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Cat. No. | Product Name | ||
---|---|---|---|
L3300 | 组胺&褪黑色素化合物库 | 153 compounds | |
153 种生物活性小分子化合物,用于高通量、高内涵筛选; |
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
|
Others | Others |
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。 | |||
T22721 |
DH97
DH 97 |
Others | Others |
MT2 melatonin receptor antagonist | |||
T28644 |
S20928
S 20928,S-20928 |
Others | Others |
S20928 is an antagonist of melatonin receptor. | |||
T29044 |
UCM 765
UCM-765,UCM765 |
Others | Others |
UCM 765 is a partial agonist of melatonin MT(2) receptor. | |||
T27429 |
GR 128107
GR128107,GR-128107 |
Others | Others |
GR 128107 is an antagonist of melatonin receptor. | |||
T28645 |
S-22153
|
Others | Others |
S22153 is an antagonist of melatonin receptor. | |||
T10929 |
D-3263
|
Others | Others |
D-3263 is an agonist of transient receptor potential melatonin member 8 (TRPM8) with potential antitumor activity. | |||
T69409 |
DH-97
|
Others | Others |
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 |
Others | Others |
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. | |||
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. | |||
TP2515 |
Cyclo(L-Leu-L-Trp)
|
Others | Others |
Cyclo(L-Leu-L-Trp) is a diketopiperazine metabolite initially derived from Penicillium, exhibiting antibacterial (MICs = 125-1000 µg/ml) and antifungal activities (MICs = 8-64 µg/ml). It also demonstrates antioxidant properties by reducing the production of hydroxy radicals, as evidenced in an electron spin resonance (ESR) spectroscopy assay (IC50 = 1.8 µM). Additionally, Cyclo(L-Leu-L-Trp) has been identified as a bitter compound capable of quickly crossing rat taste cell membranes ex vivo at a... | |||
T85299 |
ML-252 hydrochloride
|
Others | Others |
ML-252 is a potent, selective inhibitor of the Kv7.2 voltage-gated potassium channel, demonstrating an IC50 value of 69 nM in patch clamp assays. It exists as the (S)-enantiomer, which is significantly more effective than both its (R)-enantiomer counterpart and the racemic mixture, with respective IC50 values of 944 nM and 160 nM. ML-252 exhibits high selectivity for Kv7.2 over other potassium channel subtypes and shows minimal activity against more than 68 G protein-coupled receptors, various t... |
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。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TMIH-0485 |
Ramelteon-d3
|
||
Ramelteon-d3 是 Ramelteon 的氘代化合物。Ramelteon 的 CAS 号为 196597-26-9。Ramelteon 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。 | |||
TMIH-0486 |
Ramelteon-d5
|
||
Ramelteon-d5 是 Ramelteon 的氘代化合物。Ramelteon 的 CAS 号为 196597-26-9。Ramelteon 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。 | |||
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... |