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22

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T33412	MitoPQ MitoParaquat	Glucokinase; transporter	Metabolism
	MitoPQ (MitoParaquat) 是一个线粒体靶向的小分子化合物。MitoPQ 选择性加强线粒体超氧化物和过氧化氢的含量，抑制胰岛素刺激的葡萄糖摄取和葡萄糖转运蛋白 4 (GLUT4）向脂肪细胞和肌管中质膜的易位。MitoPQ 可用于研究线粒体氧化应激与调节的 GLUT4 转运。
T13867	RH01386	Others	Others
	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。
T17177	TUG-424 TUG424	Others	Others
	TUG-424 是一种有效且选择性的游离脂肪酸受体 1 (FFA1/GPR40) 激动剂，EC50 为 32 nM。TUG-424 在 100 nM 处显著增加葡萄糖刺激的胰岛素分泌。TUG-424 可能有助于探索 FFA1 在糖尿病或肥胖等代谢性疾病中的作用。
T12853	SBI-477	Others	Others
	SBI-477 是化学探针，能够使转录因子MondoA 失活，刺激胰岛素信号传导，使胰岛素途径抑制剂硫氧还蛋白相互作用蛋白和抑制蛋白结构域 4 的表达降低。它能够协调地抑制三酰基甘油酯合成，促进人骨骼肌细胞中的基础葡萄糖摄取。
TP2258	HNGF6A	Others	Others
	increases glucose stimulated insulin secretion and glucose metabolism
T70113	ATM-1001
	ATM-1001 is an inhibitor of the cancer-associated tropomyosin 3.1 (Tpm3.1), suppressing glucose-stimulated insulin secretion (GSIS) from the pancreatic islets.
T17094	Tifenazoxide NN414	Others	Others
	Tifenazoxide is an effective and SUR1/Kir6.2 selective KATP channels opener. Tifenazoxide has an anti-diabetic effect, can inhibit glucose-stimulated insulin release in vitro and in vivo.
TP2020	[Pro3]-GIP (Mouse)
	GIP receptor antagonist (IC50 = 2.6μM). Inhibits GIP-stimulated insulin release from pancreatic β cells in vitro. In ob/ob mice, blocks the effects of GIP on insulin release and plasma glucose levels. Also improves intraperitoneal glucose tolerance, insul
T62836	Hit 1
	Hit 1 是一种胰岛素降解酶 (IDE) 的激活剂 (EC50: 5.5 μM)，能够降低刺激葡萄糖的胰岛素分泌。
T71251	DS-1558
	DS-1558 is a potent and orally available GPR40 agonist.DS-1558 was found to have potent glucose lowering effects during an oral glucose tolerance test in ZDF rats. DS-1558 significantly and dose-dependently improved hyperglycemia and increased insulin secretion during the oral glucose tolerance test in Zucker fatty rats, the model of insulin resistance and glucose intolerance. DS-1558 not only increased the glucose-stimulated insulin secretion by GLP-1 but also potentiated the maximum insulinog...
T75833	HNGF6A TFA
	HNGF6A TFA 是一种人类素类似物。HNGF6A TFA 可以增加葡萄糖刺激的胰岛素分泌和葡萄糖代谢，并可用于糖尿病的研究。HNGF6A TFA 在氧化应激期间抑制ROS 的产生。HNGF6A TFA 可以在体内预防内皮功能障碍和动脉粥样硬化。
TP2033	[Des-His1,Glu9]-Glucagon amide des-His1-[Glu9]-Glucagon (1-29) amide
	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
T76326	[Des-His1,Glu9] Glucagon
	[Des-His1,Glu9] Glucagon 是一种有效的胰高血糖素受体系统多肽拮抗剂。[Des-His1,Glu9] Glucagon 增强胰岛细胞在葡萄糖刺激下释放胰岛素。[Des-His1,Glu9] Glucagon 可用于糖尿病的研究。
T80766	Xenin-8 TFA
	Xenin-8 TFA为Xenin的C端八肽段，同时是其生物活性片段。该化合物隶属于神经降压素/xenopsin家族多肽中。它能激发基础胰岛素的分泌并剂量依赖性地加强胰岛素对葡萄糖反应(EC50=0.16 nM)。
T35604	Osteocalcin (1-49) (human) (trifluoroacetate salt)
	Osteocalcin (1-49) is a non-collagenous peptide that is secreted by osteoblasts and odontoblasts and comprises 1-2% of the total protein in bone. Secretion of osteocalcin (1-49) is stimulated by 1,25-dihydroxy vitamin D and plasma levels increase in diseases that induce dysregulated bone turnover such as osteoporosis, Paget's disease, and primary hyperparathyroidism. Osteocalcin (1-49) is positively correlated with insulin sensitivity and negatively correlated with high blood glucose levels in w...
T35854	9(Z),11(E)-Conjugated Linoleic Acid (sodium salt)
	9(Z),11(E)-Conjugated linoleic acid is an isomer of linoleic acid that has been found in beef and milk fat.1It binds to peroxisome proliferator-activated receptor α (PPARα; IC50= 140 nM) and activates the receptor in a reporter assay using COS-1 cells expressing mouse PPARα when used at a concentration of 100 μM.29(Z),11(E)-Conjugated linoleic acid inhibits TNF-α-inducedGLUT4expression and increases insulin-stimulated glucose transport in 3T3-L1 adipocytes.3Dietary administration of 9(Z)11(E)-co...
T64553	GLP-1(7-37) TFA salt
	The truncated glucagon-like peptides GLP-1(7-37) is naturally occurring peptide product of the preproglucagon gene that are synthesized primarily in the intestine and acts as incretin that are released from the intestine into the bloodstream in response to food and stimulate insulin secretion. GLP-1(7-37) produced a dose-related enhancement of the glucose-stimulated increase in plasma insulin concentration and an increased rate of glucose infusion in Sprague-Dawley Rats at a dosing rang of 0.5, ...
T78066	BBT	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	BBT是一种增强剂，用于改善受损的葡萄糖刺激胰岛素分泌(GSIS)。该化合物展现出抗高血糖的活性，并能在2型糖尿病模型中，对β细胞起到保护作用，抵御细胞因子或链脲佐菌素(STZ)引起的细胞死亡。BBT的作用机制涉及通过cAMP/PKA及持久（L型）电压依赖性Ca2+通道/CaMK2通路。
T83694	Gastric Inhibitory Peptide (1-42) (porcine) TFA GIP (1-42),Glucose-dependent Insulinotropic Polypeptide (1-42)
	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。
T37579	GW 1929 hydrochloride
	Highly selective orally active peroxisome proliferator-activated receptor (PPAR)γ agonist (pEC50 values are 8.05, < 4 and < 4 for human PPARγ, PPARα and PPARδ receptors respectively). Decreases glucose, fatty acid and triglyceride levels following oral administration in vivo. Brown et al (1999) A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-γ reverses the diabetic phenotype of the Zucker diabetic fatty rat. Diabetes 48 1415 PMID:10389847 \|Nugent et al (2001) Pote...
T35598	Neuromedin U-25 (human) (trifluoroacetate salt)
	Neuromedin U (NMU) is a neuropeptide first demonstrated to drive smooth muscle contraction.1Translated as a 174 amino acid propeptide, NMU is cleaved to different lengths in different animals. It has diverse receptor-mediated rolesin vivo, as it regulates feeding, vasoconstriction, nociception, and bone remodeling and contributes to obesity, cancer and septic shock.2,2NMU-25 is the active form of NMU in humans. It binds with high affinity to receptors on human left ventricle and coronary artery ...
T35814	Urocortin III (human) (trifluoroacetate salt)
	Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively)....

化合物

Cat.No: T33412

Synonym: MitoParaquat

Target: Glucokinase, transporter

Cat.No: T13867

Target: Others

Cat.No: T17177

Synonym: TUG424

Target: Others

Cat.No: T12853

Target: Others

Cat.No: TP2258

Target: Others

Cat.No: T70113

Cat.No: T17094

Synonym: NN414

Target: Others

[Pro3]-GIP (Mouse)

Cat.No: TP2020

Cat.No: T62836

Cat.No: T71251

Cat.No: T75833

[Des-His1,Glu9]-Glucagon amide

Cat.No: TP2033

Synonym: des-His1-[Glu9]-Glucagon (1-29) amide

[Des-His1,Glu9] Glucagon

Cat.No: T76326

Cat.No: T80766

Osteocalcin (1-49) (human) (trifluoroacetate salt)

Cat.No: T35604

9(Z),11(E)-Conjugated Linoleic Acid (sodium salt)

Cat.No: T35854

GLP-1(7-37) TFA salt

Cat.No: T64553

Cat.No: T78066

Target: Calcium Channel

Gastric Inhibitory Peptide (1-42) (porcine) TFA

Cat.No: T83694

Synonym: GIP (1-42),Glucose-dependent Insulinotropic Polypeptide (1-42)

GW 1929 hydrochloride

Cat.No: T37579

Neuromedin U-25 (human) (trifluoroacetate salt)

Cat.No: T35598

Urocortin III (human) (trifluoroacetate salt)

Cat.No: T35814

Cat. No.	Product Name	Target	Signaling Pathways
T1286	Vincamine Angiopac,Oxybral,Devincan,Novicet,Equipur,长春胺,Perval	GPR; Others	Endocrinology/Hormones; GPCR/G Protein; Others
	Vincamine (Perval) 是从长春花中提取的单萜类吲哚生物碱，可作为外周血管扩张剂，对脑微血管循环有选择性的血管调节作用。它可改善体内葡萄糖稳态，对 2 型糖尿病具有研究潜力。它是GPR40激动剂，通过改善 β 细胞功能障碍和促进葡萄糖刺激型胰岛素分泌发挥 β 细胞保护作用。
T2755	Rhoifolin 野漆树苷,Apigenin-7-O-rhamnoglucoside,Apigenin 7-O-neohesperidoside,Rhoifoloside	Others; p38 MAPK; NF-κB; transporter; IGF-1R; Autophagy	Autophagy; MAPK; Metabolism; NF-κB; Others; Tyrosine Kinase/Adaptors
	Rhoifolin (Apigenin 7-O-neohesperidoside) 是从琯溪蜜柚叶子分离的一种黄酮糖苷。它通过 RANKL 诱导的NF-κB 和MAPK 途径改善钛颗粒刺激的骨溶解并减少破骨细胞生成。它通过增强脂联素分泌，胰岛素受体-β的酪氨酸磷酸化和GLUT4易位有助于治疗糖尿病并发症。
T3S0381	Chrysophanol 8-O-glucoside	Serine Protease	Proteases/Proteasome
	Chrysophanol 8-O-glucoside 来自Rumex acetosa 根部，具有中等的弹性蛋白酶抑制特性。它具有温和的细胞毒性和抗糖尿病特性，能够在胰岛素刺激的葡萄糖转运途径中发挥代谢作用。
TWO2727	Propane-1,2,3-triyl tripalmitate Palmitic Triglyceride,Tripalmitin,Tripalmitoylglycerol,Glycerol Tripalmitate,三棕榈酸甘油酯	Others; Endogenous Metabolite	Metabolism; Others
	Propane-1,2,3-triyl tripalmitate (Glycerol Tripalmitate) 是内源性代谢产物的一种。
TN4584	Morolic acid	IL Receptor; COX; HIV Protease	Immunology/Inflammation; Microbiology/Virology; Neuroscience; Proteases/Proteasome
	Morolic acid and moronic acid have shown sustained antidiabetic and antihyperglycemic action possibly mediated by an insulin sensitization with consequent changes of glucose, cholesterol and triglycerides, in part mediated by inhibition of 11β-HSD 1. Moro

天然产物

Cat.No: T1286

Synonym: Angiopac,Oxybral,Devincan,Novicet,Equipur,长春胺,Perval

Target: GPR, Others

Cat.No: T2755

Synonym: 野漆树苷,Apigenin-7-O-rhamnoglucoside,Apigenin 7-O-neohesperidoside,Rhoifoloside

Target: Others, p38 MAPK, NF-κB, transporter, IGF-1R, Autophagy

Chrysophanol 8-O-glucoside

Cat.No: T3S0381

Target: Serine Protease

Propane-1,2,3-triyl tripalmitate

Cat.No: TWO2727

Synonym: Palmitic Triglyceride,Tripalmitin,Tripalmitoylglycerol,Glycerol Tripalmitate,三棕榈酸甘油酯

Target: Others, Endogenous Metabolite

Cat.No: TN4584

Target: IL Receptor, COX, HIV Protease

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