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35

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T4330	CaCCinh-A01	Chloride channel	Membrane transporter/Ion channel
	CaCCinh-A01 是钙激活氯离子通道和TMEM16A 抑制剂，IC50值分别为 10 和 2.1 μM。
T1476	Pramipexole SND 919,普拉克索	Dopamine Receptor	GPCR/G Protein; Neuroscience
	Pramipexole (SND 919) 是能够透过血脑屏障的 D2 型多巴胺受体的选择性激动剂，对 D2 型受体、D2、D3、D4亚型受体的Ki 分别为 2.2 nM、3.9 nM、0.5 nM、1.3 nM。它可用于研究帕金森综合症和腿多动综合征。
T23146	PHA 568487 free base PHA 568487	AChR	Neuroscience
	PHA 568487 free base 是一种选择性的 α7 烟碱乙酰胆碱受体激动剂，可用于减缓神经炎症。
T6951	Pramipexole dihydrochloride hydrate Pramipexole 2HCl Monohydrate,普拉克索盐酸盐水合物,Mirapex,普拉克索	Dopamine Receptor	GPCR/G Protein; Neuroscience
	Pramipexole dihydrochloride hydrate (Mirapex) 是选择性的，具有血脑屏障 (BBB) 渗透性的 D2 型多巴胺受体激动剂，对 D2 型受体、D2、D3、D4亚型受体的 Ki 分别为 2.2 nM、3.9 nM、0.5 nM、1.3 nM，可用于研究帕金森综合症和腿多动综合征。
T27830	Lifarizine RS 87476,RS 87476-000,RS-87476,RS-87476-000,RS87476	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Lifarizine (RS-87476) 是一种钙钠通道拮抗剂，在简化的大鼠双血管闭塞存活模型中显示出神经保护活性。
T24873	TGX-115 TGX 115	PI3K	PI3K/Akt/mTOR signaling
	TGX-115是一种细胞渗透性和有效的PI 3-K 异构体p110β/p110δ抑制剂(对p110β IC50值为 0.13 μM, 对p110δ值为0.63 μM），是一种调节血小板粘附过程的酶，可抑制磷酸肌苷（PI）3-激酶，可用来治疗冠状动脉闭塞、中风、急性冠状动脉综合征、急性心肌梗塞、血管再狭窄、动脉硬化和不稳定心绞痛等心血管疾病。
T11994	Melagatran	Thrombin	Proteases/Proteasome
	Melagatran 是一种直接作用且可口服的凝血酶抑制剂。Melagatran 专一性抑制凝血酶，但不影响凝血级联中的其他酶或纤溶酶。Melagatran不依赖内源性辅因子发挥其抗凝血酶效果，可缓解内毒素血症的有害影响。因此，Melagatran作为预防动脉闭塞的策略显示出前景。
T70540	Pinokalant LOE-908	SARS-CoV; TRP/TRPV Channel	Membrane transporter/Ion channel; Microbiology/Virology
	Pinokalant (LOE-908) 是一种新型非选性阳离子通道抑制剂。Pinokalant 在体内实验中可显著减少皮质梗死体积，可改善缺血半影区的代谢和电生理状态，可减少大鼠大脑中动脉闭塞后急性期磁共振图像上的病变大小。Pinokalant是一种潜在的SARS-CoV-2蛋白酶抑制剂，可用于研究脑卒中。
T35689	MTP 131 acetate	Others	Others
	MTP 131 acetate 是一种小的线粒体靶向四肽。
T27897	LY 215490 LY215490,LY-215490
	LY 215490 is a selective, competitive and systemically active antagonist of AMPA receptor. LY 215490 has neuroprotective effect against focal ischaemia in a model of permanent MCA occlusion in the rat.
T16902	SMND-309	Others	Others
	SMND-309 is a metabolite of salvianolic acid B. It also shows neuroprotective effects in cultured neurons and in permanent middle cerebral artery occlusion rats.
T41029	Streptokinase
	Streptokinase is a bacterial protein that acts as a plasminogen activator, commonly employed in the investigation of blood-clotting disorders. Its application extends to enhancing reperfusion blood flow after coronary artery occlusion.
T27351	Fostedil KB-944,KB944,A 53986,KB 944,A-53986,BRN 3626546
	Fostedil is a calcium channel antagonist. KB-944 increased regional segment function in normal and ischemic regions and maintained distal coronary artery perfusion pressure, coronary flow and transmural regional myocardial blood flow during partial corona
T68814	GZN39838
	GZN39838, also known as 6beta-Acetoxy-7alpha-hydroxyroyleanone is a natural blocker of Kv1.2 channels, not involving direct occlusion of the outer pore but depending on C-type inactivation.
T76987	Tarcocimab
	Tarcocimab (OG1953) 是一种人源化抗VEGFA 单克隆抗体 (IgG1 型)。Tarcocimab 可用于视网膜静脉阻塞 (RVO) 和湿性老年性黄斑变性 (AMD) 的研究。
T81455	Piridoxilate Piridoxylate
	Piridoxilate (Piridoxylate)，一种乙醛酸酯衍生物，属于抗缺氧剂。该化合物主要应用于血管疾病及冠状动脉闭塞的研究领域。
T28414	Piclozotan SUN-N-4057,SUN4057,SUNN-4057,SUN-4057,SUNN4057	5-HT Receptor	GPCR/G Protein; Neuroscience
	Piclozotan (anhydrous) 是一种 5-HT1A 受体激动剂，在短暂的大脑中动脉闭塞（t-MCAO）模型中表现出显着的神经保护活性,可以改善晚期帕金森病患者的运动并发症。
T83730	Tat-M2NX TFA
	Tat-M2NX是一种瞬时受体电位麦拉斯汀2（TRPM2）的肽类拮抗剂。在25到100µM的浓度范围内，能够抑制表达人类TRPM2的HEK293细胞中氢过氧化物诱导的钙离子流入。在体内，Tat-M2NX（20 mg/kg）通过在中大脑动脉阻塞（MCAO）诱导的中风模型中，如果在阻塞前或阻塞后3小时内给药，能减少雄性小鼠的脑梗塞体积，但对雌性小鼠无效。
T36570	KUS121
	KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50= 330 nM).1It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in anin vitromodel of cerebral ischemia.2It red...
T35463	(±)14(15)-EET (±)14,15-EET,(±)14,15-EpETrE,(±)14(15)-EET
	(±)14(15)-EET is a metabolite of arachidonic acid that is formed via epoxidation of arachidonic acid by cytochrome P450.[1],[2] It prevents increases in leukotriene B4, ICAM-1, and chemokine (C-C motif) ligand 1 (CCL2) induced by oxidized LDL in primary rat pulmonary artery endothelial cells (RPAECs) when used at a concentration of 1 μM.[3] (±)14(15)-EET induces dilation of preconstricted isolated canine coronary arterioles (EC50 = 0.2 pM).[4] It reduces myocardial infarct size as a percentage o...
T28933	TCV-309 TCV309
	TCV-309 is an inhibitor of platelet activating factor (PAF). TCV-309 reduces graft PMN infiltration and enhances early function of 24-hour-preserved rat kidneys with long warm ischemia. TCV-309 attenuates the priming effects of bronchoalveolar macrophages
T69813	AZD-6126
	AZD6126, also known as ANG-453, a water-soluble phosphate prodrug of N-acetylcolchinol with potential antiangiogenesis and antineoplastic activities. AZD-6126 is an angiogenesis inhibitor and tubulin inhibitor potentially for the treatment of solid tumours. AZD6126 is converted in vivo into N-acetylcolchinol. N-acetylcolchinol binds to and destabilizes the tubulin cytoskeleton of endothelial cells in tumor blood vessels, which may result in tumor endothelial cel apoptosis, the selective occlusio...
T34112	Porfimer Sodium DHE,dihematoporphyrin ether,CL184116,CL-184116,CL 184116,Porfimer
	Porfimer sodium is t he sodium salt of a mixture of oligomers formed by ether and ester linkages of up to eight porphyrin units with photodynamic activity. Absorbed selectively by tumor cells, porfimer produces oxygen radicals after activation by 630 nm w
T36553	Thrombin Receptor Peptide Ligand (trifluoroacetate salt)
	Thrombin receptor peptide ligand is antagonist of the thrombin receptor (EC50s = 16-33 μM to inhibit platelet aggregation in vitro). It inhibits α-thrombin and platelet aggregation induced by thrombin receptor activating peptide in vitro when used at a concentration of 32 μM but does not affect platelet aggregation induced by ADP or collagen. It also inhibits thrombin- and TRAP-induced proliferation of vascular smooth muscle cells (VSMCs). Thrombin receptor peptide ligand (100 μmol/kg bolus, i.v...
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...
T83695	MOG Peptide (human, bovine) acetate Myelin Oligodendrocyte Glycoprotein Peptide
	Myelin Oligodendrocyte Glycoprotein (MOG) peptide 是 MOG 的一种内源性肽段截取，存在于髓鞘的细胞外表面。当与抗原血清型HLA-DR2结合时，MOG peptide 在通过中脑动脉阻塞（MCAO）诱导的缺血性中风模型中，能减少皮层和纹状体梗死体积，降低管-角转测试中的感觉运动障碍，增加对新奇气味的探索时间，以及增加雌性（但不是雄性）小鼠对笼伴侣发出的呼叫持续时间。
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...
T71402	Nicorandil-d4
	Nicorandil-d4 is intended for use as an internal standard for the quantification of nicorandil by GC- or LC-MS. Nicorandil is an activator of sulfonylurea receptor 2B (SUR2B) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = ~10 µM) and a nitric oxide (NO) donor. It is selective for SUR2B/Kir6.2 over the SUR2A/Kir6.2 channel (EC50 = >500 µM). Nicorandil activates soluble guanylate cyclase in a cell-free assay and relaxes partially depolarized isolated bovine coronary artery strips (EC50 =...
T83777	LAU-0901
	LAU-0901是一种血小板活化因子(PAF)受体拮抗剂。在体内，LAU-0901（30、60及90 mg/kg）通过减少梗塞体积和改善大鼠由中脑动脉阻塞(MCAO)引起的脑缺血模型中的神经功能来发挥作用。它还能减少同一模型中的小胶质细胞浸润，并增加星形胶质细胞和神经元的存活率。单独使用LAU-0901（30 mg/kg）或与阿托伐他汀联合使用，能减少U87MG胶质母细胞瘤小鼠原位肿瘤模型中的肿瘤生长。
T36722	Deltorphin II (trifluoroacetate salt)
	Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid...
T83729	Tat-CIRP TFA Tat-Cold-inducible RNA Binding Protein
	Tat-CIRP是一种肽类抑制剂，用于抑制髓样分化2蛋白(MD-2，亦称淋巴细胞抗原96 [LY96])与寒冷诱导的RNA结合蛋白(CIRP)之间的蛋白-蛋白相互作用。它通过与MD-2结合，干扰MD-2与CIRP之间的相互作用，这一作用在共免疫沉淀实验中得到证实。在体内实验中，Tat-CIRP (10及20 mg/kg) 能够减少由中脑动脉闭塞(MCAO)引发的小鼠脑梗死体积。同样，在通过血栓引发脑梗死的恒河猴模型中，Tat-CIRP同样能减少脑梗死体积，并缩短患中风一侧手臂抓取并放下食物的时间。
T83727	Tat-NTS Peptide TFA Tat-Nuclear Translocation Signal Peptide
	Tat-NTS肽是一种能穿透细胞的肽，由HIV-1 Tat蛋白的转导域与对应于脂联素A1重复III域残基228-237的10个氨基酸肽链接而成，扮演核转运信号（NTS）的角色。它通过阻断脂联素A1与进口素β之间的蛋白质-蛋白质相互作用，阻止脂联素A1在初级鼠海马神经元中的核内转运。Tat-NTS抑制初级鼠海马神经元在葡萄糖-氧剥夺及再灌注诱导的细胞凋亡。在体内，Tat-NTS（10 mg/kg）有效减少了由中脑动脉闭塞（MCAO）引起的缺血-再灌注损伤模型小鼠的梗塞体积和神经元凋亡，并缩短了在Morris水迷宫测试中达到平台的时间。
T83731	Tat-CBD3 TFA
	Tat-CBD3是一种抑制N型电压门控钙通道Cav2.2与collapsin response mediator protein 2 (CRMP2)之间的蛋白质-蛋白质相互作用的抑制剂。它还能抑制CRMP2与NMDA受体NR2B亚单位之间的蛋白质-蛋白质相互作用。在无细胞实验中，Tat-CBD3 (10 µM)能将Cav2.2-CRMP2相互作用抑制43%，并在免疫共沉淀实验中抑制NMDA受体NR2B亚单位-CRMP2相互作用。它能在初级大鼠背根神经节 (DRG) 神经元中减少约60%的电压诱导钙电流，并在初级大鼠海马神经元中减少谷氨酸诱导的胞内钙水平增加。Tat-CBD3 (20 mg/kg)在大鼠中脑动脉闭塞 (MCAO) 引发的脑缺血模型中减少梗死体积。鞘内给药Tat-CBD3 (20 µg/5 µl)可防止大鼠卡拉胶诱导的热敏感性。
T83682	Tat-Gap 19 TFA
	Tat-Gap 19是一种针对连接蛋白43 (Cx43) 半通道的肽抑制剂，由HIV-1 Tat蛋白传导域与对应于Cx43第128-136残基的九氨基酸肽连接而成。Tat-Gap 19 (10 µM) 能够抑制初级大鼠肝细胞中由谷氨酸引发的ATP释放，这是Cx43半通道活性的标志。在通过中脑动脉堵塞(MCAO)诱导的小鼠脑缺血再灌注损伤模型中，以25 mg/kg的剂量进行给药，可减少梗死体积。腹腔内注射Tat-Gap 19 (1 mg/kg 每天) 能够减少硫代乙酰胺引起的小鼠肝损伤模型中的纤维化病灶面积及表达α-平滑肌肌动蛋白 (α-SMA) 的肝星状细胞（成纤维细胞的前体）面积，并提高同种小鼠分离的肝细胞中超氧化物歧化酶 (SOD) 活性。
T83825	Trofinetide acetate NNZ-2566
	Trofinetide是一种衍生自具有神经保护作用的三肽Gly-Pro-Glu的化合物，后者是胰岛素样生长因子-1（IGF-1）的N-端序列。在10 nM的浓度下使用时，它能减少由蛋白磷酸酶抑制剂奥卡达酸在原代大鼠胚胎纹状体神经元中引起的细胞死亡。Trofinetide在一种由穿透性弹道样脑损伤引起的大鼠神经炎症模型中减少了编码IL-1β、TNF-α、IL-6和E-selectin的mRNA的脑表达。在通过中脑动脉闭塞（MCAO）引起的大鼠脑损伤模型中，以30和60 mg/kg的剂量给药时，它减少了皮层和纹状体梗塞区域。Trofinetide（每天100 mg/kg）减少了树突棘的数量，并逆转了在fmr1-/-敲除小鼠脆性X综合征模型中的社交识别和情景恐惧条件反射的缺陷，同时也减少了睾丸重量的增加。含有Trofinetide的制剂已被用于治疗Rett综合征。

化合物

Cat.No: T4330

Target: Chloride channel

Cat.No: T1476

Synonym: SND 919,普拉克索

Target: Dopamine Receptor

PHA 568487 free base

Cat.No: T23146

Synonym: PHA 568487

Target: AChR

Pramipexole dihydrochloride hydrate

Cat.No: T6951

Synonym: Pramipexole 2HCl Monohydrate,普拉克索盐酸盐水合物,Mirapex,普拉克索

Target: Dopamine Receptor

Cat.No: T27830

Synonym: RS 87476,RS 87476-000,RS-87476,RS-87476-000,RS87476

Target: Calcium Channel

Cat.No: T24873

Synonym: TGX 115

Target: PI3K

Cat.No: T11994

Target: Thrombin

Cat.No: T70540

Synonym: LOE-908

Target: SARS-CoV, TRP/TRPV Channel

MTP 131 acetate

Cat.No: T35689

Target: Others

Cat.No: T27897

Synonym: LY215490,LY-215490

Cat.No: T16902

Target: Others

Cat.No: T41029

Cat.No: T27351

Synonym: KB-944,KB944,A 53986,KB 944,A-53986,BRN 3626546

Cat.No: T68814

Cat.No: T76987

Cat.No: T81455

Synonym: Piridoxylate

Cat.No: T28414

Synonym: SUN-N-4057,SUN4057,SUNN-4057,SUN-4057,SUNN4057

Target: 5-HT Receptor

Cat.No: T83730

Cat.No: T36570

Cat.No: T35463

Synonym: (±)14,15-EET,(±)14,15-EpETrE,(±)14(15)-EET

Cat.No: T28933

Synonym: TCV309

Cat.No: T69813

Porfimer Sodium

Cat.No: T34112

Synonym: DHE,dihematoporphyrin ether,CL184116,CL-184116,CL 184116,Porfimer

Thrombin Receptor Peptide Ligand (trifluoroacetate salt)

Cat.No: T36553

Cat.No: T37671

Synonym: CAY10608

MOG Peptide (human, bovine) acetate

Cat.No: T83695

Synonym: Myelin Oligodendrocyte Glycoprotein Peptide

Cat.No: T70063

Cat.No: T71402

Cat.No: T83777

Deltorphin II (trifluoroacetate salt)

Cat.No: T36722

Cat.No: T83729

Synonym: Tat-Cold-inducible RNA Binding Protein

Tat-NTS Peptide TFA

Cat.No: T83727

Synonym: Tat-Nuclear Translocation Signal Peptide

Cat.No: T83731

Cat.No: T83682

Trofinetide acetate

Cat.No: T83825

Synonym: NNZ-2566

Cat. No.	Product Name	Target	Signaling Pathways
T2163	Dihydrocapsaicin CCRIS1589,二氢辣椒素,6,7-Dihydrocapsaicin,8-Methyl-N-vanillylnonanamide	Others; TRP/TRPV Channel	Membrane transporter/Ion channel; Others
	Dihydrocapsaicin (CCRIS1589) 是一种天然来源的辣椒素，是TRPV1的选择性激动剂，同时可以增加 p-Akt 水平。它可以增强低温诱导的神经保护。
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

Dihydrocapsaicin

Cat.No: T2163

Synonym: CCRIS1589,二氢辣椒素,6,7-Dihydrocapsaicin,8-Methyl-N-vanillylnonanamide

Target: Others, TRP/TRPV Channel

Monomethyl lithospermate

Cat.No: TN3323

Synonym: Lithospermic acid monomethyl ester

Target: Akt, PI3K

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