剂，IC50为 500 nM。
T3414	Morroniside 莫诺苷,奎宁树	Apoptosis; MMP; Pyroptosis	Apoptosis; Immunology/Inflammation; Proteases/Proteasome
	Morroniside 通过抑制神经元凋亡和 MMP9/2 的表达从而发挥神经保护作用，可作为 db/db 小鼠肝脏炎症反应和脂质代谢的调节剂。它通过抑制高血糖和氧化应激表现出对糖尿病肾损伤和人脐静脉内皮细胞的保护作用。
T5S0636	Citric acid 柠檬酸,Citro,Citretten	Apoptosis; Others; Endogenous Metabolite; Antibacterial; Antibiotic	Apoptosis; Metabolism; Microbiology/Virology; Others
	Citric acid (Citro) 是柑橘类水果中发现的弱有机三羧酸。柠檬酸是食品添加剂和天然防腐剂。
T3S1729	Dihydrolycorine	Others	Others
	Dihydrolycorine 是分离自Lycoris radiate 草药中，是一种真核细胞中蛋白质合成的抑制剂。
T5232	3-Methyl-2-oxobutanoic acid 3-甲基-2-氧丁酸,2-Oxoisovaleric acid,alpha-Ketoisovaleric acid	Others; Endogenous Metabolite	Metabolism; Others
	3-Methyl-2-oxobutanoic acid (2-Oxoisovaleric acid) 是大肠杆菌中泛酸的前体。它是由支链氨基酸的不完全分解产生的一种异常代谢物。
TN2257	Tanshinone IIB 丹参酮ⅡB	BCL; Caspase; P-gp	Apoptosis; Membrane transporter/Ion channel; Neuroscience; Proteases/Proteasome
	Co-treatment with Tanshinone IIB (TSB) significantly inhibits the DNA laddering, cytotoxicity and apoptosis of rat cortical neurons induced by staurosporine in a concentration-dependent manner; TSB also suppresses the elevated Bax protein and decreased bc
TN3323	Monomethyl lithospermate Lithospermic acid monomethyl ester	Akt; PI3K	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	Monomethyl lithospermate (Lithospermic acid monomethyl ester) 具有潜在的抗病毒活性，通过激活PI5K/Akt信号传导，减轻体内大脑中动脉闭塞小鼠缺血性中风损伤，并在体外保护氧葡萄糖剥夺/复氧诱导的SHSY-3Y细胞。Monomethyl lithospermate 能提高 SHSY-5Y 细胞的生存能力，抑制线粒体膜电位 (MMOP) 崩溃，抑制细胞凋亡。Monomethyl lithospermate 还降低中动脉闭塞 (MCAO) 大鼠脑组织中的氧化应激水平，改善缺血性中风 (IS) 大鼠神经损伤。

天然产物

Cat.No: T4S1725

Synonym: Galantamine,加兰他敏

Target: Apoptosis, AChE

Cat.No: T3414

Synonym: 莫诺苷,奎宁树

Target: Apoptosis, MMP, Pyroptosis

Cat.No: T5S0636

Synonym: 柠檬酸,Citro,Citretten

Target: Apoptosis, Others, Endogenous Metabolite, Antibacterial, Antibiotic

Dihydrolycorine

Cat.No: T3S1729

Target: Others

3-Methyl-2-oxobutanoic acid

Cat.No: T5232

Synonym: 3-甲基-2-氧丁酸,2-Oxoisovaleric acid,alpha-Ketoisovaleric acid

Target: Others, Endogenous Metabolite

Cat.No: TN2257

Synonym: 丹参酮ⅡB

Target: BCL, Caspase, P-gp

Monomethyl lithospermate

Cat.No: TN3323

Synonym: Lithospermic acid monomethyl ester

Target: Akt, PI3K

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