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38

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T11995	Melatonin-d4 N-Acetyl-5-methoxytryptamine D5,Melatonin D5,褪黑素 D5	Others	Others
	Melatonin D5, a deuterium-labeled version of melatonin, is a hormone produced by the pineal gland, known for its role as a selective ATF-6 inhibitor that promotes apoptosis in human hepatoma cells via COX-2 downregulation. Additionally, it activates melatonin receptors and exhibits antioxidative and anti-inflammatory properties.
T64745	Melatonin Biotin
	Melatonin Biotin 是一种有用的有机化合物，可用于生命科学领域的相关研究，其产品编号为 T64745。
T60490	Melatonin receptor agonist 1
	Melatonin receptor agonist 1 (compound 20c) 是褪黑激素受体 (MT) 的有效激动剂，对MT2的Ki 值为 108 nM，对MT1的Ki 值为 1140 nM。
T14042	4-P-PDOT 4-phenyl-2- propionamidotetralin	Melatonin Receptor; MT Receptor	GPCR/G Protein; Neuroscience
	4-P-PDOT (4-phenyl-2- propionamidotetralin) 是一种选择性和亲和性的褪黑激素受体拮抗剂，可显著抵消褪黑激素介导的抗氧化作用。它对MT2的选择性是 MT1 的 300 倍以上。
T8600	N-ACETYLTRYPTAMINE	Melatonin Receptor	GPCR/G Protein
	N-Acetyltryptamine 是视网膜褪黑素受体的部分激动剂，可用于 5-羟色胺 N-乙酰转移酶活性的检测。
T9193	ACH-000143	Melatonin Receptor; MT Receptor	GPCR/G Protein; Neuroscience
	ACH-000143 是一种可口服的褪黑素受体激动剂，对 MT1 和 MT2 的EC50值分别为0.06 和0.32 nM。
T15795	Luzindole N-乙酰-2-苄基色胺,N-0774	Melatonin Receptor; MT Receptor	GPCR/G Protein; Neuroscience
	Luzindole (N-0774) 是一种选择性褪黑素受体拮抗剂，可抑制实验性自身免疫性脑脊髓炎，有抗抑郁样活性。它优先靶向 MT2 (Mel1b)，对于人 MT2 和 MT1 的 Ki 值分别为 10.2 和 158 nM。
T1463	Ramelteon 雷美替胺,TAK-375	Melatonin Receptor; MT Receptor	GPCR/G Protein; Neuroscience
	Ramelteon (TAK-375) 是强效高选择性和可口服的 MT1/MT2激动剂，Ki 值分别为 14 和 112 pM，有用于失眠症的研究潜力。
T3495	Tasimelteon 他司美琼,VEC-162,BMS-214778	Melatonin Receptor; MT Receptor	GPCR/G Protein; Neuroscience
	Tasimelteon (BMS-214778) 是一种褪黑激素受体激动剂，用于治疗盲人的非 24 小时睡眠-觉醒障碍。
T1445	Agomelatine Thymanax,S-20098,Valdoxan,阿戈美拉汀	Melatonin Receptor; 5-HT Receptor	GPCR/G Protein; Neuroscience
	Agomelatine (Valdoxan) 是褪黑激素受体的强效激动剂和 5-羟色胺-2C (5-HT2C) 受体的拮抗剂，在猪和人 5-HT2C 克隆受体中pKi 分别为 6.4 和 6.2。
T16834	S26131 N-[2-[7-[3-[8-(2-acetamidoethyl)naphthalen-2-yl]oxypropoxy]naphthalen-1-yl]ethyl]acetamide	MT Receptor	Neuroscience
	S26131 (N-[2-[7-[3-[8-(2-acetamidoethyl)naphthalen-2-yl]oxypropoxy]naphthalen-1-yl]ethyl]acetamide) 是一种选择性的褪黑激素配体 MT1 和 MT2 拮抗剂，对 MT1 和 MT2 的 Ki 值分别为 0.5 和 112 nM。
T22530	6-Chloromelatonin	Melatonin Receptor; Dopamine Receptor	GPCR/G Protein; Neuroscience
	6-Chloromelatonin 是一种有效的褪黑素受体 (melatonin receptor) 激动剂，是一种5-甲氧基吲哚化合物，可竞争兔视网膜中相同的突触前褪黑激素受体位点，可抑制[3H]多巴胺的钙依赖性释放具有比褪黑素更高的代谢稳定性。6-Chloromelatonin 竞争 [3H] 褪黑素与 MT2 受体结合 (pKi=9.77)，可能用于研究与抑郁症相关的失眠和睡眠障碍。
T10073	2-Iodomelatonin	Melatonin Receptor	GPCR/G Protein
	2-Iodomelatonin 是褪黑激素受体 1 (MT1) 的强效激动剂，Ki 为 28 pM，对 MT1的选择性是 MT2 的 5 倍以上。2-Iodomelatonin 可用于鉴定，表征和定位脑和周围组织的褪黑激素结合位点。
T10929L	D-3263 hydrochloride EC D-3263 HCl,D3263 HCl salt	TRP/TRPV Channel	Membrane transporter/Ion channel
	D-3263 hydrochloride (D3263 HCl salt) 是一种具有口服活性的 TRPM8 激动剂。
T41345	AFMK Formyl-N-acetyl-5-methoxykynurenamine,Acetyl-N-formyl-5-methoxykynurenamine	Apoptosis; Free radical scavengers; Antioxidant; Endogenous Metabolite	Apoptosis; Metabolism; oxidation-reduction
	AFMK (Formyl-N-acetyl-5-methoxykynurenamine) 是褪黑激素的活性代谢物，具有抗氧化和自由基清除活性。 AFMK 是一种凋亡调节剂，可提高吉西他滨在 PANC-1 细胞中的抗肿瘤作用。
T10198	8-M-PDOT 8-Methoxy-2-propionamidotetralin,AH-002	MT Receptor	Neuroscience
	8-M-PDOT (AH-002) 是一种具有选择性和有效性的褪黑激素 MT2 受体激动剂，对 MT1 受体也具有抑制作用。8-M-PDOT 具有抗焦虑活性，可用于研究由 MT2 诱导的神经疼痛。
T34081	Piromelatine NEU-P-11,NEU-P 11,NEU-P11	P2X Receptor; 5-HT Receptor; MT Receptor; Sodium Channel; TRP/TRPV Channel	GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	Piromelatine 是褪黑激素 MT1/MT2 受体、5-HT1A 和 5-HT1D 的激动剂，也是 5-HT2B 的拮抗剂。Piromelatine 具有抗痛觉活性，对 P2X3、TRPV1 和 Nav1.7 通道有抑制作用，可用于促进睡眠、缓解疼痛、抗神经退行性疾病和抗抑郁疾病的研究。
T27429	GR 128107 GR128107,GR-128107
	GR 128107 is an antagonist of melatonin receptor.
T28645	S-22153
	S22153 is an antagonist of melatonin receptor.
T13707	Pareptide monohydrochloride	Others	Others
	Pareptide monohydrochloride is a metabolically stable analog of melatonin inhibitor (MIF).
T27430	GR 196429 GR-196429,GR 196,429,GR-196,429,GR196429,GR196,429
	GR 196429, a melatonin receptor agonist, exhibits selectivity for the MT1 subtype. This compound not only promotes sleep and alters circadian rhythms but also stimulates melatonin release in mice.
T22499	UCM 608 2-Phenylmelatonin	Others	Others
	melatonin agonist
T69409	DH-97
	DH-97 is a potent MT2 melatonin receptor antagonist (pKi value = 8.03).
T28644	S20928 S 20928,S-20928
	S20928 is an antagonist of melatonin receptor.
T29044	UCM 765 UCM-765,UCM765
	UCM 765 is a partial agonist of melatonin MT(2) receptor.
T22721	DH97 DH 97	Others	Others
	MT2 melatonin receptor antagonist
T17095	TIK-301 PD-6735,LY-156735	5-HT Receptor	GPCR/G Protein; Neuroscience
	TIK-301 is a chlorinated melatonin derivative and a potent, high-affinity, and orally active melatonin MT1 and MT2 receptors agonist (Kis: 0.081 nM and 0.042 nM, respectively). TIK-301 is also a 5-HT2B/5-HT2C receptor antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment.
T10929	D-3263	Others	Others
	D-3263 is an agonist of transient receptor potential melatonin member 8 (TRPM8) with potential antitumor activity.
T71182	N 0745
	N 0745 inhibits 2-[125I]-iodomelatonin binding to median eminence/pars tuberalis membranes with an affinity similar to that of melatonin.
T12689	Ramelteon metabolite M-II	Others	Others
	Ramelteon metabolite M-II is the major Ramelteon metabolite(human melatonin receptors (MT1 or MT2) with IC50s of 208 pM, 1470 pM). Ramelteon is an agonist of selective melatonin.
T21366	Sapropterin free base BPH4,Dapropterin,6R-BH4,Tetrahydro-6-biopterin,THB,Phenoptin
	Sapropterin is a naturally occurring essential cofactor of the three aromatic amino acid hydroxylase enzymes, used in the degradation of amino acid phenylalanine and in the biosynthesis of dopamine, epinephrine, melatonin, norepinephrine, neurotransmitter
T38112	DL-Tryptophan octyl ester (hydrochloride)
	Tryptophan is an amino acid precursor of serotonin and melatonin. DL-Tryptophan octyl ester is a tryptophan derivative with an octyl ester protected COOH group. This addition creates a stable, cell-permeable molecule capable of generating free tryptophan upon hydrolysis of the ester bond.
T36176	AMK (hydrochloride)
	AMK is an active metabolite of the neurohormone melatonin .1,2,3,4It is formed from melatoninviathe metabolic intermediate AFMK that is then deformylated by catalase or formamidase.5,6AMK scavenges singlet oxygenin vitrowhen used at a concentration of 200 μM.1It inhibits the epinephrine- and arachidonic acid-induced production of prostaglandin E2and PGD2in ovine seminal vesicle microsomes in a concentration- and time-dependent manner, as well as LPS-induced increases in COX-2 levels in RAW 264.7...
T33450	ML 23 ML-23,ML23
	ML 23 is a melatonin analogue in the treatment and management of Parkinson's disease. ML-23 is a potential clinical candidate for the treatment of PD, and the present study has been undertaken to determine the efficacy of ML-23 in the 1-methyl-4-phenyl, 1
T73832	Tubulin inhibitor 21
	Tubulin inhibitor 21 (compound 6f) 为基于查尔酮与褪黑激素混合的有效tubulin抑制剂。该化合物对SW480细胞展现显著的细胞毒性活性（IC50=0.26 μM），对非恶性细胞的毒性较低。
T70035	Tasimelteon-d5
	Tasimelteon-d5 is intended for use as an internal standard for the quantification of tasimelteon by GC- or LC-MS. Tasimelteon is a melatonin (MT) receptor agonist. It selectively binds MT1 and MT2 receptors over a panel of 160 additional receptors and enzymes at 10 µM. Tasimelteon inhibits forskolin-induced cAMP accumulation with EC50 values of 0.79 and 1 nM in NIH3T3 cells expressing the MT1 or MT2 receptor, respectively. Formulations containing tasimelteon have been used in the treatment of no...
T71963	(−)-WIN 55,212-3 mesylate
	(−)-WIN 55,212-3 mesylate is an aminoalkylindole derivative which acts as a competitive neutral antagonist of the human cannabinoid CB2 receptor, blocking both the stimulating action of CP 55,940 and the inverse agonism of SR 144528. (−)-WIN 55,212-3 neither antagonizes nor mimics the effects of Δ9-THC on rat cerebellar membranes, which presumably express the CB1 receptor. (−)-WIN 55,212-3 also weakly antagonizes the melatonin MT1 and muscarinic M4 receptors but has no effect on several other G ...
T35993	Epitalon (acetate)
	Epitalon is a synthetic tetrapeptide with anti-aging properties.1,2,3,4 Dietary administration of epitalon (0.00001% w/w) reduces levels of lipid peroxidation products in aged D. melanogaster tissue homogenates.1 Epitalon (1 μg/animal) delays age-related estrous shutdown and decreases the frequency of bone marrow cell chromosomal aberrations in female mice.2 It decreases spontaneous mammary gland and ovarian tumor development and metastasis in aged female mice.3 Epitalon also stimulates melatoni...

化合物

Cat.No: T11995

Synonym: N-Acetyl-5-methoxytryptamine D5,Melatonin D5,褪黑素 D5

Target: Others

Melatonin Biotin

Cat.No: T64745

Melatonin receptor agonist 1

Cat.No: T60490

Cat.No: T14042

Synonym: 4-phenyl-2- propionamidotetralin

Target: Melatonin Receptor, MT Receptor

N-ACETYLTRYPTAMINE

Cat.No: T8600

Target: Melatonin Receptor

Cat.No: T9193

Target: Melatonin Receptor, MT Receptor

Cat.No: T15795

Synonym: N-乙酰-2-苄基色胺,N-0774

Target: Melatonin Receptor, MT Receptor

Cat.No: T1463

Synonym: 雷美替胺,TAK-375

Target: Melatonin Receptor, MT Receptor

Cat.No: T3495

Synonym: 他司美琼,VEC-162,BMS-214778

Target: Melatonin Receptor, MT Receptor

Cat.No: T1445

Synonym: Thymanax,S-20098,Valdoxan,阿戈美拉汀

Target: Melatonin Receptor, 5-HT Receptor

Cat.No: T16834

Synonym: N-[2-[7-[3-[8-(2-acetamidoethyl)naphthalen-2-yl]oxypropoxy]naphthalen-1-yl]ethyl]acetamide

Target: MT Receptor

6-Chloromelatonin

Cat.No: T22530

Target: Melatonin Receptor, Dopamine Receptor

2-Iodomelatonin

Cat.No: T10073

Target: Melatonin Receptor

D-3263 hydrochloride

Cat.No: T10929L

Synonym: EC D-3263 HCl,D3263 HCl salt

Target: TRP/TRPV Channel

Cat.No: T41345

Synonym: Formyl-N-acetyl-5-methoxykynurenamine,Acetyl-N-formyl-5-methoxykynurenamine

Target: Apoptosis, Free radical scavengers, Antioxidant, Endogenous Metabolite

Cat.No: T10198

Synonym: 8-Methoxy-2-propionamidotetralin,AH-002

Target: MT Receptor

Cat.No: T34081

Synonym: NEU-P-11,NEU-P 11,NEU-P11

Target: P2X Receptor, 5-HT Receptor, MT Receptor, Sodium Channel, TRP/TRPV Channel

Cat.No: T27429

Synonym: GR128107,GR-128107

Cat.No: T28645

Pareptide monohydrochloride

Cat.No: T13707

Target: Others

Cat.No: T27430

Synonym: GR-196429,GR 196,429,GR-196,429,GR196429,GR196,429

Cat.No: T22499

Synonym: 2-Phenylmelatonin

Target: Others

Cat.No: T69409

Cat.No: T28644

Synonym: S 20928,S-20928

Cat.No: T29044

Synonym: UCM-765,UCM765

Cat.No: T22721

Synonym: DH 97

Target: Others

Cat.No: T17095

Synonym: PD-6735,LY-156735

Target: 5-HT Receptor

Cat.No: T10929

Target: Others

Cat.No: T71182

Ramelteon metabolite M-II

Cat.No: T12689

Target: Others

Sapropterin free base

Cat.No: T21366

Synonym: BPH4,Dapropterin,6R-BH4,Tetrahydro-6-biopterin,THB,Phenoptin

DL-Tryptophan octyl ester (hydrochloride)

Cat.No: T38112

AMK (hydrochloride)

Cat.No: T36176

Cat.No: T33450

Synonym: ML-23,ML23

Tubulin inhibitor 21

Cat.No: T73832

Cat.No: T70035

(−)-WIN 55,212-3 mesylate

Cat.No: T71963

Epitalon (acetate)

Cat.No: T35993

Cat. No.	Product Name	Target	Signaling Pathways
T1659	Melatonin Melatonine,松果体素,N-Acetyl-5-methoxytryptamine,褪黑素	CaMK; Apoptosis; Mitophagy; Estrogen/progestogen Receptor; Melatonin Receptor; Glutathione Peroxidase; Endogenous Metabolite; ROR; Autophagy	Apoptosis; Autophagy; Endocrinology/Hormones; GPCR/G Protein; Metabolism; Neuroscience
	Melatonin (Melatonine) 是一种由松果体制成的激素，可激活褪黑激素受体。它在睡眠中起作用，有抗氧化和抗炎特性。它是新型选择性ATF-6抑制剂，可诱导细胞凋亡。
T13520	6-Hydroxymelatonin	Others	Others
	6-Hydroxymelatonin is a primary metabolic of Melatonin, which is metabolized by CYP 1A2.
T13513	5-Methoxyindole-3-acetic acid Methoxyindoleacetic acid,5-Methoxyindoleacetic acid,5-甲氧基吲哚-3-乙酸	Endogenous Metabolite	Metabolism
	5-Methoxyindole-3-acetic acid (5-Methoxyindoleacetic acid) 是一种 Melatonin 的代谢产物。
T1354	N-Acetyl-5-hydroxytryptamine Normelatonin,N-乙酰-5-羟色胺,O-Demethylmelatonin,N-Acetylserotonin	Trk receptor; Endogenous Metabolite	Metabolism; Tyrosine Kinase/Adaptors
	N-Acetyl-5-hydroxytryptamine (O-Demethylmelatonin) 是褪黑激素的直接前体，能够有效激活TrkB 受体。
T8181	Poricoic acid A Poricoic acid A(F),茯苓新酸 A	Others	Others
	Poricoic acid A (Poricoic acid A(F)) 是提取于 Poria cocos 中，拥有抗肿瘤作用。它通过调节Gas6/AxlNFκB/Nrf2 轴提高AKI-to-CKD 的褪黑激素抑制。

天然产物

Cat.No: T1659

Synonym: Melatonine,松果体素,N-Acetyl-5-methoxytryptamine,褪黑素

Target: CaMK, Apoptosis, Mitophagy, Estrogen/progestogen Receptor, Melatonin Receptor, Glutathione Peroxidase, Endogenous Metabolite, ROR, Autophagy

6-Hydroxymelatonin

Cat.No: T13520

Target: Others

5-Methoxyindole-3-acetic acid

Cat.No: T13513

Synonym: Methoxyindoleacetic acid,5-Methoxyindoleacetic acid,5-甲氧基吲哚-3-乙酸

Target: Endogenous Metabolite

N-Acetyl-5-hydroxytryptamine

Cat.No: T1354

Synonym: Normelatonin,N-乙酰-5-羟色胺,O-Demethylmelatonin,N-Acetylserotonin

Target: Trk receptor, Endogenous Metabolite

Poricoic acid A

Cat.No: T8181

Synonym: Poricoic acid A(F),茯苓新酸 A

Target: Others

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