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抑制剂 & 化合物

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天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
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。
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。
T11167	EHMT2-IN-2	Others	Others
	EHMT2-IN-2 Used in the research of blood disease or cancer. EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2.
T11166	EHMT2-IN-1	Others	Others
	EHMT2-IN-1 is a potent EHMT inhibitor, . Used in the research of blood disorder or cancer.with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2.
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。
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。
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。
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。
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。
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。
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。
T60523	Agomelatine hydrochloride S-20098 hydrochloride	MT Receptor	Neuroscience
	Agomelatine hydrochloride (S-20098 hydrochloride) (S-20098 hydrochloride) 是特异性的MT1和MT2受体激动剂，对 CHO-hMT1的Ki 值为0.1 nM，对HEK-hMT1的Ki 值为0.06 nM，对CHO-hMT2的Ki 值为0.12 nM，对HEK-hMT2 的Ki 值为0.27 nM。Agomelatine hydrochloride 是选择性的5-羟色胺2C(5-HT2C)受体拮抗剂，对天然 (猪) 和克隆的人 5-HT2C 受体的pKi 值分别为 6.4 和 6.2。
T69409	DH-97
	DH-97 is a potent MT2 melatonin receptor antagonist (pKi value = 8.03).
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.
T22721	DH97 DH 97	Others	Others
	MT2 melatonin receptor antagonist
T10266	Agomelatine-d6 Agomelatine D6,S-20098 D6	Others	Others
	Agomelatine D6 (S-20098 D6) is a deuterium-labeled Agomelatine. Agomelatine is a specific agonist of MT1 and MT2 receptors.
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...
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。
T10267	Agomelatine (L(+)-Tartaric acid) 阿戈美拉汀 L(+)-酒石酸,S-20098 L(+)-Tartaric acid	5-HT Receptor	GPCR/G Protein; Neuroscience
	Agomelatine (S-20098) L(+)-Tartaric acid is a specific agonist of MT1 and MT2 receptors (Kis: 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2). It also is a selective 5-HT2C receptor antagonist (pKis: 6.4 and 6.2 at native (porcine) and cloned (human) 5-HT2C receptors).
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.
T10193	7-Desmethyl-agomelatine	Others	Others
	7-Desmethyl-agomelatine is a metabolite of Agomelatine and has less activity than Agomelatine. Agomelatine is a melatonergic (MT1 and MT2) agonist and 5-HT2C antagonist.
T10192	7-Desmethyl-3-hydroxyagomelatine 3-Hydroxy-7-desmethyl agomelatine	5-HT Receptor	GPCR/G Protein; Neuroscience
	7-Desmethyl-3-hydroxyagomelatine is a metabolite of Agomelatine and has less activity than Agomelatine. Agomelatine is a melatonergic (MT1 and MT2) agonist and 5-HT2C antagonist.
T28645	S-22153
	S22153 is an antagonist of melatonin receptor.

化合物

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: T16834

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

Target: MT Receptor

Cat.No: T1445

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

Target: Melatonin Receptor, 5-HT Receptor

Cat.No: T11167

Target: Others

Cat.No: T11166

Target: Others

Cat.No: T15795

Synonym: N-乙酰-2-苄基色胺,N-0774

Target: Melatonin Receptor, MT Receptor

Cat.No: T9193

Target: Melatonin Receptor, MT Receptor

Cat.No: T10198

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

Target: MT Receptor

6-Chloromelatonin

Cat.No: T22530

Target: Melatonin Receptor, Dopamine Receptor

Cat.No: T14042

Synonym: 4-phenyl-2- propionamidotetralin

Target: Melatonin Receptor, 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

2-Iodomelatonin

Cat.No: T10073

Target: Melatonin Receptor

Agomelatine hydrochloride

Cat.No: T60523

Synonym: S-20098 hydrochloride

Target: MT Receptor

Cat.No: T69409

Cat.No: T17095

Synonym: PD-6735,LY-156735

Target: 5-HT Receptor

Cat.No: T22721

Synonym: DH 97

Target: Others

Cat.No: T10266

Synonym: Agomelatine D6,S-20098 D6

Target: Others

Cat.No: T70035

Melatonin receptor agonist 1

Cat.No: T60490

Agomelatine (L(+)-Tartaric acid)

Cat.No: T10267

Synonym: 阿戈美拉汀 L(+)-酒石酸,S-20098 L(+)-Tartaric acid

Target: 5-HT Receptor

Ramelteon metabolite M-II

Cat.No: T12689

Target: Others

7-Desmethyl-agomelatine

Cat.No: T10193

Target: Others

7-Desmethyl-3-hydroxyagomelatine

Cat.No: T10192

Synonym: 3-Hydroxy-7-desmethyl agomelatine

Target: 5-HT Receptor

Cat.No: T28645

Cat. No.	Product Name	Target	Signaling Pathways
T2O2728	glycine 2-Aminoacetic acid,Glycolixir,Aminoacetic acid,Glycosthene,Glycocoll,甘氨酸	MT Receptor; Endogenous Metabolite; iGluR	Membrane transporter/Ion channel; Metabolism; Neuroscience
	glycine (2-Aminoacetic acid) 是中枢神经系统的抑制性神经递质，也是谷氨酸的联合激动剂，有促进谷氨酸能NMDA 受体兴奋的潜力。它主要存在于明胶和丝素蛋白中，并在治疗上用作营养物质。

天然产物

Cat.No: T2O2728

Synonym: 2-Aminoacetic acid,Glycolixir,Aminoacetic acid,Glycosthene,Glycocoll,甘氨酸

Target: MT Receptor, Endogenous Metabolite, iGluR

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