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T9266
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Fatostatin
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Lipid;
Fatty Acid Synthase |
Metabolism |
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Fatostatin A 是一种SREBP 活化的特异性抑制剂，能够抑制 SREBP-1 和 SREBP-2 的活化。它与 SCAP (SREBP 裂解激活蛋白) 结合，抑制 SREBPs 的 ER-Golgi 易位。它具有抗肿瘤活性，能抑制ob/ob 小鼠的高血糖。它抑制细胞中成脂基因的转录。 |
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T6832
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Fatostatin hydrobromide
Fatostatin HBr,Fatostatin A,Fatostatin A HBr,Fatostatin
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NPC1L1;
Fatty Acid Synthase |
Membrane transporter/Ion channel;
Metabolism |
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Fatostatin hydrobromide (Fatostatin A HBr) 是一种 SREBP 活化的特异性抑制剂，可抑制 SREBP-1 和 SREBP-2 的活化。它与 SCAP (SREBP 裂解激活蛋白) 结合，抑制 SREBPs 的 ER-Golgi 易位。它具有抗肿瘤作用，能抑制 ob/ob 小鼠的高血糖。它抑制了细胞中成脂基因的转录。 |
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TP1376
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GLP-1(7-37) acetate(106612-94-6 free base)
GLP-1(7-37) acetate
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Others;
Glucagon Receptor |
GPCR/G Protein;
Others |
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GLP-1(7-37) acetate 是肠道胰岛素激素，能够促进葡萄糖诱导的胰岛素分泌。 |
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T8773
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MID-1
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Others;
IGF-1R |
Others;
Tyrosine Kinase/Adaptors |
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MID-1 是 MG53-IRS-1 相互作用的抑制剂，能够破坏 MG53 与 IRS-1 的分子缔合，并消除 MG53 诱导的 IRS-1 泛素化和骨骼肌降解，升高 IRS-1 表达水平，增加胰岛素信号传导和葡萄糖摄取。 |
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T13867
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RH01386
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Others |
Others |
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RH01386是可以预防 ER 应激诱导的β细胞功能障碍和死亡、抑制促凋亡基因表达的小分子。它恢复内质网应激受损的葡萄糖刺激的胰岛素分泌反应。对2型糖尿病具有潜在的研究价值。 |
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TP2209L
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Xenin 8 acetate
Xenin 8 acetate (117442-28-1 Free base)
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IGF-1R |
Tyrosine Kinase/Adaptors |
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Xenin 8 acetate 是神经降压素/异视素家族中 Xenin 的生物活性片段。 Xenin 8 acetate 增强精氨酸诱导的胰岛素释放（40%）并增强胰高血糖素对精氨酸（60%）和卡巴胆碱（50%）的反应。 |
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T2160
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Suramin Sodium Salt
苏拉明钠,BAY-205,Suramin hexasodium salt,苏拉明钠盐,NF-060
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Apoptosis;
Phosphatase;
SARS-CoV;
Sirtuin;
Reverse Transcriptase;
Topoisomerase;
Parasite |
Apoptosis;
Chromatin/Epigenetic;
DNA Damage/DNA Repair;
Metabolism;
Microbiology/Virology |
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Suramin Sodium Salt (BAY-205) 是可逆的竞争性蛋白酪氨酸磷酸酶抑制剂。它抑制 IP5K，是抗寄生虫，抗肿瘤和抗血管生成剂。它是sirtuins 的有效抑制剂，也是 SARS-CoV-2 RNA 依赖性 RNA 聚合酶抑制剂。 |
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T15368L
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Galantide acetate
Galantide acetate(138579-66-5 Free base)
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Neuropeptide Y Receptor |
GPCR/G Protein;
Neuroscience |
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Galantide acetate 是一种特殊的甘丙肽受体 (galanin receptor) 拮抗剂，是一种由甘丙肽和 P 物质片段组成的肽段，在大鼠下丘脑可识别两类甘丙肽结合位点 (KD 分别小于 0.1 nM 和 ~6 nM)。Galantide 剂量依赖性 (IC50=1.0 nM) 拮抗甘丙肽介导的葡萄糖诱导的小鼠胰岛胰岛素分泌抑制。Galantide acetate 似乎与单一的 SP 受体群结合 (KD~40 nM)。 |
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T37892
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GLP-1(7-36), amide TFA
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GLP-1(7-36), amide TFA is a prominent intestinal hormone known to stimulate glucose-induced insulin secretion from β cells[1]. |
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T34600
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Secretin (1-6)
Secretin,N-terminal hexapeptide
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Secretin (1-6) is the N-terminal part of secretin. It can produce vitro glucose-dependent insulin release induced by secretin. |
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TP1141
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GLP-1(7-36), amide acetate
GLP-1(7-36) Acetate,Human GLP-1-(7-36)-amide Acetate
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GLP-1(7-36) Acetate is a major intestinal hormone that stimulates glucose-induced insulin secretion from β cells. |
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T26617
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AMG-221
AMG221
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AMG-221 is a potent and selective 11β-HSD1 inhibitor. AMG-221 decreased fed blood glucose and insulin levels and reduced body weight in diet-induced obesity mice. |
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T27324
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FK614
FK 614,ATx-08-001,ATx-08001,FK-614
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FK-614 is a selective agonist of peroxisome proliferator-activated receptor gamma. FK-614 improves peripheral glucose utilization while decreases hepatic insulin extraction in alloxan-induced diabetic dogs. |
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T30261
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AZD6482 (S-isomer)
AZD-6482,AZD 6482,AZD6482 (S),AZD6482
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AZD6482 (S-isomer) is a potent, selective, ATP-competitive PI3Kβ inhibitor (IC(50) 0.01 μm), which can inhibit insulin-induced in vitro glucose uptake by human adipocytes (IC(50) is 4.4 μm). |
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T76634
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(Sar1,Ile4,8)-Angiotensin II
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(Sar1,Ile4,8)-Angiotensin II是一种对angiotensin II type 1 receptor (AT1R)具有功能选择性的激动剂，能增强胰岛素受体 (IR) 信号和糖原合成，同时还能促进Akt和GSK3α/β的磷酸化，这一过程被胰岛素刺激所增强。 |
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TP2033
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[Des-His1,Glu9]-Glucagon amide
des-His1-[Glu9]-Glucagon (1-29) amide
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Glucagon receptor antagonist (pA2 = 7.2 for inhibition of glucagon-induced adenylyl cyclase activation in rat liver membranes); displays no agonist activity. Enhances glucose-stimulated pancreatic insulin release in vitro. Blocks added glucagon-induced hy |
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T3984
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GLP-1(7-36), amide
MKC 253,胰高血糖素样肽-1,Human GLP-1-(7-36)-amide,Glucagon-like Peptide 1 (7-36) amide,Glucagon-Like Peptide (GLP) I (7-36), amide, human,GLP-1(7-36),GLP-1-(7-36)-amide
|
Glucagon Receptor |
GPCR/G Protein |
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GLP-1(7-36), amide (MKC 253) 是一种生理性肠降血糖素，能够刺激胰岛素分泌。 |
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T37120
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1,2,3-Triundecanoyl Glycerol
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1,2,3-Triundecanoyl glycerol is a triacylglycerol that contains undecanoic acid at thesn-1,sn-2, andsn-3 positions. Dietary administration of a 7:3 (w/w) mixture of 1,2,3-triundecanoyl glycerol and corn oil prevents fasting-induced decreases in plasma glucose, alanine, and insulin levels, as well as the ratio of insulin to glucagon, in rats compared with dietary administration of corn oil alone.1
1.Pi-Sunyer, F.X., Conway, J.M., Lavau, M., et al.Glucagon, insulin, and gluconeogenesis in fasted o... |
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T26724
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AZD-9164 bromide
AZD9164,AZD-9164,AZD 9164
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AMG-221 is a potent and selective 11β-HSD1 inhibitor. AMG 221 potently blocked 11β-HSD1 activity, producing sustained inhibition for the 24-hour study duration as measured in ex vivo adipose samples. AMG-221 decreased fed blood glucose and insulin levels |
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T71981
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Gliclazide-d4
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Gliclazide-d4 is intended for use as an internal standard for the quantification of gliclazide by GC- or LC-MS. Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels. It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels. Gliclazide (5 μM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin... |
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T83694
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Gastric Inhibitory Peptide (1-42) (porcine) TFA
GIP (1-42),Glucose-dependent Insulinotropic Polypeptide (1-42)
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胃抑制肽(GIP) (1-42)是一种内源性的42氨基酸肽类肠促素激素，能诱导胰岛素分泌。该激素在肠道神经内分泌K细胞和颌下腺中表达，并在餐后释放到循环中。GIP (1-42)抑制由组胺、五肽和胰岛素引起的胃酸和胃蛋白酶分泌，增加葡萄糖诱导的胰岛素释放，并在大鼠中刺激胃排空。 |
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T82295
|
GluR23Y
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GluR23Y是一种具有生物活性的肽，应用于ELISA细胞表面测定，专用于监测培养的海马神经元内AMPA受体在胰岛素刺激下的内吞情况。该肽能够阻止由胰岛素引起的AMPA受体数量的下降。通过将GluR23Y与HIV-1的膜转导结构域融合，实现对神经元的传递，从而有效抑制了胰岛素诱导的效应。 |
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T40518L
|
C-Peptide 2, rat acetate
C-Peptide 2, rat acetate (41594-08-5 Free base)
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Others |
Others |
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C-Peptide 2, rat acetate 是一种可抑制葡萄糖诱导的胰岛素分泌胰岛素原组分，由31个氨基酸残基构成的多肽和醋酸盐组成。 |
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T72591
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Sp-5,6-DCl-cBIMPS
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|
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Sp-5,6-DCl-cBIMPS 为一种高效特异的 cAMP 依赖性蛋白激酶(cAMP-PK)激活剂，能够促进胰岛素释放，并抑制U46619引起的血小板Rho、Gq及G12/G13的激活[3]。 |
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T15043
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D5D-IN-326
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Others |
Others |
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D5D-IN-326 is an orally active delta-5 desaturase (D5D) inhibitor (IC50s: 72 and 22 nM for rat and human D5D in enzymic and cell-based assays). It has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in die |
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T70468
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MK-8666
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MK-8666 is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects. |
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T71559
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Melanotan II acetate
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Melanotan II acetate is an agonist of melanocortin receptor 1 (MC1R), MC3R, MC4R, and MC5R. It has been shown to improve recovery of sciatic nerve function after mechanical injury and increase cisplatin-induced decreases in sensory nerve conduction velocity. Melanotan II acetate increases oxygen consumption and protein levels of uncoupling protein 1 (UCP1) in brown adipose tissue homogenates and decreases food intake, body weight, and serum levels of leptin, glucose, insulin, and cholesterol. |
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T21681
|
AACOCF3
Arachidonyl trifluoromethyl ketone,Arachidonyltrifluoromethane
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Phospholipase |
Metabolism |
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AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeable trifluoromethyl ketone analog of arachidonic acid. It is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). By blocking the production of arachidonate and 12-hydroxyeicosatetraenoic acid in calcium ionophore-challenged platelets, AACOCF3 hinders their synthesis. Moreover, AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. Given its diverse applications, AACOCF3 ... |
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T72460
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Dimethyl L-glutamate
Dimethyl glutamate
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Dimethyl L-glutamate (Dimethyl glutamate), 一种可透膜的谷氨酸类似物，可刺激葡萄糖诱导的胰岛素 (insulin) 释放。Dimethyl L-glutamate 抑制KATP 通道的活性。Dimethyl L-glutamate 抑制E. gracilis 生长并导致细胞异常分裂。Dimethyl L-glutamate 可用于糖尿病、葡萄糖转运、磷酸化和进一步代谢的研究。 |
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TP1954
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PHM-27 (human)
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Endogenous peptide product of human prepro-VIP and analog of porcine PHI-27; potent agonist for the human calcitonin receptor (EC50 = 11 nM). Transgenic mice expressing the human VIP/PHM 27 gene in pancreatic β-islets display enhanced glucose-induced insu |
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T69953
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MK-8666 Tris
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MK-8666 Tris is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 Tris has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects. |
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T35622
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FKGK 18
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FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2). It inhibits GVIA iPLA2 by 99.9% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively. FKGK 18 inhibits iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50s = ~1-3 μM). It inhibits gl... |
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T68976
|
Piragliatin
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Piragliatin, also known as RO4389620, is a glucokinase activator. Piragliatin greatly enhances glucose-induced pancreatic islet respiration and insulin release. Piragliatin lowers plasma glucose both in the postabsorptive state and after a glucose challenge in patients with type 2 diabetes mellitus. Piragliatin has an acute glucose-lowering action in patients with mild type 2 diabetes, mainly mediated through a generalized enhancement of β-cell function and through fasting restricted changes in ... |
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T35809
|
C20 Sphingomyelin (d18:1/20:0)
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C20 Sphingomyelin is a naturally occurring sphingolipid. Levels of C20 sphingomyelin are upregulated in the hippocampus of rats with diabetes induced by streptozotocin and in human plasma where it is positively correlated with insulin resistance in obese humans. C20 sphingomyelin is also upregulated in the liver of a mouse model of Niemann-Pick type C1 disease, a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder. The plasma concentration of C20 sphingomyelin is decreased in m... |
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T35799
|
MBX-8025 (sodium salt)
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MBX-8025 is an agonist of peroxisome proliferator-activated receptor δ (PPARδ).1 It is greater than 750- and 2,500-fold selective for PPARδ over PPARα and PPARγ. MBX-8025 (10 mg/kg per day for eight weeks) reduces increases in fasting blood glucose and serum insulin levels, and decreases insulin resistance in Alms1 mutant (foz/foz) mice fed an atherogenic diet as a model of diet-induced obesity, type 2 diabetes, and non-alcoholic steatohepatitis (NASH).2 It also decreases serum alanine transamin... |
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T68808
|
11-Dehydrocorticosterone
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11-Dehydrocorticosterone is an endogenous mineralocorticoid. It increases Na+/K+-ATPase mRNA expression in vascular smooth muscle cells and inhibits aldosterone action in B. marinus toad bladder tissue in a concentration-dependent manner. 11-Dehydrocorticosterone decreases the sodium/creatine ratio and increases the potassium/creatine ratio in rat urine in a dose-dependent manner in a model of 11β-hydroxysteroid dehydrogenase inhibition induced by carbenoxolone. Chronic administration 11-dehydro... |
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T36582
|
Glucocerebrosides (Gaucher's spleen)
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Glucocerebrosides are formed by the tethering of glucose to a ceramide by glucosylceramide synthase. They are present in neuronal and non-neuronal mammalian tissues and are found at low quantities in a large number of plant species. Glucocerebrosides are precursors in the synthesis of lactosylceramides and gangliosides. Increased levels of glucocerebrosides are associated with obesity-induced insulin resistance in mice and with neuronal deficits observed in neuronopathic Gaucher disease. This pr... |
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T36586
|
12-PAHSA
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Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are newly identified endogenous lipids regulated by fasting and high-fat feeding and associated with insulin sensitivity. Structurally, these esters are comprised of a C-16 or C-18 fatty acid (e.g., palmitoleic, palmitic, oleic, or stearic acid) linked to either a C-16 or C-18 hydroxy substituent. 12-PAHSA is a FAHFA in which palmitic acid is esterified at the 12th carbon of hydroxy stearic acid. Among the FAHFA family members, PAHSAs ar... |
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T36059
|
Dichlorphenamide-13C6
Dichlorphenamide-13C6
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Dichlorphenamide-13C6is intended for use as an internal standard for the quantification of dichlorphenamide by GC- or LC-MS. Dichlorphenamide is a sulfonamide and an orally bioavailable carbonic anhydrase (CA) inhibitor (Kis = 1.20, 38, 50, and 50 nM for the human CA isoforms CAI, CAII, CAIX, and CAXII, respectively).1It lowers intraocular pressure in rabbits when 50 μl of a 10% solution is applied topically to the eye.2Dichlorphenamide rescues the potassium deficiency and prevents insulin-induc... |
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T82254
|
GSK-LSD1
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Histone Demethylase |
Chromatin/Epigenetic |
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GSK-LSD1是一种LSD1抑制剂，能够降低肥胖小鼠模型的摄食量和体重，同时提升胰岛素敏感性与血糖控制。此外，GSK-LSD1对NAFLD也有改善作用，并能抑制COVID-19患者PBMC中SARS-CoV-2诱导的细胞因子释放。GSK-LSD1对抑制癌症的生长与转移也显示出潜在效果。 |
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T83827
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Adenosine-5'-O-(3-thiotriphosphate) sodium
ATPγS,Adenosine 5'-(γ-thio)-triphosphate
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Adenosine-5'-O-(3-thiotriphosphate)（ATPγS）是一种purinergic P2Y11受体的激动剂。在表达人类或犬类P2Y11受体的CHO-K1细胞中，能够诱导肌醇磷酸累积（EC50s分别为1.2和19.3 µM）。ATPγS（10 µM）能抑制Junin病毒导致的编码骨形态生成蛋白6（BMP6）的mRNA水平增加，并减少Junin病毒感染的初代大鼠成骨细胞中的粒子形成单位（PFUs）。使用25 µM浓度时，可以诱导MIN6胰岛β细胞分泌胰岛素。 |
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T72034
|
LI-2242
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Others |
Others |
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LI-2242是一种强效肌醇六磷酸激酶（IP6K）抑制剂，对 IP6K1、IP6K2、IP6K3和 IPMK 的 IC50s 分别为31 nM、42 nM、8.7 nM 和1944 nM。LI-2242通过减少增强脂质吸收、脂质稳定和脂肪生成的基因的表达，改善了肝脏脂肪变性，增强体外脂肪细胞和肝细胞的线粒体耗氧率（OCR）和胰岛素信号传导。 LI-2242可改善饮食诱导的小鼠肥胖症、高血糖症和肝脂肪变性。LI-2242可用于研究 II 型糖尿病、肥胖症、代谢并发症、静脉血栓和精神疾病。 |
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T35787
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Obestatin (human) (trifluoroacetate salt)
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Obestatin is a 23 amino acid peptide hormone with a conserved C-terminal glycine residue and amidation site that is formed by cleavage of the ghrelin and obestatin prepropeptide.1It binds to the orphan receptor GPR39 (Kd= 1 nM) and stimulates cAMP production in CHO and HEK293 cells overexpressing human GPR39. Obestatin inhibits contraction of isolated mouse jejunum muscle strips induced by ghrelin .In vivo, obestatin (12.5-1,000 nmol/kg) suppresses food intake in a time- and dose-dependent manne... |
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T36427
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PACAP (6-27) (human, chicken, mouse, ovine, porcine, rat) (trifluoroacetate salt)
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PACAP |
GPCR/G Protein |
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Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, ... |
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T83802
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TNP-ATP sodium
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TNP-ATP是ATP的衍生物，同时是嘌呤P2Y1、P2X3和P2X2/3受体的拮抗剂（IC50s分别为6、0.9和7 nM，在表达人类受体的HEK293细胞中）。该化合物相对于嘌呤P2X2、P2X4和P2X7受体显示出选择性（IC50s分别为2、15.2和>30 µM，在表达人类受体的HEK293细胞中）。TNP-ATP能降低表达P2X3和P2X2/3受体的1321N1细胞中乙酸诱导的钙流量（IC50s分别为100和62 nM）。它还可以减轻小鼠模型中由乙酸诱发的痛性绞曲（ED50 = 6.35 µmol/kg）。在403 nm激发下，其发射最大峰值为547 nm，当结合于胰岛素降解酶（IDE）时，其相对荧光强度增加四倍，并且发射峰移至538 nm。 |
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T83825
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Trofinetide acetate
NNZ-2566
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Trofinetide是一种衍生自具有神经保护作用的三肽Gly-Pro-Glu的化合物，后者是胰岛素样生长因子-1（IGF-1）的N-端序列。在10 nM的浓度下使用时，它能减少由蛋白磷酸酶抑制剂奥卡达酸在原代大鼠胚胎纹状体神经元中引起的细胞死亡。Trofinetide在一种由穿透性弹道样脑损伤引起的大鼠神经炎症模型中减少了编码IL-1β、TNF-α、IL-6和E-selectin的mRNA的脑表达。在通过中脑动脉闭塞（MCAO）引起的大鼠脑损伤模型中，以30和60 mg/kg的剂量给药时，它减少了皮层和纹状体梗塞区域。Trofinetide（每天100 mg/kg）减少了树突棘的数量，并逆转了在fmr1-/-敲除小鼠脆性X综合征模型中的社交识别和情景恐惧条件反射的缺陷，同时也减少了睾丸重量的增加。含有Trofinetide的制剂已被用于治疗Rett综合征。 |
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T35874
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CC260
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CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research[1].
In cultured C2C12 myotubes, CC260 (20 μM) enhances Insulin-induced Akt phosphorylation at both Thr-308 and Ser-473 but suppresses S6K phosphorylation (Thr-389) by mTORC1[1]. CC260 (2.5 μM, 5 μM, 10 μM, 20 μM) significantly increases phosph... |
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