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24

抑制剂 & 化合物

2

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Cat. No. Product Name Target Signaling Pathways
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。
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。
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。
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。
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。
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。
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。
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。
T27429 GR 128107

GR128107,GR-128107

GR 128107 is an antagonist of melatonin receptor.
T28645 S-22153

S22153 is an antagonist of melatonin receptor.
T69409 DH-97

DH-97 is a potent MT2 melatonin receptor antagonist (pKi value = 8.03).
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.
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.
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 ...

化合物

4-P-PDOT
Cat.No: T14042
Synonym: 4-phenyl-2- propionamidotetralin
Target: Melatonin Receptor, MT Receptor
N-ACETYLTRYPTAMINE
Cat.No: T8600
Synonym:
Target: Melatonin Receptor
ACH-000143
Cat.No: T9193
Synonym:
Target: Melatonin Receptor, MT Receptor
Melatonin receptor agonist 1
Cat.No: T60490
Synonym:
Target:
Agomelatine
Cat.No: T1445
Synonym: Thymanax,S-20098,Valdoxan,阿戈美拉汀
Target: Melatonin Receptor, 5-HT Receptor
Luzindole
Cat.No: T15795
Synonym: N-乙酰-2-苄基色胺,N-0774
Target: Melatonin Receptor, MT Receptor
Ramelteon
Cat.No: T1463
Synonym: 雷美替胺,TAK-375
Target: Melatonin Receptor, MT Receptor
Tasimelteon
Cat.No: T3495
Synonym: 他司美琼,VEC-162,BMS-214778
Target: Melatonin Receptor, MT Receptor
S26131
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
Synonym:
Target: Melatonin Receptor, Dopamine Receptor
D-3263 hydrochloride
Cat.No: T10929L
Synonym: EC D-3263 HCl,D3263 HCl salt
Target: TRP/TRPV Channel
2-Iodomelatonin
Cat.No: T10073
Synonym:
Target: Melatonin Receptor
8-M-PDOT
Cat.No: T10198
Synonym: 8-Methoxy-2-propionamidotetralin,AH-002
Target: MT Receptor
GR 128107
Cat.No: T27429
Synonym: GR128107,GR-128107
Target:
S-22153
Cat.No: T28645
Synonym:
Target:
DH-97
Cat.No: T69409
Synonym:
Target:
GR 196429
Cat.No: T27430
Synonym: GR-196429,GR 196,429,GR-196,429,GR196429,GR196,429
Target:
S20928
Cat.No: T28644
Synonym: S 20928,S-20928
Target:
UCM 765
Cat.No: T29044
Synonym: UCM-765,UCM765
Target:
DH97
Cat.No: T22721
Synonym: DH 97
Target: Others
TIK-301
Cat.No: T17095
Synonym: PD-6735,LY-156735
Target: 5-HT Receptor
D-3263
Cat.No: T10929
Synonym:
Target: Others
Tasimelteon-d5
Cat.No: T70035
Synonym:
Target:
(−)-WIN 55,212-3 mesylate
Cat.No: T71963
Synonym:
Target:
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。
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。

天然产物

Melatonin
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
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
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