streptozotocin

Streptozocin (NSC-85998) 是一种抗生素，可诱导 DNA 甲基化。Streptozocin 对产生胰岛素的胰岛 B 细胞具有毒性，常用于构建 1 型糖尿病的动物模型。该产品在溶液中不稳定，建议现配现用。

Anandamide ((5Z,8Z,11Z,14Z)-N-(2-Hydroxyethyl)icosa-5,8,11,14-tetraenamide) 是一种免疫调节剂，通过大麻素受体 CB1 和 CB2 起作用，还通过中枢神经系统中的其他靶点起作用，如 GPR18 GPR55。

Glibornuride 是对 ATP 敏感的 K+通道 (KATP 通道) 阻滞剂，pKi 为 5.75。Glibornuride 显示抗糖尿病活性。

LP-935509 是一种选择性、脑渗透性、小分子接头蛋白-2 相关激酶 1 (AAK1) 竞争性抑制剂，能抑制 articulin-2-associated kinase 1 (AAK1)，其 IC50值为3.3 nM，Ki值为0.9 nM。LP-935509 是 BIKE 的强效抑制剂（IC50值为14 nM）和 GAK 的中度抑制剂（IC50值320±40 nM）。

o-Phenanthroline (1,10-Phenanthroline) 是一种金属螯合剂，能够与 Fe2+形成红色螯合物，在 510 nm 处最大吸收，可防止链脲佐菌素诱导染色体畸变。它也是一种MMP 的抑制剂。

6-Hydroxyflavanone 是从菖蒲叶中提取分离，通过靶向环氧合酶-2（COX-2），5-脂氧合酶（5-LOX）以及阿片类药物和 GABA-A 受体从而具有抗炎和抗神经性疼痛活性。6-Hydroxyflavanone 在链脲佐菌素诱导的糖尿病神经病变模型中具有抗伤害感受特性。

Virginiamycin S1 是由弗氏链霉菌产生的链阳菌素 B 型抗生素， 具有抗菌活性，通过在氨酰基-tRNA 结合和肽键形成的水平上抑制细菌蛋白质合成。

Mahanimbine 存在于Murraya koenigii 的根、叶和茎中，是从Murraya koenigii 中的提取的一种具有口服活性的生物碱。Mahanimbine 具有乙酰胆碱酯酶抑制活性，可抑制了高脂肪饮食（HFD）引起的小鼠代谢并发症的发展，对科尼氏分枝杆菌叶对链脲佐菌素诱导的糖尿病大鼠胰腺β细胞组织病理学变化有作用。

IHMT-MST1-39 是一种MST激酶抑制剂，显示出口服活性，并具有对MST1和MST2的IC50分别为42 nM和109 nM。该化合物能在肝细胞中启动AMPK信号通路，同时抑制胰岛β细胞的凋亡 (apoptosis)。此外，IHMT-MST1-39 还能改善由Streptozotocin引发的小鼠一型糖尿病。

α-Glucosidase-IN-74作为一种异烟酰胺-噻唑衍生物，主要功能为抑制α-葡萄糖苷酶 (α-glucosidase)。该化合物表现出显著的抗糖尿病活性，能有效降低Streptozotocin诱发糖尿病动物模型中的血糖及甘油三酯水平。

Kv7.2 Kv7.3 agonist 1 (Compound 16) 作为一种口服激动剂，针对KV7.2 7.3通道（KV7.2 7.3 channel KCNQ2 3），其EC50值为1.03 μM。在实验动物模型中，该化合物在小鼠的慢性压迫性损伤（CCI）和Streptozotocin诱导的糖尿病周围神经性疼痛（DPNP）模型中具有显著的镇痛效果，ED50值分别达到12.02和9.63 mg kg。

TGase2-IN-1（Compound 22）为一种具口服效力的TGase2抑制剂，其对TGase2的IC50值为1.12 μM，且对人视网膜微血管内皮细胞中TGase2的抑制作用的IC50为0.07 μM。此外，TGase2-IN-1展现出74.6%的口服生物利用度，并能有效抑制小鼠Streptozotocin诱导的糖尿病模型中视网膜血管渗漏。

(6S)-CP-470711（Compound 8）作为一种山梨醇脱氢酶（sorbitol dehydrogenase, SDH）抑制剂，对人类及大鼠SDH的抑制活性表现出来，其IC50值分别为19 nM和27 nM。此外，(6S)-CP-470711能有效改善由Streptozotocin引起的大鼠糖尿病症状。

PPARγ agonist16 (Compound 4G) 是一种PPARγ激动剂，能够竞争性结合PPARγ的LBD结构域，其IC50为1790 nM。此化合物在小鼠模型中抑制耳朵肿胀，并在Streptozotocin诱导的小鼠糖尿病模型中展现抗高血糖作用。

PPARγ agonist15 (Compound 7c) 是PPARγ的激动剂，能够抑制 α-淀粉酶 (HPA) 和 α-葡萄糖苷酶 (HLAG) 的表达，IC50分别为 28.35 µM 和 26.21 µM。此外，它还能在L6肌管细胞中促进葡萄糖摄取，并在大鼠Streptozotocin-诱发的糖尿病模型中改善葡萄糖稳态、胰岛素敏感性和脂质代谢。

Salazinic Acid 是从 Lichen Hypotrachyna cirrhata 提取的化合物，具有潜在的抗氧化活性，可减轻链脲佐菌素诱导的糖尿病白化大鼠的雄性性功能障碍和睾丸氧化损伤。

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.

Ruboxistaurin is a PKC beta inhibitor. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1

PNU-282987 free base 是一种具有选择性和高效性的 α7 烟碱乙酰胆碱受体 (nAChR) 激动剂 ， 也是5-HT3受体的拮抗剂，具有抗炎活性，对脓毒症诱导的小鼠急性肺损伤有保护作用，可减弱 ILC2s 活化和链格孢菌诱导的气道炎症。PNU-282987 free base 可用于研究神经系统疾病。

α-Glucosidase-IN-16 is a highly effective and orally bioavailable inhibitor of α-glucosidase, displaying a remarkable IC50 value of 3.28 μM. This compound demonstrates the ability to significantly decrease blood glucose levels in diabetic rats induced by Streptozotocin. Notably, α-Glucosidase-IN-16 also exhibits noteworthy antidiabetic activity [1].

Ruboxistaurin mesylate monohydrate is a PKC beta inhibitor potentially for the treatment of diabetic nephropathy and diabetic macular edema. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1 Smad and GRAP pathways. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin inhibits retinal neovascularization via suppression of phosphorylation of ERK1 2 and Akt.

Theobromine-d6 is intended for use as an internal standard for the quantification of theobromine by GC- or LC-MS. Theobromine is a methylxanthine alkaloid and derivative of caffeine that has been found in cocoa beans and has diverse biological activities. It is an adenosine A1 receptor antagonist. Theobromine increases AMPK phosphorylation and inhibits adipocyte differentiation, ERK and JNK phosphorylation, and IL-6 and TNF-α production in 3T3-L1 preadipocytes cultured in differentiation medium. It inhibits decreases in renal cortex SIRT1 activity and increases in NADPH oxidase-dependent reactive oxygen species (ROS) production, as well as reduces kidney hypertrophy and albuminuria in a spontaneously hypertensive rat model of streptozotocin-induced diabetes when administered at a dose of 5 mg kg per day.3 Theobromine is toxic to dogs with an LD50 value of 250 to 500 mg kg.

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).

BBT 具有抗高血糖活性，通过 cAMP PKA 和持久（L 型）电压依赖性 Ca2+ 通道 CaMK2 通路发挥作用，保护β细胞免受细胞因子或链脲佐菌素（STZ）诱导的细胞死亡，恢复 β 细胞功能，可用于研究糖尿病。