plasma insulin

Sari 59-801 是具有口服活性的降血糖化合物，能够降低几个物种的血糖，且可以提高大鼠和小鼠的血浆中胰岛素水平。

(2S,3R,4S)-4-Hydroxyisoleucine (Hydroxyisoleucine) 是分离自胡芦巴中的一种可口服的有效成分，具有抗糖尿病、抗糖尿病肾病的作用。

Propane-1,2,3-triyl tripalmitate (Glycerol Tripalmitate) 是内源性代谢产物的一种。

APX-115 free base (Ewha-18278 free base) 是口服具有活性的、非选择性的 Nox 抑制剂，对 Nox1，Nox2和 Nox4的 Ki 分别为 1.08 μM，0.57 μM 和 0.63 μM。它能够有效预防糖尿病小鼠的肾损伤。

Gosogliptin（戈格列汀）是一种有效的口服活性、高度选择性和竞争性的DPP-4（二肽基肽酶4）抑制剂，提高肠促胰岛素肽(GLP-1)和葡萄糖依赖性促胰岛素多肽（GIP）的水平，从而增强胰岛素分泌并降低血糖水平。在动物实验中，Gosogliptin能够快速可逆地抑制血浆DPP-4活性。

ISO24 指的是以 24 ng kg min 的速率输注异丙肾上腺素。经过 120 分钟的输注后，ISO24 会导致血浆瘦素含量降低27%。同时，ISO24 还能增加血浆胰岛素的水平。

Efaroxan hydrochloride（盐酸盐依法克生）是Efaroxan的盐形式。Efaroxan 是一种选择性、可口服的α2 肾上腺素受体 (α2-adrenoceptor) 拮抗剂，可提高静息血浆胰岛素水平，并显著增强肾上腺素诱导的胰岛素水平升高。

BMS-695735, a benzimidazole inhibitor of insulin-like growth factor-1 receptor, has broad-spectrum antitumor activity in vivo. It was found that BMS-695735 had strong inhibition of CYP3A4, induction of CYP3A4 mediated by PXR transactivation, poor water so

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。

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 women. In vitro, osteocalcin induces chemotaxis of MDA-MB-231 breast cancer cells, human peripheral blood monocytes, and rat osteosarcoma cells with osteoblast-like characteristics. It is also expressed by vascular smooth muscle cells (VSMCs) displaying an osteoblast-like phenotype and has been positively associated with calcification of aortic tissue and heart valves in humans.

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 manner and reduces body weight gain and gastric emptying in mice. Obestatin (0.22 g per animal) also reduces food intake and glucose response without affecting plasma insulin responses in fasted high-fat diet fed mice.2 1.Zhang, J.V., Ren, P.C., Avsian-Kretchmer, O., et al.Obestatin, a peptide encoded by the ghrelin gene, opposes ghrelin's effects on food intakeScience310(5750)996-999(2005) 2.Subasinghage, A.P., Green, B.D., Flatt, P.R., et al.Metabolic and structural properties of human obestatin {1-23} and two fragment peptidesPeptides31(9)1697-1705(2010)

C16 Lactosylceramide is an endogenous bioactive sphingolipid. It forms membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs), suggesting a role in cell signaling. Plasma levels of C16 lactosylceramide are elevated in insulin-resistant cattle. C16 Lactosylceramide is also upregulated in a mouse model of Niemann-Pick type C1 disease, a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder.

C18:1 Ceramide (d18:1 18:1(9Z))是一种神经酰胺，C18:1-Ceramide水平在超重和胰岛素抵抗小鼠和牛以及晚期卵巢癌患者血浆和卵巢组织中升高。

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 men with prostate cancer.

Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties. In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 μM. Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity.

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, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.

Glucocerebrosides (Gaucher cerebroside) 是一种从萨摩柑橘 （Citrus unshiu） 果实中分离得到的化合物，是大多数真核细胞内膜系统和质膜的主要成分，对胰岛素信号传导有拮抗作用。

Lysophosphatidylcholine 18:2是一种小鼠代谢物，在功能上与亚油酸有关。1-亚油酰-2-羟基-SN-甘油-3-卵磷脂是氧化低密度脂蛋白的主要成分，​​​血浆中低水平的18:2 LysoPC与糖耐量受损、胰岛素抵抗、2 型糖尿病和冠状动脉疾病等代谢紊乱相关。1-Linoleoyl-2-Hydroxy-sn-glycero-3-PC同时也是Autotaxin(LysoPLD)生成溶血磷脂酸(LPA)的底物，在细胞运动中起重要作用。

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, 5, or 50 pmol min kg. Further, infusion of GLP-1(7-37) for 60 mins produced a small transitory increase in plasma insulin concentration in fasted rats and fed rats and a slight transitory decrease in plasma glucose concentration. Moreover, GLP-1(7-37) (5 pmol min kg IV) infusion for 6 h in Sprague-Dawley rats produced a sustained increase in plasma insulin concentration relative to levels in rats infused with vehicle[1].

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.

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).

BI-2081是一种GPR40 (FFAR1)部分激动剂，具有EC50值为4 nM。该化合物能诱导葡萄糖依赖性胰岛素释放，并降低血浆中葡萄糖含量，适用于研究代谢疾病，尤其是2型糖尿病。

GRPP (human)为含有30个氨基酸的Gcg衍生肽。该化合物能引起血浆胰岛素的轻微上升及血浆胰高血糖素的轻微降低，但不会影响大鼠胰岛内的胰岛素分泌。

Hylambatin是一种速激肽，它能够促进血浆葡萄糖和胰岛素的分泌，但不影响胰高血糖素的释放。该化合物通常用于糖尿病相关的研究。