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19

抑制剂 & 化合物

9

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
TP2069	BDNF (human)
	Member of the neurotrophin growth factor family that binds and activates TrkB and p75 neurotrophin receptors. Enhances the survival, growth and differentiation of neurons. BDNF expression is altered in neurodegenerative disorders such as Parkinson's and A
T8779	HBT1	GluR	Neuroscience
	HBT1 是一种 AMPA 受体增强剂，可诱导脑源性神经营养因子 (BDNF) 的产生，并且在原代神经元中几乎没有激动作用。 HBT1 以谷氨酸依赖的方式与 AMPA-R 的配体结合结构域结合。
T4646	TA-02	p38 MAPK; Autophagy	Autophagy; MAPK
	TA02 是一种Adezmapimod 类似物，是p38 MAPK 的抑制剂，其IC50值为 20 nM。它和Adezmapimod、SB 202190 具有相似的心源活性，可抑制 TGFBR-2。
TP2068L	Cyclotraxin B acetate(1203586-72-4 free base)	Trk receptor	Tyrosine Kinase/Adaptors
	Cyclotraxin B acetate(1203586-72-4 free base) 是 TrkB 受体的拮抗剂；抑制 BDNF 诱导的 TrkB 活性 (IC50 = 0.30 nM)。变构改变 TrkB 受体构象但不改变 BDNF 结合。防止 BDNF 引起的小鼠冷异常性疼痛。还显示在小鼠中表现出推定的抗焦虑特性。
T72063	PDCD4-IN-1
	PDCD4-IN-1是一种 PDCD4抑制剂（Kd ：350 nM），可促进海马神经元细胞 HT-22 中 BDNF 表达。
T7568	LM22A-4	Trk receptor	Tyrosine Kinase/Adaptors
	LM22A-4 是特异性的tyrosine kinase receptor B 激动剂，常用于研究神经系统疾病。
T4093	Fabomotizole hydrochloride Afobazole hydrochloride,CM346 hydrochloride	MAO	Metabolism; Neuroscience
	Fabomotizole hydrochloride (CM346 hydrochloride) 是一种具有抗焦虑和神经保护作用的化合物。
T25500	HHL-6
	HHL-6 is a c-Fos and BDNF protein expression modulator.
TP2068	Cyclotraxin B
	Antagonist of TrkB receptors; inhibits BDNF-induced TrkB activity (IC50 = 0.30 nM). Allosterically alters TrkB receptor conformation but does not alter BDNF binding. Prevents BDNF-induced cold allodynia in mice. Also shown to exhibit putative anxiolytic p
T75832	Cyclotraxin B TFA
	Cyclotraxin B TFA 是一种环肽，是一种高效且选择性的 TrkB 抑制剂，且不会改变 BDNF 的结合。Cyclotraxin B TFA 非竞争性地抑制 BDNF 诱导的 TrkB 活性，IC50值为 0.30 nM。Cyclotraxin B TFA 可以穿越血脑屏障，并具有止痛和抗焦虑的行为作用。
T68403	AZD-6918
	AZD6918 is a novel potent and selective inhibitor of the Trk tyrosine kinases. AZD-6918 attenuates the BDNF/TrkB-induced protection of neuroblastoma cells from etoposide in vitro and in vivo. AZD6918 inhibited wild-type TrkB-induced cell migration and cell growth.
T71827	AG-205
	(rac)-AG-205 是一种对孕激素受体膜组分1 (Pgrmc1) 的有效抑制剂，并能诱导参与甾醇合成的基因表达，这些基因涉及 INSIG1 蛋白与 PGRMC1 形成复合物的过程。(rac)-AG-205 能够抑制 NF-kB 信号及 BDNF/PI3K/AKT 通路的活化，从而防止神经元对缺氧缺血状况的抵抗。
T70818	TC-2153
	TC-2153 是纹状体富集蛋白酪氨酸磷酸酶 (STEP) 的选择性抑制剂，具有精神活性和低急性毒性。TC-2153 增加脑源性神经营养因子 (BDNF) 在大脑中的表达。它还降低MAOA 和5-HT1A receptor 受体的 mRNA 水平。TC-2153 也抑制5-HT2A 受体介导的信号传递。
T73658	Orexin A (human, rat, mouse) (acetate)
	Orexin A (Hypocretin-1) (human, rat, mouse) acetate 是一种具有镇痛特性的下丘脑神经肽 (可透过血脑屏障)。Orexin A (human, rat, mouse) acetate 也是一种OX1R 激动剂，能以时间和剂量依赖性的方式诱导 SH-SY5Y 细胞BDNF 和TH 蛋白的表达。Orexin A (human, rat, mouse) acetate 可用于食欲调节、神经退行性疾病，以及调节伤害性信息传递的研究。
T62561	TRK-IN-17
	TRK-IN-17 是一种 TRK 的有效抑制剂。其中原肌球蛋白相关激酶 (Trks) 是受体酪氨酸激酶家族成员，由神经营养因子激活。神经营养因子是一组可溶性生长因子，包括神经生长因子 (NGF)、脑源性神经营养因子 (BDNF) 和神经营养因子-3 (NT-3)，以及神经营养因子-4/5 (NT-4/5)。TRK-IN-17 具有潜力进行癌症疾病的研究。
T61617	Hcyb1
	Hcyb1 is a potent and specific inhibitor of phosphodiesterase 2 (PDE2). It exhibits a high degree of selectivity for inhibiting PDE2A with an IC50 value of 0.57 μM. In addition, Hcyb1 displays over 250-fold selectivity against other recombinant members of the PDE family. Moreover, its pharmacological actions include neuroprotective and antidepressant-like effects, which are believed to be mediated through the cAMP/cGMP-CREB-BDNF signaling pathway [1].
T37167	Reduced Haloperidol
	Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (Kis = 21, 25, and 33 μM, respectively, in COS-7 cells expressing ...
T70073	Fabomotizole dihydrochloride
	Fabomotizole, also known as Afobazole, Obenoxazine and CM346, is an anxiolytic drug launched in Russia in the early 2000s. It produces anxiolytic and neuroprotective effects without any sedative or muscle relaxant actions. Its mechanism of action remains poorly defined however, with GABAergic, NGF- and BDNF-release-promoting, MT1 receptor agonism, MT3 receptor antagonism, and sigma agonism suggested as potential mechanisms. Fabomotizole was shown to inhibit MAO-A reversibly and there might be al...
T63346	TRK-IN-18
	TRK-IN-18 是 TRK 的有效抑制剂。其中原肌球蛋白相关激酶 (Trks) 是一种受体酪氨酸激酶家族，由神经营养因子激活，神经营养因子是一组可溶性生长因子，包含神经生长因子 (NGF)、脑源性神经营养因子 (BDNF) 和神经营养因子-3 (NT-3)，以及神经营养因子-4/5 (NT-4/5)。TRK-IN-18 表现出对癌症疾病的研究潜力。

化合物

Cat.No: TP2069

Cat.No: T8779

Target: GluR

Cat.No: T4646

Target: p38 MAPK, Autophagy

Cyclotraxin B acetate(1203586-72-4 free base)

Cat.No: TP2068L

Target: Trk receptor

Cat.No: T72063

Cat.No: T7568

Target: Trk receptor

Fabomotizole hydrochloride

Cat.No: T4093

Synonym: Afobazole hydrochloride,CM346 hydrochloride

Target: MAO

Cat.No: T25500

Cat.No: TP2068

Cyclotraxin B TFA

Cat.No: T75832

Cat.No: T68403

Cat.No: T71827

Cat.No: T70818

Orexin A (human, rat, mouse) (acetate)

Cat.No: T73658

Cat.No: T62561

Cat.No: T61617

Reduced Haloperidol

Cat.No: T37167

Fabomotizole dihydrochloride

Cat.No: T70073

Cat.No: T63346

Cat. No.	Product Name	Target	Signaling Pathways
TN2100	Pratensein 红车轴草素,三叶草	Others; NF-κB	NF-κB; Others
	Pratensein 是黄酮类化合物，能够减少氧化损伤和恢复突触和 BDNF 水平，改善 β-淀粉样蛋白诱导的大鼠认知障碍。
T0948L	Corticosterone 皮质酮,17-Deoxycortisol,11β,21-Dihydroxyprogesterone,Kendall's compound B,肾上腺酮,Corticosterone (From plants)	Glucocorticoid Receptor; Endogenous Metabolite	Endocrinology/Hormones; Metabolism
	Corticosterone (Kendall's compound B) 是一种肾上腺皮质类固醇，有盐皮质激素和糖皮质激素的活性，具有口服活性。Corticosterone 参与体内能量、免疫反应和应激反应的调节。
T4779	4-Methylcatechol p-Methylcatechol,3,4-二羟基甲苯,Homocatechol,4-methylbenzene-1,2-diol,3,4-Dihydroxytoluene	Others; Endogenous Metabolite	Metabolism; Others
	4-Methylcatechol (3,4-Dihydroxytoluene) 是 p-toluate 的代谢物，它是 Catechol 2,3-Dioxygenase 的自杀性底物抑制剂。
TN1236	3',4',7-Trihydroxyisoflavone	MAPK; JNK	MAPK
	3',4',7-Trihydroxyisoflavone 是大豆异黄酮大豆苷元衍生物，是 Cot (Tpl2/MAP3K8) 和 MKK4 抑制剂，具有抗癌、抗血管生成和自由基清除特性。3',4',7-Trihydroxyisoflavone 通过调节小鼠胆碱能功能和BDNF信号通路增强记忆作用，可改善因内源性或外源性糖皮质激素而受损的皮肤屏障功能，可用于研究特应性皮炎。
TN1015	Meranzin	Adrenergic Receptor; Immunology/Inflammation related	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Meranzin 是从传统中药 Chaihu-Shugan-San (CSS) 中的生物活性化合物，是从紫茉莉叶中分离出的，能够调节共有的 α2-肾上腺素受体，并参与 AMPA-ERK1/2-BDNF 信号传导。它有潜在的预防动脉粥样硬化和抑郁症合并症。
T5S0890	Oleandrin Neriostene,Folinerin,Foliandrin,欧夹竹桃苷	Apoptosis; ATPase; Potassium Channel; Sodium Channel	Apoptosis; Membrane transporter/Ion channel
	Oleandrin (Folinerin) 是夹竹桃属中的一种类固醇，可抑制Na+/K+-ATPase 活性，IC50为 620 nM。
TN1922	Meranzin hydrate	ERK; Adrenergic Receptor	GPCR/G Protein; MAPK; Neuroscience
	Meranzin hydrate 是来源于中药柴胡疏肝散中的吸收的生物活性化合物，表现出抗抑郁和抗动脉粥样硬化活性。
T3779	Crocin II Crocin 2,西红花苷II,Crocetin gentiobiosylglucosyl ester,藏红花,Tricrocin,Crocin B	Caspase; COX; NO Synthase	Apoptosis; Immunology/Inflammation; Neuroscience; Proteases/Proteasome
	Crocin II (Crocetin gentiobiosylglucosyl ester) 是从栀子果实中分离出来的一种天然产物，具有抗氧化、抗癌和抗抑郁活性。它抑制 iNOS 和 COX-2的蛋白质和 m-RNA 的表达，还抑制NO 产生，IC50值为 31.1 μM。
T81072	Suffruticosol A
	Suffruticosol A是一种从P. lactiflora种子中分离得到的神经保护剂，能够逆转由Scopolamine诱导的细胞神经退行性损伤。该化合物还能改善海马体胆碱能缺陷并部分增强BDNF信号传导，从而在Scopolamine诱导模型中显示出改善神经功能的作用，可恢复小鼠记忆与认知行为。

天然产物

Cat.No: TN2100

Synonym: 红车轴草素,三叶草

Target: Others, NF-κB

Cat.No: T0948L

Synonym: 皮质酮,17-Deoxycortisol,11β,21-Dihydroxyprogesterone,Kendall's compound B,肾上腺酮,Corticosterone (From plants)

Target: Glucocorticoid Receptor, Endogenous Metabolite

4-Methylcatechol

Cat.No: T4779

Synonym: p-Methylcatechol,3,4-二羟基甲苯,Homocatechol,4-methylbenzene-1,2-diol,3,4-Dihydroxytoluene

Target: Others, Endogenous Metabolite

3',4',7-Trihydroxyisoflavone

Cat.No: TN1236

Target: MAPK, JNK

Cat.No: TN1015

Target: Adrenergic Receptor, Immunology/Inflammation related

Cat.No: T5S0890

Synonym: Neriostene,Folinerin,Foliandrin,欧夹竹桃苷

Target: Apoptosis, ATPase, Potassium Channel, Sodium Channel

Meranzin hydrate

Cat.No: TN1922

Target: ERK, Adrenergic Receptor

Cat.No: T3779

Synonym: Crocin 2,西红花苷II,Crocetin gentiobiosylglucosyl ester,藏红花,Tricrocin,Crocin B

Target: Caspase, COX, NO Synthase

Suffruticosol A

Cat.No: T81072

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