pancreatic β cell

RH01687 是可以保护胰腺 β 细胞免受内质网应激诱导的细胞死亡的化合物。它对糖尿病具有潜在的研究价值。

Streptozotocin (Streptozocin, NSC-85998) 是一种抗生素，能够通过葡萄糖转运体（GLUT2）进入胰岛β细胞并诱导DNA甲基化，导致β细胞凋亡，对胰岛素产生细胞具有毒性，常用于构建糖尿病动物模型，且该产品在溶液中不稳定，建议现配现用。

PX-478 是一种 HIF-1α 抑制剂，具有选择性、口服活性和血脑屏障渗透性。PX-478 具有抗肿瘤活性，还可以保护糖尿病中的胰腺 β 细胞功能，用于 2 型糖尿病的研究。

Imeglimin (EMD 387008) 是一种可口服的抗糖尿病化合物，可增强线粒体功能、增强胰岛素分泌、促进β细胞增殖并改善小鼠胰岛β细胞存活率。

Dorzagliatin (HMS5552) 是双重作用的葡萄糖激酶 (glucokinase;GK) 激活剂，可改善 2 型糖尿病的血糖控制，提高胰腺 β 细胞功能。

WS3 是一种可促进鼠和人原代胰岛的胰腺 β 细胞增殖的增殖分子。它可用于研究 I 型糖尿病。

ZP3022是一种兼具glucagon-like peptide 1 receptor (GLP-1R)和cholecystokinin 2 (CCK2) receptor的激动剂。它在表达GLP-1R或CCK2 receptor的HEK293细胞中，选择性增加cAMP积累或ERK磷酸化，而在表达CCK1 receptor的HEK293细胞中，该作用较弱（人类受体的EC50分别为0.02, 10.3和>1,000 nM）。ZP3022（40 nM）在体外实验中促进大鼠新生β细胞的增殖，并在大鼠胰岛中以10和100 nM浓度应用时增强葡萄糖诱导的胰岛素分泌（GSIS），同时以40 nmol/kg剂量每日两次给药可减少大鼠体重。在db/db小鼠中，每日100 nmol/kg剂量的ZP3022增加β细胞和胰腺总体积，同时改善葡萄糖耐量。此外，它在db/db小鼠中降低食物摄入量，但不影响体重。

Linogliride 是一种基于胍的胰岛素分泌抑制剂，也是 pirogliride 的结构类似物，具有降血糖活性。它可以阻断胰腺β细胞膜上对 ATP 敏感的钾通道，从而刺激胰岛素分泌并改善葡萄糖耐受性。

Linogliride fumarate 是Linogliride 的富马酸盐。Linogliride 是一种基于胍的胰岛素分泌抑制剂，也是pirogliride 的结构类似物，具有降血糖活性。它可以阻断胰腺β细胞膜上对ATP 敏感的钾通道，从而刺激胰岛素分泌并改善葡萄糖耐受性。

BRD0476 is a suppressor of pancreatic β-cell apoptosis. BRD0476 inhibits interferon-gamma (IFN-γ)-induced Janus kinase 2 (JAK2) and signal transducer and activation of transcription 1 (STAT1) signaling to promote β-cell survival. BRD0476 inhibits JAK-STAT

KM10103 exhibits β-cell-protective activities against ER stress, which plays an important role in the decline in pancreatic β cell function and mass observed in type 2 diabetes.

WB403 is a TGR5 activator. WB403 significantly decreases fasting blood glucose, postprandial blood glucose and HbA1c, improves glucose tolerance in type 2 diabetic mice. WB403 increases pancreatic β-cells and restores the normal distribution pattern of α-

Rhein-13C4 is intended for use as an internal standard for the quantification of rhein by GC- or LC-MS. Rhein is an anti-inflammatory anthraquinone found in rhubarb and is the bioactive derivative of its prodrug diacerein . At 10 μM, rhein inhibits IL-1β signaling, suppressing signaling through NF-κB, and reduces the expression of the matrix metalloproteases MMP-1 and MMP-13.1 It inhibits IKKβ (IC50 = 11.8 μM), decreasing iNOS and IL-6 expression in LPS-stimulated macrophages but paradoxically increasing TNF-α, IL-1β, and HMBG1 expression.2 Rhein shows efficacy against pancreatic fibrosis, chronic pancreatitis, and hyperglycemia-induced pancreatic β-cell apoptosis.3,4 It also inhibits angiogenesis of breast cancer cells under normoxic and hypoxic conditions.5

Amylin (8-37), human, derived from human Amylin, possesses direct vasodilator effects in isolated mesenteric resistance arteries of rats. Human Amylin is a small pancreatic β-cell hormone that forms aggregates in the absence of insulin and is a key pathological feature of type II diabetes mellitus.

Amylin (8-37), human acetate(135702-23-7 free base) 源自人 Amylin，对大鼠离体肠系膜阻力动脉具有直接血管舒张作用。 Amylin (8-37), human acetate，是一种小型胰腺 β 细胞激素，在没有胰岛素的情况下会形成聚集体，是 II 型糖尿病的一个关键病理特征。

DIM-C-pPhOH (CDIM8) 是一种核受体 4A1(NR4A1) 拮抗剂，可降低细胞增殖，对 ACHN 细胞和 786-O 细胞的IC50值分别为 13.6 μM 和 13.0 μM。它抑制癌细胞的生长和 mTOR 信号传导，诱导细胞凋亡和细胞应激。

Vin-C01 可用于研究Ⅱ型糖尿病，是胰腺 β 细胞的有效保护剂 (EC 50 = 0.22 μM)。Vin-C01 保护 β 细胞免受 STZ 诱导的细胞凋亡，并有效促进 β 细胞存活。

Vin-F03 可用于研究2型糖尿病，它是胰腺 β 细胞的有效保护剂 (EC50 = 0.27 μM)。Vin-F03 有效促进 β 细胞存活并且保护 β 细胞免受 STZ 诱导的细胞凋亡。

GKA50 quarterhydrate 是一种有效的葡萄糖激酶激活剂，其 EC50 值为 33 nM。GKA50 quarterhydrate 是一种啮齿动物和人类胰岛中 β 细胞代谢的葡萄糖样激活剂，也是一种 Ca2+依赖性胰岛素分泌调节剂。GKA50 quarterhydrate 能够刺激小鼠胰岛分泌胰岛素，可以显著降低高脂喂养的雌性大鼠血糖。

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 glucose turnover.

Cinnamic acid, hydrazide is an unsaturated carboxylic acid and precursor to aspartame via enzyme-catalysed amination to phenylalanine. Cinnamic acid may be useful in prevention or treatment of Diabetes through various mechanism of actions including stimulation of insulin secretion, improvement of pancreatic β-cell functionality, inhibition of hepatic gluconeogenesis, enhanced glucose uptake, increased insulin signaling pathway, delay of carbohydrate digestion and glucose absorption, and inhibition of protein glycation and insulin fibrillation.

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 resistance induced by hydrogen peroxide. Gliclazide (5 and 10 μg/ml) reduces LDL oxidation by human aortic smooth muscle cells (HASMCs), decreasing TBARS content and 8-isoprostane levels. It also decreases oxidized LDL-induced HASMC proliferation and monocyte adhesion when used at concentrations ranging from 1 to 10 μg/ml. Gliclazide (5 mg/kg) reduces serum glucose levels and increases glucose uptake by isolated rat hindquarters in a model of diabetes induced by streptozotocin (STZ).

Amylin (1-37) (human) (hIAPP (1-37)) 为胰岛β细胞分泌颗粒中的肽类激素，其C端经酰胺化处理，第2和第7个半胱氨酸残基间形成二硫键。

GIP, rat TFA 是一种源自大鼠的生物活性肽。GIP（Glucose-dependent Insulinotropic Polypeptide，又名 Gastric Inhibitory Polypeptide）是由十二指肠与空肠中的K细胞在摄食后释放的一种含42个氨基酸的多肽。作为肠促胰岛素激素肽家族的一部分，GIP和GLP（Glucagon-Like Peptide）共同调控胰岛β细胞的胰岛素分泌，并可能促进β细胞扩增及存活。此外，近期研究显示GIP参与调节脂质平衡，并可能在肥胖的病理生理中扮演角色。