pancreatic α

ABzOH 是一种苯甲酸衍生物，结构类似于阿司匹林等非甾体抗炎药，具有抗炎、抗肿瘤和抗增殖作用。ABzOH 不仅可以抑制肿瘤坏死因子- α (TNF-a)、白细胞介素-1β (IL-1β)和白细胞介素-6 (IL-6)等促炎细胞因子的表达还对乳腺癌、肺癌和胰腺癌具有抑制作用。

Ethyl trans-caffeate (Caffeic Acid Ethyl Ester) 具有抗炎作用。 它是一种有前途的天然化合物，未来在慢性肝病中的应用。它是一种有效的化学预防化合物，可防止因太阳紫外线照射引起的皮肤癌变。它是与人胰腺α-淀粉酶复合的代表性抑制剂的高分辨率结构。 它强烈抑制 JB6 Cl41细胞的肿瘤转化，无毒性。 PI3K、ERK1 2 和 p38 激酶活性在体外通过与 HOEC 直接结合而受到抑制。

E3330 是一种口服有效的选择性 AP 内切核酸酶 1 (APE1; REF-1) 抑制剂，可抑制NF-κB DNA 结合活性。它阻断 TNF-α 诱导的肝癌细胞系中 IL-8 的激活，可以抑制癌细胞的生长和迁移，具有抗癌活性。

Glucagon (1-29), bovine, human, porcine hydrochloride 是一种由胰腺 α 细胞产生的多肽激素。它可激活 HNF4α 并促进 HNF4α 磷酸化，促进糖异生。

Devimistat (6,8-Bis(benzylthio)octanoic acid) 是一种线粒体代谢抑制剂，还是一种lipoic acid 拮抗剂，能阻断线粒体能量代谢，诱导多种癌细胞凋亡。

Pancreatic Polypeptide (human) acetate 是一种 C 末端酰胺化的 36 个氨基酸肽，可作为神经肽 Y (NPY) Y4 Y5 受体激动剂。

Pancreatic Polypeptide, rat acetate 是 NPY 受体的激动剂，对 NPYR4 具有高亲和力。

Agonist at Y4 neuropeptide Y receptors.

Pancreatic polypeptide 是由胰腺内分泌的 PP 细胞所分泌的多肽，具有调节胰腺分泌功能、影响肝糖原储存及胃肠分泌的作用。

Pancreatic lipase Carboxylesterase 1-IN-1 (Compound 39) 是一种有效的、双重的胰脂酶 (PL) 和人羧酸酯酶 1A (hCES1A) 抑制剂，作用于 PL (IC50: 2.13 μM) 和 hCES1A (IC50: 0.055 μM)。

Pancreatic Polypeptide, rat, is an agonist of the NPY receptor with high affinity at NPYR4. Pancreatic polypeptide (PP) is a 36-amino acid, C-terminally amidated peptide, and a member of the PP-fold peptide family, produced and secreted by the PP cells.

Endogenous high affinity agonist for human NPY Y4 receptor (Ki = 0.056 nM). Believed to play an important role in the function of the gastrointestinal tract.

GLP-1 amide is a peptide hormone cleaved from proglucagon in the pancreas.1,2 Mice lacking the glucagon receptor (Gcgr-/-) have approximately nine-fold higher levels of total GLP-1 amide, including GLP-1 (1-36) amide and truncated GLP-1 (7-36) amide , in pancreatic tissue compared to wild-type mice.2References1. Schjoldager, B.T., Mortensen, P.E., Christiansen, J., et al. GLP-1 (glucagon-like peptide 1) and truncated GLP-1, fragments of human proglucagon, inhibit gastric acid secretion in humans. Dig. Dis. Sci. 34(5), 703-708 (1989).2. Gelling, R.W., Du, X.Q., Dichmann, D.S., et al. Lower blood glucose, hyperglucagonemia, and pancreatic α cell hyperplasia in glucagon receptor knockout mice. Proc. Natl. Acad. Sci. U.S.A. 100(3), 1438-1443 (2003). GLP-1 amide is a peptide hormone cleaved from proglucagon in the pancreas.1,2 Mice lacking the glucagon receptor (Gcgr-/-) have approximately nine-fold higher levels of total GLP-1 amide, including GLP-1 (1-36) amide and truncated GLP-1 (7-36) amide , in pancreatic tissue compared to wild-type mice.2 References1. Schjoldager, B.T., Mortensen, P.E., Christiansen, J., et al. GLP-1 (glucagon-like peptide 1) and truncated GLP-1, fragments of human proglucagon, inhibit gastric acid secretion in humans. Dig. Dis. Sci. 34(5), 703-708 (1989).2. Gelling, R.W., Du, X.Q., Dichmann, D.S., et al. Lower blood glucose, hyperglucagonemia, and pancreatic α cell hyperplasia in glucagon receptor knockout mice. Proc. Natl. Acad. Sci. U.S.A. 100(3), 1438-1443 (2003).

Certepetide (CEND-1)，即双功能环肽（a.k.a. iRGD），是一种具有穿透肿瘤功能的多肽。通过与α-V整联蛋白（alphav-integrins）的RGD motif相互作用，以及激活神经纤毛蛋白1（NRP-1），Certepetide能够将实体瘤微环境转化成临时的活性分子通道，从而在肿瘤中累积。该化合物在胰腺癌和其他实体瘤的研究中具有应用潜力。

Orlistat-d3 is intended for use as an internal standard for the quantification of orlistat by GC- or LC-MS. Orlistat is a digestive lipase inhibitor. It inhibits diacylglycerol lipase α (DAGLα), DAGLβ, α/β-hydrolase domain-containing protein 12 (ABHD12), ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH; IC50s = 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively), as well as pancreatic lipase and hormone-sensitive lipase (IC50s = 0.65 and 2.1 µg/ml, respectively) but does not inhibit fatty acid amide hydrolase (FAAH) or KIAA1363 (IC50s = >100 µM for both). Orlistat decreases ionomycin-induced production of the endocannabinoid 2-arachidonoyl glycerol (2-AG) in N18TG2 murine neuroblastoma cells when used at a concentration of 1 µM. It also inhibits fatty acid synthase (FASN; Kiapp = ~0.1 µM for the human enzyme) and the proliferation of PC3 prostate cancer cells in a concentration-dependent manner. Orlistat (10 mg/kg) decreases serum cholesterol levels and total bod......

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

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-

Rosolic Acid是Nrf2及其下游靶点的激活剂，能够提升血管生成因子的水平，并降低TNF-α和IL-1β等炎症标志物以及CXCL10和CCL2等凋亡标志物的水平。同时，Rosolic Acid能够恢复胰腺细胞功能，并对受到内质网应激影响的内皮细胞(EC)提供保护。

HPA-IN-1 (Compound 1)为高效、选择性的人类胰腺α淀粉酶(HPA)抑制剂，其对HPA及α-glucosidase的IC50值分别为12.0 μM与410.4 μM。

Glucagon, a peptide hormone derived from proglucagon in pancreatic α cells, regulates glucose metabolism. It stimulates glucose production in rat hepatocytes ex vivo and enhances glucose output from perfused rat livers through elevated gluconeogenesis and glycogenolysis, while reducing glycolysis, and raises plasma glucose levels in rats. Glucagon secretion decreases following food intake in healthy rats and humans, yet remains unchanged or increases in individuals with type 2 diabetes.

G3-CNP is a colorimetric substrate for α-amylases.1Upon hydrolysis by α-amylases, 2-chloro-4-nitrophenol is released which can be quantified by colorimetric detection at 405 nm as a measure of enzyme activity. G3-CNP has been used to characterize the activity of human pancreatic or salivary amylase.

Glucagon is a peptide hormone, produced by pancreatic α-cells. Glucagon reduces the activity of HNF-4. Glucagon stimulates gluconeogenesis. Glucagon enhances HNF4α phosphorylation.

α-Thevetin B（Compound 24）, 一种从Thevetia peruviana分离得到的心脏苷，用于肺癌、胃癌和胰腺癌的研究。

5,4'-Dihydroxy-3,4,3'-trimethoxybibenzyl (compound 8) 是从漏斗石斛 (D. infundibulum) 中分离出的化合物。该化合物不具有对 α-葡萄糖苷酶和胰脂肪酶的抑制活性。