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43

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T4542	Clonixin Clonixic acid,氯尼辛	Others	Others
	Clonixin (Clonixic acid) 是一种非甾体抗炎药，具有口服活性。
T16240	N,N'-Diacetyl-L-cystine (Ac-Cys-OH)2,DiNAC	Others	Others
	N,N'-Diacetyl-L-cystine (DiNAC) 是一种具有免疫调节特性的 N-乙酰基半胱氨酸的二硫二聚体。它在高脂血症兔中也具有抗动脉粥样硬化的作用。它是啮齿类动物中接触敏感/迟发型超敏反应的有效口服活性调节剂。
T24121	GW438014A GW 438014 A,GW-438014-A	Neuropeptide Y Receptor	GPCR/G Protein; Neuroscience
	GW438014A 是一种有效且具有选择性的 NPY-Y5 受体拮抗剂。GW438014A 对食物摄入并减少肥胖啮齿动物的体重增加具有抑制作用。
T4351	DAMGO Dagol,DAGO,RX-783006	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	DAMGO (DAGO) 是一种阿片受体激动剂，Kd 值为 3.46 nM。它能够影响啮齿动物的运动活动，可作为镇痛剂。
T16816	S 18986	GluR	Neuroscience
	S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors, showcasing cognitive-enhancing properties in rodents. It induces the release of noradrenaline and acetylcholine in the rat hippocampus, leading to enhanced object-recognition memory.
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。
T60221	Tabernanthalog TBG	5-HT Receptor	GPCR/G Protein; Neuroscience
	Tabernanthalog (TBG) 是一种5-HT2A 激动剂。在啮齿类动物中，Tabernanthalog 已被发现可促进结构神经可塑性并产生抗抑郁作用。
T28531	Facinicline hydrochloride RG3487	5-HT Receptor; AChR	GPCR/G Protein; Neuroscience
	Facinicline hydrochloride (RG3487) 是一种口服有效的烟碱α7 receptor 部分激动剂，对人 nAChR 的 Ki 值为 6 nM。它可改善啮齿类动物的认知和感觉运动门控。它与5-HT3受体结合的 Ki 为 1.2 nM。
T8862	ML 254	GluR	Neuroscience
	是一种化学合成中的砌块
T21556	Hydroxytacrine maleate Velnacrine maleate,HP 029 maleate	AChE	Neuroscience
	Hydroxytacrine maleate (Velnacrine maleate) 是一种胆碱酯酶(cholinesterase) 抑制剂，可增强啮齿动物的记忆力，可用于研究阿尔茨海默型老年性痴呆（SDAT）。
T13318	VU0650786	GluR	Neuroscience
	VU0650786 是能透过中枢神经系统的，选择性谷氨酸受体亚型 3 的一种负变构调节剂，IC50值为 392 nM，有抗抑郁和抗焦虑活性。
T7720	CGP 37849 CGP-37849,CGP37849	NMDAR; iGluR	Membrane transporter/Ion channel; Neuroscience
	CGP 37849 是一种竞争性口服活性 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂（(Ki = 35 nM)），具有有效性。CGP 37849 是啮齿动物的抗惊厥药，也具有抗抑郁和抗焦虑的特性。
T25672	Lesopitron	5-HT Receptor	GPCR/G Protein; Neuroscience
	Lesopitron 是一种具有突触前和突触后5-HT1A 激动剂活性的抗焦虑剂，在大鼠社会交往和狨猴焦虑模型中比5-HT1A 激动剂更有效。Lesopitron 能对抗苯二氮卓类药物戒断引起的啮齿动物的焦虑且急性毒性很低，不会增强酒精或巴比妥类药物的作用。
T67955	Ensaculin Anseculin
	Ensaculin (Anseculin) 是一种用哌嗪部分取代的新型苯并吡喃酮，在正常和人工遗忘啮齿动物的被动和条件回避范式中显示出记忆增强作用。它在NMDA 毒性模型中表现出神经保护活性，在原代培养的大鼠脑细胞中表现出神经营养作用。Ensaculin 可用于治疗痴呆。
T8720	PRX-07034 hydrochloride PRX-07034	5-HT Receptor	GPCR/G Protein; Neuroscience
	PRX-07034 hydrochloride 是一种有效的高度选择性5-HT6受体拮抗剂，Ki 为 4-8 nM，IC50为 19 nM，可用于增强工作记忆和认知灵活性的研究。
TF0106	Cholesteryl Hemisuccinate Tris Salt	Apoptosis	Apoptosis
	Cholesteryl Hemisuccinate Tris Salt 是一种具有保肝和抗癌活性的酸性胆固醇酯，是一种含有柴胡皂苷-d的二棕榈酰磷脂酰胆碱脂质体中的膜稳定剂，可增强顺铂的抗癌功效。Cholesteryl hemisuccinate 具有抗肿瘤活性，抑制肿瘤生长，抑制对乙酰氨基酚 (AAP) 的肝毒性，预防 AAP 诱导的肝细胞凋亡。Cholesteryl hemisuccinate 可保护啮齿动物免受对乙酰氨基酚、阿霉素、四氯化碳、氯仿和半乳糖胺的毒性作用。
T27948	LY-368975 LY 368975,(R)-Thionisoxetine
	LY-368975 is a potent and selective inhibitor of the norepinephrine (NE) reuptake site. LY-368975 reduces food consumption in rodents.
T13371	YM-53601 free base	AMPK	Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
	YM-53601 free base is an inhibitor of squalene synthetase which suppresses lipogenic biosynthesis and lipid secretion in rodents.
T28926	TASP0390325 TASP-0390325,TASP 0390325
	TASP0390325, a potent and orally active V1B receptor antagonist, has antidepressant and anxiolytic activities in rodents.
T68676	Ciladopa (free base)
	Ciladopa (free base) is a dopamine agonist with a similar chemical structure to dopamine. It was under investigation as an antiparkinsonian agent but was discontinued due to concerns of tumorogenesis in rodents.
T29979	Amidantel hydrochloride BAY-d 8815,BAY d 8815
	Amidantel hydrochloride is a new aminophenylamidine with an interesting anthelminthic spectrum. In rodents the compound is active against nematodes, filariae and cestodes. Of special interest is the high efficacy in dogs against hookworms and large roundw
T74285	EDMPC
	EDMPC，一种阳离子脂质，有效递送DNA至肺组织，亦用于向啮齿动物叶内递送DNA。
T81626	Obestatin(11-23)mouse, rat
	Obestatin(11-23)mouse, rat 是多肽，涉及能量平衡调节，抑制摄食。该化合物能使啮齿类动物食量减少、体重降低、及空肠收缩。
T37416	Tauro-α-muricholic Acid (sodium salt)
	Tauro-α-muricholic acid (TαMCA) is an antagonist of the farnesoid X receptor (FXR; IC50 = 28 μM) and a taurine-conjugated form of the murine-specific primary bile acid α-muricholic acid . TαMCA is common in rodents but has also been found in small amounts in human serum.
T29979L	Amidantel free base BAYd 8815,BAY d8815,BAYd-8815,Amidantel,BAY d-8815,BAY d 8815
	Amidantel free base is a new aminophenylamidine with an interesting anthelminthic spectrum. In rodents the compound is active against nematodes, filariae and cestodes. Of special interest is the high efficacy in dogs against hookworms and large roundworms
T81336	PZ-1190	Dopamine Receptor	GPCR/G Protein; Neuroscience
	PZ-1190是一种多靶点配体，针对啮齿动物的serotonin和dopamine受体，展现出潜在的抗精神病活性。
T13691	Etifoxine HOE 36-801	Others	Others
	Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors. GABAA receptor Etifoxine exhibits anxiolytic activity in rodents and humans with no sedative, myorelaxant or mnesic side effects. Etifoxine acts as a ligand of the translocator protein (TSPO); promotes axonal regeneration. Etifoxine(HOE 36-801) is potentiator of GABAA receptor function in cultured neurons.
T62919	CDK9-IN-13
	CDK9-IN-13 是一种有效的、选择性的 CDK 抑制剂 (IC50<3 nM)。CDK9-IN-13 在啮齿动物中的半衰期很短。
T38959	BMS-604992 dihydrochloride EX-1314 dihydrochloride,BMS-604992 dihydrochloride
	BMS-604992 (EX-1314) dihydrochloride is a selective and orally active small-molecule agonist of the growth hormone secretagogue receptor (GHSR). It exhibits high-affinity binding (k i = 2.3 nM) and potent functional activity (EC 50 = 0.4 nM). Furthermore, BMS-604992 dihydrochloride has been shown to stimulate food intake in rodents.
T40876	BMS-604992 free base BMS-604992 free base,EX-1314 free base
	BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. It exhibits high-affinity binding (k i = 2.3 nM) and potent functional activity (EC 50 = 0.4 nM). Moreover, BMS-604992 free base has the ability to stimulate food intake in rodents.
T70718	CR-6086
	CR6086 is a novel, potent EP4 antagonist showing favourable immunomodulatory properties, striking DMARD effects in rodents, and anti-inflammatory activity targeted to immune-mediated inflammatory diseases and distinct from the general effects of cyclooxygenase inhibitors. CR6086 showed selectivity and high affinity for the human EP4 receptor (Ki = 16.6 nM) and functioned as a pure antagonist (half-maximal inhibitory concentration, 22 nM) on PGE2-stimulated cAMP production.
T27269	Ensaculin HCl KA 672,KA672,Ensaculin,Anseculin Hydrochloride,KA-672 HCl
	Ensaculin is a NMDA antagonist and a 5HT1A agonist potentially for the treatment of Alzheimer's disease (AD). Ensaculin showed memory-enhancing effects in paradigms of passive and conditioned avoidance in both normal and artificially amnesic rodents. It e
T78460	1-Methylpyrene
	1-Methylpyrene是一种环境污染物和已知的啮齿动物致癌物，它的诱变活性依赖于CYP和磺酰转移酶（SULT）系列酶的连续活化。该化合物可诱导染色体缺失和有丝分裂障碍，可能机制为对有丝分裂纺锤体和中心粒的干扰。
T62848	AMG 837 hemicalcium
	AMG 837 hemicalcium 是一种有效的、口服具有活力的 GPR40/FFA1部分激动剂。AMG 837 hemicalcium 能够抑制 [3H]AMG 837 与人类 FFA1受体的特异性结合 (pIC50: 8.13)。AMG 837 hemicalcium 能够提高啮齿动物的胰岛素分泌，减少葡萄糖水平。
T76655	Prokineticin 2 Isoform 2 (human)
	Prokineticin 2 Isoform 2 (human) 为一下丘脑神经肽，能减少食物摄入，并在啮齿动物的体温调节与能量代谢中发挥作用。此外，Prokineticin 2 对高血糖、代谢综合征 (MetS) 及肥胖研究具有潜在价值。
T14215	AMG 837 sodium salt	Others	Others
	AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. IC50 value: 13 nM (EC50) [1] Target: GPR40 agonist AMG 837 displayed the expected t
T28685	SB236057 SB-236057,SB 236057
	SB236057 is a potent and selective inverse agonist for the 5-HT receptor, acting especially at 5-HT autoreceptors on nerve terminals. It produces a rapid increase in 5-HT levels in the brain. SB236057 also acts as a potent teratogen, producing severe musc
T80287	KLTWQELYQLKYKGI	VEGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	KLTWQELYQLKYKGI (QK) 是一种与VEGF受体结合并同VEGF竞争的VEGF模拟肽。在口服或全身给药时，该化合物对啮齿类动物胃溃疡的愈合展现了活性。此外，KLTWQELYQLKYKGI 在体外具有诱导毛细血管形成和组织的能力。
T79475	GPR119 agonist 2
	GPR119 agonist2（化合物43）是一种口服活性的GPR119激动剂。在啮齿动物中表现出优良的药代动力学特性，并能有效提高小鼠和大鼠的葡萄糖耐受性。GPR119 agonist2有望用于研究II型糖尿病。
T17231	Vicagrel	Others	Others
	Vicagrel 是一种有效的、具有口服活性抗血小板化合物，通过不可逆地抑制 P2Y12 受体，降低代谢失活，增强了阿司匹林对啮齿类动物血小板聚集和血栓形成起抑制作用。Viagrel 可用于治疗冠状动脉疾病、外周血管疾病和脑血管疾病中血栓。
T14216	AMG 837	Others	Others
	AMG 837 was found to be a partial agonist on GPR40 with maximal activity 85% of that shown by DHA under our standard assay conditions. Overall, AMG 837 was both highly potent and selective in vitro. AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a sup
T36618	Rupatadine
	Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in hu...
T35560	SAR502250
	SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD)[1][2]. SAR502250 (0.01-1 μM; 36 h) attenuates the Aβ25-35-induced cell death in rat embryonic hippocampal neurons[2]. SAR502250 (1-100 mg/kg; a single p.o,) attenuates tau hyperphosphorylation in the cortex and spinal cord of transgenic mic...

化合物

Cat.No: T4542

Synonym: Clonixic acid,氯尼辛

Target: Others

N,N'-Diacetyl-L-cystine

Cat.No: T16240

Synonym: (Ac-Cys-OH)2,DiNAC

Target: Others

Cat.No: T24121

Synonym: GW 438014 A,GW-438014-A

Target: Neuropeptide Y Receptor

Cat.No: T4351

Synonym: Dagol,DAGO,RX-783006

Target: Opioid Receptor

Cat.No: T16816

Target: GluR

Cat.No: T21380

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

Target: Cannabinoid Receptor

Cat.No: T60221

Synonym: TBG

Target: 5-HT Receptor

Facinicline hydrochloride

Cat.No: T28531

Synonym: RG3487

Target: 5-HT Receptor, AChR

Cat.No: T8862

Target: GluR

Hydroxytacrine maleate

Cat.No: T21556

Synonym: Velnacrine maleate,HP 029 maleate

Target: AChE

Cat.No: T13318

Target: GluR

Cat.No: T7720

Synonym: CGP-37849,CGP37849

Target: NMDAR, iGluR

Cat.No: T25672

Target: 5-HT Receptor

Cat.No: T67955

Synonym: Anseculin

PRX-07034 hydrochloride

Cat.No: T8720

Synonym: PRX-07034

Target: 5-HT Receptor

Cholesteryl Hemisuccinate Tris Salt

Cat.No: TF0106

Target: Apoptosis

Cat.No: T27948

Synonym: LY 368975,(R)-Thionisoxetine

YM-53601 free base

Cat.No: T13371

Target: AMPK

Cat.No: T28926

Synonym: TASP-0390325,TASP 0390325

Ciladopa (free base)

Cat.No: T68676

Amidantel hydrochloride

Cat.No: T29979

Synonym: BAY-d 8815,BAY d 8815

Cat.No: T74285

Obestatin(11-23)mouse, rat

Cat.No: T81626

Tauro-α-muricholic Acid (sodium salt)

Cat.No: T37416

Amidantel free base

Cat.No: T29979L

Synonym: BAYd 8815,BAY d8815,BAYd-8815,Amidantel,BAY d-8815,BAY d 8815

Cat.No: T81336

Target: Dopamine Receptor

Cat.No: T13691

Synonym: HOE 36-801

Target: Others

Cat.No: T62919

BMS-604992 dihydrochloride

Cat.No: T38959

Synonym: EX-1314 dihydrochloride,BMS-604992 dihydrochloride

BMS-604992 free base

Cat.No: T40876

Synonym: BMS-604992 free base,EX-1314 free base

Cat.No: T70718

Cat.No: T27269

Synonym: KA 672,KA672,Ensaculin,Anseculin Hydrochloride,KA-672 HCl

Cat.No: T78460

AMG 837 hemicalcium

Cat.No: T62848

Prokineticin 2 Isoform 2 (human)

Cat.No: T76655

AMG 837 sodium salt

Cat.No: T14215

Target: Others

Cat.No: T28685

Synonym: SB-236057,SB 236057

KLTWQELYQLKYKGI

Cat.No: T80287

Target: VEGFR

GPR119 agonist 2

Cat.No: T79475

Cat.No: T17231

Target: Others

Cat.No: T14216

Target: Others

Cat.No: T36618

Cat.No: T35560

Cat. No.	Product Name	Target	Signaling Pathways
T5573	Coenzyme Q9 辅酶Q9,Ubiquinone Q9,Ubiquinone 9,CoQ9	Apoptosis; Endogenous Metabolite	Apoptosis; Metabolism
	Coenzyme Q9 (Ubiquinone 9) 是啮齿类动物泛醌的主要形式，是电子传递链中的一种双亲分子组分，具有内源性抗氧化剂的作用。它可减轻糖尿病引起的抗氧化防御机制的下降，改善左心室功能，减少心肌梗死面积和心肌细胞凋亡。
T8141	L-Cysteine hydrochloride L-Cysteine HCl,L-半胱氨酸盐酸盐,L-半胱氨酸盐酸盐(无水物)	Others; Endogenous Metabolite	Metabolism; Others
	L-Cysteine hydrochloride (L-Cysteine HCl) 是一种条件必需氨基酸，是硫化氢 (H2S)、牛磺酸谷胱甘肽和等生物特性分子的前体。它能抑制胃饥饿素，抑制啮齿动物和人类的食欲。
TN5283	L-Cysteine hydrochloride hydrate L-Cysteine hydrochloride monohydrate,L-半胱氨酸盐酸盐一水物,L-半胱氨酸盐酸盐一水合物	Others; Endogenous Metabolite	Metabolism; Others
	L-Cysteine hydrochloride hydrate (L-Cysteine hydrochloride monohydrate) 是条件必需氨基酸，是硫化氢、谷胱甘肽和牛磺酸等生物活性分子的前体。它可以抑制胃饥饿素，抑制啮齿动物和人类的食欲。
T19623	α-Muricholic acid	AChR	Neuroscience
	α-Muricholic acid is the most abundant primary bile acid in rodents.
T40584	Corymbiferin
	Corymbiferin, a chemical compound, exhibits significant anti-diabetic properties by enhancing antioxidant capacity and carbohydrate metabolism in diabetic rodents. In addition, Corymbiferin promotes the improvement of histopathology in both the liver and pancreatic β cells.
T1208	Citicoline sodium Citicoline sodium salt,CDP-choline,胞磷胆碱钠	Apoptosis; Others; Endogenous Metabolite	Apoptosis; Metabolism; Others
	Citicoline sodium (CDP-choline) 是一种合成细胞膜组分磷脂酰胆碱的中间体，有神经保护作用。
T36563	(E)-Guggulsterone
	Bile acids are essential for solubilization and transport of dietary lipids, are the major products of cholesterol catabolism, and are physiological ligands for farnesoid X receptor (FXR), a nuclear receptor that regulates genes involved in lipid metabolism.1They are also inherently cytotoxic, as physiological imbalance contributes to increased oxidative stress.2,3Bile acid-controlled signaling pathways are promising novel targets to treat such metabolic diseases as obesity, type II diabetes, hy...

天然产物

Cat.No: T5573

Synonym: 辅酶Q9,Ubiquinone Q9,Ubiquinone 9,CoQ9

Target: Apoptosis, Endogenous Metabolite

L-Cysteine hydrochloride

Cat.No: T8141

Synonym: L-Cysteine HCl,L-半胱氨酸盐酸盐,L-半胱氨酸盐酸盐(无水物)

Target: Others, Endogenous Metabolite

L-Cysteine hydrochloride hydrate

Cat.No: TN5283

Synonym: L-Cysteine hydrochloride monohydrate,L-半胱氨酸盐酸盐一水物,L-半胱氨酸盐酸盐一水合物

Target: Others, Endogenous Metabolite

α-Muricholic acid

Cat.No: T19623

Target: AChR

Cat.No: T40584

Citicoline sodium

Cat.No: T1208

Synonym: Citicoline sodium salt,CDP-choline,胞磷胆碱钠

Target: Apoptosis, Others, Endogenous Metabolite

(E)-Guggulsterone

Cat.No: T36563

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