37
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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T39461 |
MT1
|
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MT1, a bivalent chemical probe targeting BET bromodomains, demonstrates an IC50 value of 0.789 nM for BRD4(1). | |||
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。 | |||
T8841 |
IMT1
Propanamide, N,N-dimethyl-2-[[4-(2-methylphenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-,LDC195943(IMT1) |
Others; DNA/RNA Synthesis; Mitochondrial Metabolism | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism; Others |
IMT1 (Propanamide, N,N-dimethyl-2-[[4-(2-methylphenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-) 是一种非竞争特异性人类线粒体 RNA 聚合酶(POLRMT) 抑制剂,可引起 POLRMT 的构象变化,以剂量依赖性方式阻断底物结合和转录。它可降低脱氧核苷三磷酸水平和柠檬酸循环中间体,导致细胞氨基酸水平显著消耗,有用于线粒体转录等相关疾病的研究潜力。 | |||
T11063 |
DMT1 blocker 1
|
Others | Others |
DMT1 blocker 1 是二价金属转运蛋白1 (DMT1) 的阻断剂,IC50 为 0.64 μM,可以阻断体内肠细胞的铁摄取。 | |||
T11064 |
DMT1 blocker 2
|
Others | Others |
DMT1 blocker 2 是一种二价金属转运蛋白 1 的直接抑制剂(IC50:0.83 μM)。它可以阻断体内肠细胞的铁摄取。 | |||
T8842 |
IMT1B
3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)-,LDC203974 |
Others; DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others |
IMT1B (LDC203974) 是一种特异性的、具有口服活性的、非竞争性的线粒体 RNA 聚合酶 (POLRMT) 别构抑制剂,能够抑制线粒体 DNA (mtDNA) 的表达,具有抗肿瘤活性。 | |||
T60129 |
MT189
Antiproliferative agent-14 |
Microtubule Associated | Cytoskeletal Signaling |
MT189 (Antiproliferative agent-14)是一种有效的微管蛋白聚合 (tubulin polymerization) 抑制剂,IC50 为 3.41 μM。MT189 具有优异的抗增殖活性。Antiproliferative agent-14 具有在细胞周期的 G2/M 期阻滞细胞的能力。 | |||
T71739 |
PTPMT1-IN-1
|
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PTPMT1-IN-1 is a PTEN-like mitochondrial phosphatase PTPMT1 inhibitor. | |||
T38421 |
PRMT1-IN-1
PRMT1-IN-1 |
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PRMT1-IN-1 is a PRMT1 inhibitor. | |||
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。 | |||
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。 | |||
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。 | |||
T1891 |
NSC 405020
|
MMP | Proteases/Proteasome |
NSC 405020 是一种 MT1-MMP 的非催化抑制剂,可特异地靶向 MT1-MMP 的 PEX 结构域,不会抑制 MT1-MMP 和 MMP-2的催化活性。 | |||
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。 | |||
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。 | |||
T28145 |
ND-322 HCl
ND 322 Hydrochloride,ND322 Hydrochloride,ND-322 Hydrochloride,ND322 HCl |
MMP | Proteases/Proteasome |
ND-322 HCl (ND 322 Hydrochloride) 是 MT1-MMP 和 MMP2 的选择性抑制剂,可减少体外黑色素瘤细胞的生长、迁移和侵袭。 | |||
T4093 |
Fabomotizole hydrochloride
Afobazole hydrochloride,CM346 hydrochloride |
MAO | Metabolism; Neuroscience |
Fabomotizole hydrochloride (CM346 hydrochloride) 是一种具有抗焦虑和神经保护作用的化合物。 | |||
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。 | |||
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。 | |||
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。 | |||
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. | |||
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。 | |||
T27430 |
GR 196429
GR-196429,GR 196,429,GR-196,429,GR196429,GR196,429 |
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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. | |||
T80217 |
BT1718
|
MMP | Proteases/Proteasome |
BT1718是一种针对MT1-MMP的双功能抗癌肽,通过MT1-MMP靶向肿瘤来传递细胞毒性有效载荷Mertansine。作为一种多肽-毒素偶联物,其KD值为3 nM。MT1-MMP在多种晚期实体肿瘤如三阴性乳腺癌(TNBC)和非小细胞肺癌中呈现过表达。 | |||
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
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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... | |||
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. | |||
T78436 |
Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2
|
MMP | Proteases/Proteasome |
Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 (FS-6) 是一种用于实时定量测定基质金属蛋白酶(MMP)酶活性的猝灭荧光肽底物。该化合物是MMP底物(FS-1)的衍生物,对胶原酶MMP-1、MMP-8、MMP-13及MT1-MMP的特异性常数更高,具备较强的底物特异性。荧光激发与发射波长分别为325 nm和400 nm。 | |||
T70073 |
Fabomotizole dihydrochloride
|
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Fabomotizole, also known as Afobazole, Obenoxazine and CM346, is an anxiolytic drug launched in Russia in the early 2000s. It produces anxiolytic and neuroprotective effects without any sedative or muscle relaxant actions. Its mechanism of action remains poorly defined however, with GABAergic, NGF- and BDNF-release-promoting, MT1 receptor agonism, MT3 receptor antagonism, and sigma agonism suggested as potential mechanisms. Fabomotizole was shown to inhibit MAO-A reversibly and there might be al... | |||
T71963 |
(−)-WIN 55,212-3 mesylate
|
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(−)-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 ... | |||
T60490 |
Melatonin receptor agonist 1
|
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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。 | |||
T28645 |
S-22153
|
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S22153 is an antagonist of melatonin receptor. |
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。 |