目录号 | 产品详情 | 靶点 | |
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T71884 | |||
β-Carboline-1-carboxylic acid is an alkaloid that has been found in P. quassioides and has diverse biological activities. It reduces LPS-induced increases in MCP-1, TNF-α, IL-6, and IL-1β levels in RAW 264.7 cells when used at a concentration of 15 µg/ml and inhibits the epithelial-to-mesenchymal transition (EMT) induced by TGF-β1 in A549 cells. β-Carboline-1-carboxylic acid induces cytotoxicity in CT26.WT, K562, and SGC-7901 cells (IC50s = 14.96, 22.11, and 19.7 µg/ml, respectively) but not HepG2 or A549 cells (IC50s = 36.41 and 41.51 µg/ml, respectively). It also inhibits cAMP phosphodiesterase with an IC50 value of 96 µM. | |||
T71328 | |||
Theobromine-d6 is intended for use as an internal standard for the quantification of theobromine by GC- or LC-MS. Theobromine is a methylxanthine alkaloid and derivative of caffeine that has been found in cocoa beans and has diverse biological activities. It is an adenosine A1 receptor antagonist. Theobromine increases AMPK phosphorylation and inhibits adipocyte differentiation, ERK and JNK phosphorylation, and IL-6 and TNF-α production in 3T3-L1 preadipocytes cultured in differentiation medium. It inhibits decreases in renal cortex SIRT1 activity and increases in NADPH oxidase-dependent reactive oxygen species (ROS) production, as well as reduces kidney hypertrophy and albuminuria in a spontaneously hypertensive rat model of streptozotocin-induced diabetes when administered at a dose of 5 mg/kg per day.3 Theobromine is toxic to dogs with an LD50 value of 250 to 500 mg/kg. | |||
T79941 | Apoptosis | ||
Anticanceragent 141(compound AE)是一种针对HPV感染宫颈癌具有抑制作用的抗霉素生物碱。该化合物能够抑制宫颈癌HeLa细胞的增殖并导致细胞周期在S期停滞。Anticanceragent 141破坏线粒体功能,诱导caspase依赖性细胞凋亡,并激活ROS介导的泛素依赖性蛋白酶体系统,进而引起E6/E7癌蛋白的降解。 | |||
T78135 | |||
Nicotelline(Nicotellin)是一种与尼古丁相关的生物碱,作为人类cDNA表达的细胞色素P-450 2A6(CYP2A6)的弱抑制剂,不显著抑制该酶介导的香豆素7-羟基化反应,在300 μM浓度下效果更是如此。此外,Nicotelline还被用作烟草烟雾中颗粒物(PM)的示踪剂和生物标记物。 | |||
T75238 | |||
YS-49 (单水合物) 作为PI3K/Akt(RhoA的下游靶点)的激活剂,有效降低3-甲基胆碱处理的细胞中RhoA/PTEN的活性。此外,YS-49通过促进血红素加氧酶(HO-1)的表达,抑制血管紧张素II(Ang II)诱导的血管平滑肌细胞(VSMC)增殖。作为一种异喹啉化合物生物碱,YS-49因激活心脏β-adrenoceptors而显示出显著的正性肌力效应。 | |||
T75436 | |||
Jatrorrhizine hydroxide, 一种从黄连中提取的生物碱,展现了神经保护、抗菌、抗疟原虫及抗氧化的活性。作为一种高效的乙酰胆碱酯酶(AChE)抑制剂(IC50=872 nM),其对BuChE的选择性高达115倍。此外,Jatrorrhizine hydroxide还能通过抑制uptake-2 transporter活性来减少血清素(5-HT)和去甲肾上腺素(NE)的摄取,表现出口服活性。 | |||
T83913 | |||
Mitraciliatine是一种在M. speciosa(泰国称为Kratom)中发现的生物碱,是μ-阿片受体(MOR)部分激动剂和κ-阿片受体(KOR)激动剂。该化合物对MOR和KOR具有选择性,与δ-阿片受体(DOR; EC50s分别为228, 218, 和 >1,000 nM,针对小鼠受体在GTPγS结合实验中的表现)。Mitraciliatine(100 nmol/动物,脑室内注射)在小鼠的热水尾部缩回实验中延长了撤回潜伏期,这一效果可以通过敲除MOR而非KOR来逆转。与吗啡不同,Mitraciliatine不会诱发过度活动或呼吸抑制。 | |||
TN4997 | IGF-1R | ||
Serpentine 是一种玫瑰花根中的生物碱,可用作胰岛素增敏剂,以协助胰岛素降低血糖。Serpentine 可激活 AMPK 磷酸化,从而刺激C2C12细胞对葡萄糖的摄取。Serpentine 可增加了肌肉组织中GSK-3β mRNA的表达,从而增强葡萄糖摄取。Serpentine 显著增加胰高血糖素分泌和肝糖异生。在高脂肪饮食/链脲佐菌素(HFD/STZ)诱导的糖尿病小鼠中,Serpentine 显著延长了胰岛素的降血糖时间,显著降低了外源性胰岛素的使用,抑制了内源性胰岛素的分泌。 | |||
T37452 | |||
Stephacidin B is a fungal metabolite that has been found inA. ochraceus.1Dimeric stephacidin B is rapidly converted to a monomer, avrainvillamide ,in vitro.2Stephacidin B is cytotoxic to a variety of cancer cells, including testosterone-independent PC3 and -sensitive LNCaP prostate cancer cells (IC50s = 0.37 and 0.06 μM, respectively) and estradiol-independent SK-BR-3 and -sensitive MCF-7 breast cancer cells (IC50s = 0.32 and 0.27 μM, respectively).1It induces apoptosis in HepG2 and Huh7 hepatocellular carcinoma cells when used at a concentration of 4 μM.3 1.Qian-Cutrone, J., Huang, S., Shu, Y.-Z., et al.Stephacidin A and B: Two structurally novel, selective inhibitors of the testosterone-dependent prostate LNCaP cellsJ. Am. Chem. Soc.124(49)14556-14557(2002) 2.Wulff, J.E., Herzon, S.B., Siegrist, R., et al.Evidence for the rapid conversion of stephacidin B into the electrophilic monomer avrainvillamide in cell cultureJ. Am. Chem. Soc.129(16)4898-4899(2007) 3.Hu, L., Zhang, T., Liu, D., et al.Notoamide-type alkaloid induced apoptosis and autophagy via a P38/JNK signaling pathway in hepatocellular carcinoma cellsRSC Adv.9(34)19855-19868(2019) |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPH-03402 | STR1 Protein, Rauvolfia serpentina, Recombinant (His & Myc) | Rauvolfia serpentina | E. coli | ||
Catalyzes the stereospecific condensation of tryptamine with secologanin to form strictosidine, the key intermediate of indole alkaloid biosynthesis.
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TMPH-00861 | HTR1D Protein, Human, Recombinant (His & KSI) | Human | E. coli | ||
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Regulates the release of 5-hydroxytryptamine in the brain, and thereby affects neural activity. May also play a role in regulating the release of other neurotransmitters. May play a role in vasoconstriction.
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TMPH-00860 | HTR1D Protein, Human, Recombinant (hFc) | Human | HEK293 | ||
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Regulates the release of 5-hydroxytryptamine in the brain, and thereby affects neural activity. May also play a role in regulating the release of other neurotransmitters. May play a role in vasoconstriction.
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TMPH-00859 | HTR1B Protein, Human, Recombinant (His) | Human | in vitro E. coli expression system | ||
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Regulates the release of 5-hydroxytryptamine, dopamine and acetylcholine in the brain, and thereby affects neural activity, nociceptive processing, pain perception, mood and behavior. Besides, plays a role in vasoconstriction of cerebral arteries.
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