streptozotocin

Streptozotocin (Streptozocin, NSC-85998) is an antibiotic that enters pancreatic β-cells via the glucose transporter (GLUT2) and induces DNA methylation, leading to β-cell apoptosis. It is toxic to insulin-producing cells and commonly used to establish diabetic animal models. This product is unstable in solution and is recommended to be prepared freshly before use.

Anandamide ((5Z,8Z,11Z,14Z)-N-(2-Hydroxyethyl)icosa-5,8,11,14-tetraenamide), an immune modulator, acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55) in the central nervous system.

Glibornuride, a blocker of ATP-sensitive K+ channels (pKi: 5.75), inhibits high-affinity [3H]-glibenclamide binding with potencies corresponding to its K+ channel activity.

LP-935509 is a selective, brain-permeable, small molecule competitive inhibitor of articulin-2-associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM. LP-935509 is a potent inhibitor of BIKE (IC50 of 14 nM) and a moderate inhibitor of GAK (IC50 of 320±40 nM).

o-Phenanthroline (1,10-Phenanthroline) , a metal chelator, prevents the induction of chromosomal aberrations in streptozotocin-treated cells.o-Phenanthroline protects mammalian cells from hydrogen peroxide-induced gene mutation and morphological transformation.

6-Hydroxyflavanone, extracted from the leaves of Acorus calamus, exhibits anti-inflammatory and anti-neuropathic pain activity by targeting cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), as well as opioid and GABA-A receptors. 6-Hydroxyflavanone has anti-injury sensory properties in a streptozotocin-induced diabetic neuropathy model. in a streptozotocin-induced diabetic neuropathy model with anti-injury sensory properties.

Virginiamycin S1 is a streptozotocin B antibiotic produced by Streptomyces verticillioides, which has antibacterial activity by inhibiting bacterial protein synthesis at the level of aminoacyl-tRNA binding and peptide bond formation.

Mahanimbine is found in the roots, leaves and stems of Murraya koenigii and is an orally active alkaloid extracted from Murraya koenigii. Bifidobacterium bifidum leaves on histopathological changes in pancreatic beta cells of streptozotocin-induced diabetic rats.

α-Glucosidase-IN-74, a nicotinamide-thiazole derivative, functions as an α-glucosidase (α-glucosidase) inhibitor. It demonstrates antidiabetic activity by reducing blood glucose and triglyceride levels in Streptozotocin-induced diabetic animals.

Kv7.2/Kv7.3 agonist 1 (Compound 16) is an orally effective agonist for the KV7.2/7.3 channels (KV7.2/7.3 channel/KCNQ2/3) with an EC50 of 1.03 μM. This compound demonstrates analgesic effects in mouse models of chronic constriction injury (CCI) and Streptozotocin-induced diabetic peripheral neuropathy (DPNP), with ED50 values of 12.02 mg/kg and 9.63 mg/kg, respectively.

TGase2-IN-1 (Compound 22) is an orally effective TGase2 inhibitor with an IC50 of 1.12 µM. It inhibits TGase2 in human retinal microvascular endothelial cells with a strikingly lower IC50 of 0.07 µM. The oral bioavailability of TGase2-IN-1 is 74.6%. Additionally, it can suppress retinal vascular leakage in a mouse model of diabetes induced by Streptozotocin.

(6S)-CP-470711 (Compound 8) acts as an inhibitor of sorbitol dehydrogenase (SDH) in both humans and rats, exhibiting inhibitory concentrations (IC50) of 19 nM and 27 nM, respectively. Additionally, (6S)-CP-470711 has been shown to ameliorate diabetes in rats induced by Streptozotocin.

PPARγ agonist16 (Compound 4G) is a PPARγ agonist that competitively binds to the ligand-binding domain (LBD) of PPARγ with an IC50 of 1790 nM. It reduces ear swelling in mouse models and exhibits antihyperglycemic activity in mice with Streptozotocin-induced diabetes.

PPARγ agonist15 (Compound 7c) functions as an agonist of PPARγ, inhibiting the expression of α-amylase (HPA) and α-glucosidase (HLAG) with IC50 values of 28.35 µM and 26.21 µM, respectively. It enhances glucose uptake in L6 myotubes and improves glucose homeostasis, insulin sensitivity, and lipid metabolism in a rat model of Streptozotocin-induced diabetes.

α-Glucosidase-IN-43 (compound AS14) is an α-glucosidase inhibitor with an IC50 of 4.32 μM, demonstrating acute blood-glucose-lowering properties. It is safe and effective in vivo, showing no toxicity to normal fibroblasts in mice and can ameliorate diabetes induced by streptozotocin in rats. α-Glucosidase-IN-43 is applicable for research on postprandial hyperglycemia in diabetic patients.

20-SOLA is the first water-soluble 20-HETE antagonist with oral bioavailability. It significantly improves blood pressure changes and kidney damage associated with the streptozotocin (STZ) diabetic mouse model. Additionally, 20-SOLA acts as a GPR75 receptor blocker. This compound is useful in research related to cardiovascular pathology.

eeAChE-IN-3 (compound YS3g) is an orally bioavailable and potent inhibitor of EeAChE and IL-6, with IC50 values of 0.54 μM for EeAChE, 0.49 μM for RatAChE, 8.54 μM for RatBuChE, and 0.57 μM for IL-6. It can enhance learning and memory deficits in mice induced by STZ (streptozotocin) and shows potential for Alzheimer's disease (AD) research.

7,4'-Dimethoxy-3-hydroxyflavone is an orally active PAR4 antagonist. This compound inhibits PAR4-mediated human platelet aggregation with an IC50 of 1.4 μM. It disrupts PAR4-mediated aggregation and related signaling pathways, including NF-κB, Ca2+/protein kinase C (PKC), Akt, ERK, and p38. In a streptozotocin (STZ)-induced diabetic mouse model, 7,4'-Dimethoxy-3-hydroxyflavone inhibits vascular PAR4 expression, improves endothelial dysfunction, and reduces oxidative stress. Additionally, it prevents thrombosis in mice without affecting bleeding time.

DPP-4-IN-17 is an orally active and selective inhibitor of dipeptidyl peptidase-4 (DPP-4) with an IC50 value of 0.12 nM. It increases the enzyme's Km value (75.73 μM compared to the substrate alone at 27.18 μM) and reduces catalytic efficiency. In Streptozotocin (STZ)/Nicotinamide (NA)-induced diabetic rats, DPP-4-IN-17 lowers blood glucose levels and reverses weight loss. This compound is useful for research in type 2 diabetes (T2DM).

Salazinic Acid, a compound extracted from the Lichen Hypotrachyna cirrhata, has potential antioxidant activity and attenuates male sexual dysfunction and testicular oxidative damage in streptozotocin-induced diabetic albino rats.

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) is a potent agonist of α7 nicotinic acetylcholine receptor (nAChR) with an EC50 of 154 nM and a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. It can be used for central and peripheral nervous system studies[1].

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 significantly decreases blood glucose levels in Streptozotocin-induced diabetic rats and exhibits noteworthy antidiabetic activity [1].