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22

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T14767	BP 897 hydrochloride	Dopamine Receptor	GPCR/G Protein; Neuroscience
	BP 897 hydrochloride 是有效的部分多巴胺 D3受体激动剂和弱 D2受体拮抗剂，在多巴胺 D3 受体 (Ki=0.92 nM) 上显示出高亲和力，而在 D2 受体上显示出 70 倍的低亲和力 (Ki=61 nM)。它表现出对可卡因寻求行为的选择性抑制。
T9100	BP 897 2-Naphthalenecarboxamide, N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-	Dopamine Receptor	GPCR/G Protein; Neuroscience
	BP 897 (2-Naphthalenecarboxamide, N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-) 是一种有效的部分多巴胺D3受体激动剂和弱D2受体拮抗剂，在多巴胺 D3 受体(Ki=0.92 nM) 上显示出高亲和力，而在 D2 受体上显示出 70 倍的低亲和力 (Ki=61 nM)。它表现出对可卡因寻求行为的选择性抑制。
T21380	Pravadoline WIN 48098-6,WIN48098-6,普拉朵林,WIN-48098-6	Cannabinoid Receptor	GPCR/G Protein
	Pravadoline (WIN48098-6) 是一种 cannabinoid 受体激动剂。 Pravadoline 抑制小鼠大脑中的 PGs 合成，并在受到各种热、化学和机械伤害性刺激的啮齿动物中显示出镇痛活性。
T29968	AMG-0347 UNII-CD7L9290QR	TRP/TRPV Channel	Membrane transporter/Ion channel
	AMG-0347 (UNII-CD7L9290QR)是一种靶向TRPA1(瞬时受体电位锚蛋白1)离子通道的小分子抑制剂，是一种在感觉神经元中发现的受体，参与疼痛和环境刺激物的检测。AMG-0347通过阻断TRPA1的功能起作用，具有镇痛作用。
T36310	AKT-IN-6 INCB-047775	Akt	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	AKT-IN-6 (INCB-047775)对ATK 有抑制作用。Akt 是对生长因子、细胞因子和其他细胞刺激的细胞信号传导的重要组成部分。Akt 的异常激活与2型糖尿病和癌症的发生密切相关。
T1627	Famotidine MK-208,法莫替丁	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Famotidine (MK-208) 是一种具有抗酸活性的丙脒和组胺 H2 受体拮抗剂。
T14198	ALX-1393	GlyT	Neuroscience
	ALX-1393 是一种选择性 GlyT2 抑制剂，通过浓度依赖性的方式有效地降低了神经元动作电位的活性，抑制自发网络通过在脊髓腹角诱导甘氨酸能强直电流的活动。对大鼠急性疼痛模型中的热，机械和化学刺激具有抗伤害作用。
T35105	Way 100252 Way-100252,Way100252
	Way 100252 inhibits evoked [3H]GABA release when tested against a number of release-inducing stimuli.
T35082	VU6010608 VU-6010608,VU 6010608
	VU6010608 is an effective mGlu7 NAM with excellent CNS permeability and is powerful in electrophysiological studies in blocking long-term enhancement of high-frequency stimuli.
TP1608	PTD-p65-P1 Peptide
	PTD-p65-P1 Peptide, a selective inhibitor of the nuclear transcription factor NF-kappaB, consists of a conjugation between a membrane-translocating peptide derived from antennapedia (PTD) and p65-P1. This composition effectively inhibits activation triggered by diverse inflammatory stimuli.
TP1395	PTD-p65-P1 Peptide TFA
	Ptd-p65-p1 Peptide TFA is a nuclear transcription factor nf-kappab inhibitor, consisting of a membrane transport Peptide sequence derived from antennapedia linked to p65-p1, selectively inhibiting nf-kappab activity induced by various stimuli.
T26807	Bifeprunox Mesylate Bifeprunox,DU 127090,DU-127090,DU127090
	Bifeprunox is a partial dopamine and serotonin agonist potentially for the treatment of schizophrenia. Bifeprunox suppresses in vivo VTA dopaminergic neuronal activity via D2 and not D3 dopamine autoreceptor activation. Bifeprunox influences nicotine-seek
T70581	CY208-243 Mandelate
	CY208-243 is a D1 agonist. CY208-243 attenuates the pattern electroretinogram to low spatial frequency stimuli in the monkey. CY208-243 stimulates adenylate cyclase in rat striatal homogenates with an EC50 of 125 nM. CY208,243 was superior in improving the strength of neuronal outcome sensitivity to the working memory-related choice behavior in the T-maze.
TP2176	amyloid A protein fragment [Homo sapiens]	Others	Others
	Amyloid A proteins (H2N-Ala-Gly-Leu-Pro-Glu-Lys-Tyr-OH) are a family of apolipoproteins associated with high-density lipoprotein in plasma. Different isoforms of SAA are expressed constitutively at different levels or in response to inflammatory stimuli.
T67212	Ligustrazine HCl
	Ligustrazine Hydrochloride, is a natural substance discovered in the plant Ligusticum chuanxiong Hort. It inhibits platelet aggregation, improves atherosclerosis situation, protects endothelium injury, and has antithrombotic effects.in vivo,ligustrazine hydrochloride at 10 and 20 mg/kg produced significant analgesic effects against mechanical stimuli,and ligustrazine hydrochloride at 80 mg/kg, also significantly alleviated cold hypersensitivity manifested by reduction in cold vocalization temper...
T74779	JNJ-28583113
	JNJ-28583113 是一种具有脑透性的 TRPM2拮抗剂。JNJ-28583113 抑制 TRPM2 阻断 GSK3α和β亚基的磷酸化。JNJ-28583113 保护细胞免受氧化应激诱导的细胞死亡。JNJ-28583113 还抑制小胶质细胞响应促炎刺激而释放细胞因子。
T36838	(R)-Bromoenol lactone
	The phospholipases are an extensive family of lipid hydrolases that function in cell signaling, digestion, membrane remodeling, and as venom components. The calcium-independent phospholipases (iPLA2) are a PLA2 subfamily closely associated with the release of arachidonic acid in response to physiologic stimuli. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). Unlike (S)-BEL, (R)-BEL does not inhibit iPLA2β exce...
T82771	CB2-H
	CB2-H为一种高特异性双通道荧光探针，专门设计用于HOCl和ONOO-的同时检测。该探针在两个分离的通道中对HOCl和ONOO-无交叉干扰的检测能力使其适用于对活细胞和斑马鱼样本内HOCl及ONOO-的内源性水平进行双通道荧光成像分析，即使在不同生物刺激下也能保持准确性。
T79556	NDBM	Autophagy	Autophagy
	NDBM为一种结合Pim-1 kinase的肿瘤特异性探针，具备释放强荧光及细胞毒性，用于筛选及杀伤肿瘤细胞。该化合物特异性地靶向溶酶体并对pH值具有高度敏感性，适用于监测自噬(autophagy)过程及细胞内环境在外部刺激下的pH变化。
T21750	A 784168
	A-784168 是一种有效的、口服活性的香草素受体 1 型 (TRPV1) 抑制剂。香草素受体 1 型 (TRPV1) 是一种配体门控非选择性阳离子通道，被认为是各种疼痛刺激 (如内源性脂质、辣椒素、热和低 pH 值) 的重要整合剂。口服给药时，A-784168 具有良好的 CNS 渗透性。
T83749	Tertiapin LQ TFA TPNLQ
	Tertiapin LQ是源自蜜蜂毒素肽tertiapin的肽衍生物，同时也是向内整流钾(Kir)通道的抑制剂。它能够抑制由G蛋白激活的向内整流钾通道1（GIRK1）和GIRK4（即Kir3.1和Kir3.4）组成的异源多聚钾通道，以及向内整流钾通道1（Kir1.1）。在活体内，tertiapin LQ抑制在雪貂中对条件刺激的Purkinje细胞暂停响应。
T38193	β-Endorphin (1-27) (human) (trifluoroacetate salt)
	β-Endorphin (1-27) is an endogenous peptide that binds to μ-, δ-, and κ-opioid receptors (Kis = 5.31, 6.17, and 39.82 nM, respectively, in COS-1 cells expressing rat receptors). It binds to rat and mouse brain membrane preparations (IC50s = 1.1 and 5.7 nM, respectively) and induces chemotaxis of human monocytes in vitro when used at a concentration of 1 nM. Intracerebroventricular administration of β-endorphin (1-27) increases the latency to tail withdrawal in response to thermal stimulation in ...

化合物

BP 897 hydrochloride

Cat.No: T14767

Target: Dopamine Receptor

Cat.No: T9100

Synonym: 2-Naphthalenecarboxamide, N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-

Target: Dopamine Receptor

Cat.No: T21380

Synonym: WIN 48098-6,WIN48098-6,普拉朵林,WIN-48098-6

Target: Cannabinoid Receptor

Cat.No: T29968

Synonym: UNII-CD7L9290QR

Target: TRP/TRPV Channel

Cat.No: T36310

Synonym: INCB-047775

Target: Akt

Cat.No: T1627

Synonym: MK-208,法莫替丁

Target: Histamine Receptor

Cat.No: T14198

Target: GlyT

Cat.No: T35105

Synonym: Way-100252,Way100252

Cat.No: T35082

Synonym: VU-6010608,VU 6010608

PTD-p65-P1 Peptide

Cat.No: TP1608

PTD-p65-P1 Peptide TFA

Cat.No: TP1395

Bifeprunox Mesylate

Cat.No: T26807

Synonym: Bifeprunox,DU 127090,DU-127090,DU127090

CY208-243 Mandelate

Cat.No: T70581

amyloid A protein fragment [Homo sapiens]

Cat.No: TP2176

Target: Others

Ligustrazine HCl

Cat.No: T67212

Cat.No: T74779

(R)-Bromoenol lactone

Cat.No: T36838

Cat.No: T82771

Cat.No: T79556

Target: Autophagy

Cat.No: T21750

Tertiapin LQ TFA

Cat.No: T83749

Synonym: TPNLQ

β-Endorphin (1-27) (human) (trifluoroacetate salt)

Cat.No: T38193

Cat. No.	Product Name	Target	Signaling Pathways
T2P2870	Damascenone trans-damascenone,Beta-Damascenone,大马烯酮,大马酮	Others; NF-κB; Endogenous Metabolite	Metabolism; NF-κB; Others
	Damascenone (trans-damascenone) 是一种 E-和 Z-异构体大马士革酮的混合物，源于 Epipremnum pinnatum 的具有抗炎特性的特性化合物。
TN3460	Asebogenin	Antifungal	Microbiology/Virology
	Asebogenin 是从丹参中分离出来的化合物，具有抗真菌活性，对GPVI 诱导的血小板反应有抑制作用，抑制促炎刺激诱导的 NET 形成。
TN5131	Tetrahydrocannabivarin THCV,delta9-Tetrahydrocannabivarin,CRM,Tetrahydrocannavarin	Cannabinoid Receptor	GPCR/G Protein
	Tetrahydrocannabivarin (CRM) 是 cannabinoid type 1 receptor 的中性拮抗剂，对 2 型糖尿病有潜在治疗价值。
T32614	L-Clausenamide (-)-Clausenamide	Microtubule Associated	Cytoskeletal Signaling
	L-Clausenamide 是从黄皮 (Clausena lansium (Lour) skeels) 的树叶中提取出来的生物碱，可用于提高认知功能。L-Clausenamide 对β-淀粉样蛋白 (Aβ) 毒性有抑制作用，通过抑制 tau 蛋白磷酸化阻止神经纤维缠结的形成。L-Clausenamide 具有神经保护活性，可用于调节 Aβ25-35 引发的刺激。L-Clausenamide 可用于研究阿尔兹海默症类的神经系统疾病。
T10109	3-Carene Delta-3-Carene	COX; Antifungal	Immunology/Inflammation; Microbiology/Virology; Neuroscience
	3-Carene（Delta-3-Carene）是西部落叶松和花旗松中提取的双环单萜烯，可做为植物杀菌剂。3-Carene 对痛觉刺激引起的炎症浸润和 COX-2 过表达有抑制作用。3-Carene 具有抗伤害作用，能促进成骨细胞分化的早期标志物碱性磷酸酶的活性和表达。

天然产物

Cat.No: T2P2870

Synonym: trans-damascenone,Beta-Damascenone,大马烯酮,大马酮

Target: Others, NF-κB, Endogenous Metabolite

Cat.No: TN3460

Target: Antifungal

Tetrahydrocannabivarin

Cat.No: TN5131

Synonym: THCV,delta9-Tetrahydrocannabivarin,CRM,Tetrahydrocannavarin

Target: Cannabinoid Receptor

Cat.No: T32614

Synonym: (-)-Clausenamide

Target: Microtubule Associated

Cat.No: T10109

Synonym: Delta-3-Carene

Target: COX, Antifungal

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