GLUT Activator

Antidiabetic agent 9 is an orally active antidiabetic agent. Antidiabetic agent 9 promotes the translocation of GLUT4 to the cell surface, activates the AMPK signaling pathway, and has no effect on the PI-3-K/AKT signaling pathway. Antidiabetic agent 9 reduces blood glucose levels in Streptozotocin (HY-13753)-induced diabetic rats. Antidiabetic agent 9 can be used in the research of diabetes.

GTPγS (Guanosine 5'-[γ-thio]triphosphate) tetralithium is a G-protein activator that protects proteins from proteolytic degradation, stimulates GLUT4 translocation in a tyrosine kinase-dependent manner, stimulate phospholipases and induce actin polymerization. GTPγS tetralithium to couple with G- protein α, to study its effect on kinase activity. GTPγS tetralithium acts as a component of lysis buffer.

Rhoifolin is a flavone glycoside can be isolated from Rhus succedanea. Rhoifolin has anti-diabetic effect acting through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin has an anti-inflammatory action via multi-level regulation of inflammatory mediators. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways. Rhoifolin also has cytotoxic activity against different cancer cell lines.

MOTS-c (human) is a blood-brain barrier-penetrating, mitochondrial-derived peptide that modulates the AMPK/PGC-1α pathway to enhance insulin sensitivity. MOTS-c (human) inhibits the folate cycle and de novo purine synthesis, increases AICAR levels to activate AMPK, and then regulates the Nrf2/Keap1 antioxidant pathway and inhibits the NF-κB inflammatory pathway, while promoting mitochondrial biogenesis and energy metabolism. MOTS-c (human) has the effects of improving glucose and lipid metabolism, anti-oxidative stress, anti-inflammatory and neuroprotection, and can be used in the study of type 2 diabetes, traumatic brain injury, inflammatory diseases and aging-related metabolic disorders.

MOTS-c (human) acetate is a blood-brain barrier-penetrating, mitochondrial-derived peptide that modulates the AMPK/PGC-1α pathway to enhance insulin sensitivity. MOTS-c (human) acetate inhibits the folate cycle and de novo purine synthesis, increases AICAR levels to activate AMPK, and then regulates the Nrf2/Keap1 antioxidant pathway and inhibits the NF-κB inflammatory pathway, while promoting mitochondrial biogenesis and energy metabolism. MOTS-c (human) acetate has the effects of improving glucose and lipid metabolism, anti-oxidative stress, anti-inflammatory and neuroprotection, and can be used in the study of type 2 diabetes, traumatic brain injury, inflammatory diseases and aging-related metabolic disorders.

D927 (DS11252927) is an orally active glucose transporter type 4 (GLUT4) translocation activator with an EC₅₀ of 0.14 μM. D927 enhances the binding affinity of PI3Kα catalytic subunit p110α to canonical RAS proteins (KRAS4A, KRAS4B) and RRAS, RRAS2, MRAS. D927 activates the PI3Kα-AKT pathway (increasing phosphorylation of AKT, p70S6 kinase) without affecting the RAF-ERK1/2 pathway. D927 improves hyperglycemia in type 1 and type 2 diabetes mice model. D927 can be used for the study of glucose homeostasis disorders and diabetes.

Hydroxylamine (50% w/w in water) is an inorganic highly reactive compound and antibacterial agent. Hydroxylamine (50% w/w in water) acutely activates the transport activity of GLUT1, inhibits Monoamine oxidase activity. Hydroxylamine (50% w/w in water) inhibits nitrite oxidizing bacteria. Hydroxylamine (50% w/w in water) activates glucose uptake. Hydroxylamine (50% w/w in water) can be used in the research of inflammatory diseases and allergies[1][2][3][4].

p-Synephrine is an orally active alkaloid dietary supplement without indirect sympathomimetic activity or cardiovascular stimulatory activity. p-Synephrine stimulates AMPK phosphorylation and mediates Glut4 translocation to increase glucose consumption and lactate production in skeletal muscle cells. p-Synephrine also downregulates the p38 MAPK and NF-κB signaling pathways to inhibit pro-inflammatory cytokine production and alter oxidative metabolism. p-Synephrine exhibits low subchronic toxicity in mice. p-Synephrine can be applied to research related to systemic inflammatory response syndrome, obesity, and type 2 diabetes.

SIRT6-IN-6 (compound 6d) is a potent and selective SIRT6 inhibitor with an IC₅₀ of 4.93 μM and a K_i of ~10 μM. SIRT6-IN-6 shows selectivity against other members of the HDAC family (SIRT1-3 and HDAC1-11). SIRT6-IN-6 significantly increases the level of glucose transporter GLUT-1, thereby reducing blood glucose in a mouse model of type 2 diabetes. SIRT6-IN-6 can be used for type 2 diabetes research.

Licarin B, a nitric oxide production inhibitor extracted from the component of the seeds of Myristica fragrans, improves insulin sensitivity via PPARγ and activation of GLUT4 in the IRS-1/PI3K/AKT pathway.

DS02312223 (D223) is a molecular glue that promotes the binding of RAS to PI3Kα, with a K_d of 0.76 μM for p110α. DS02312223 increases the binding affinity between GTP-bound KRAS (KRAS-GMPPNP) and p110α by nearly three orders of magnitude (K_D = 0.017 μM). DS02312223 stimulates the translocation of GLUT4 to the plasma membrane. DS02312223 promotes glucose uptake in the absence of insulin. DS02312223 can be used in diabetes research.

Allyl methyl sulfide is an orally active organic sulfide. Allyl methyl sulfide is one of the main active ingredients in garlic volatile metabolites. Allyl methyl sulfide can be extracted from garlic. Allyl methyl sulfide enhances SOD activity, inhibits NF-κB signaling pathway, and upregulates pancreatic GLUT2 expression. Allyl methyl sulfide has significant antioxidant, anti-inflammatory and hypoglycemic activities. Allyl methyl sulfide can be used in the research of diabetes and its complications.

Deoxyandrographolide is an orally active lactone found in the Andrographis paniculata Nees. Deoxyandrographolide shows a K_D of 38.4 μM of HDAC1. Deoxyandrographolide enhances GLUT4 plasma membrane translocation, activates PI3K and AMPK-dependent signaling pathways, suppresses fasting blood glucose, serum insulin, triglycerides, and LDL-cholesterol levels. Deoxyandrographolide enhances HDAC1 expression via inhibited ubiquitination degradation, represses H3K4me3, improves chromosome stability, and restrains aging biomarkers p16, p21, γH2A.X, p53 and ROS production. Deoxyandrographolide interacts with Foot-and-Mouth Disease Virus 3Cpro active site, inhibits protease and IFN-antagonist activity, derepresses ISG expression, and inhibits viral replication. Deoxyandrographolide can be used for the researches of type 2 diabetes mellitus, vascular senescence and virus infection.

Sennidin B, a stereoisomer isolated from the leaves of Cassia angustifolia, has lower activity than Sennidin A. Sennidin A inhibits HCV NS3 helicase, with an IC₅₀ of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation .

Pongamol (Lanceolatin C) is an orally active flavonoid with an IC₅₀ of 75 μM and a K_i of 58 μM against PTPase-1B, and an IC₅₀ of 103.5 μM against intestinal α-Glycosidase. Pongamol reduces the release of IL‑1β, TNF‑α, COX‑2 and iNOS in cells, reverses the nuclear translocation of NF‑κB, and upregulates the levels of Beclin 1 and LC3 Ⅱ/LC3 Ⅰ. Pongamol promotes glucose uptake by increasing the level of GLUT4 on the surface of skeletal muscle cells. Pongamol inhibits epithelial-mesenchymal transition by suppressing the FAK/Akt-mTOR signaling pathway. Pongamol inhibits neuronal cytotoxicity, suppresses cell apoptosis and extends the lifespan of Caenorhabditis elegans by activating the MAPKs/Nrf2 signaling pathway. Pongamol exerts hypoglycemic effects in diabetic mouse models. Pongamol exhibits antibacterial activity. Pongamol alleviates oxidative stress, neuroinflammation, Aβ deposition and excessive phosphorylation of Tau Protein, and restores autophagy function in Alzheimer's disease mouse models by inhibiting the Akt/mTOR signaling pathway. Pongamol is applicable to research related to Alzheimer's disease, type 2 diabetes, non-small cell lung cancer and postprandial hyperglycemia.

Pterosin A ((2S)-Pterosin A) is a sesquiterpene compound. Pterosin A is an orally active AMPK activator with anti-diabetic effect. Pterosin A can promote glucose uptake, increase serum insulin, and improve hyperglycemia and glucose intolerance. Pterosin A can prevent insulin-secreting cells death and reduce ROS production. Pterosin A can be used for the research of metabolic disease, such as diabetes.

CM002 is a circadian clock activator. CM002 inhibits the lineage commitment and terminal differentiation of preadipocytes by activating the circadian clock, thereby blocking the adipogenesis process driven by Wnt signaling-mediated transcriptional induction. CM002 attenuates lipid storage in a clock-dependent manner via inhibition of the lipogenic program in mature adipocytes. CM002 enhances circadian clock output across various adipose depots in both lean and obese mice through BMAL1/CLOCK-dependent metabolic reprogramming, inhibits adipocyte development and hypertrophy, and improves insulin sensitivity. CM002 can be used in research on obesity and type 2 diabetes.

3-Fluoro-evodiamine glucose (Compound 8) is an evodiamine-glucose conjugate. 3-Fluoro-evodiamine glucose activates the expression of glucose transporter 1 (GLUT1), and inhibits topoisomerase I/II. 3-Fluoro-evodiamine glucose induces apoptosis and arrests the cell cycle at G2/M phase. 3-Fluoro-evodiamine glucose exhibits antitumor efficacy in vivo and in vitro, without significant toxicity.

Rhoifolin (Standard) is the analytical standard of Rhoifolin. This product is intended for research and analytical applications. Rhoifolin is a flavone glycoside can be isolated from Rhus succedanea. Rhoifolin has anti-diabetic effect acting through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin has an anti-inflammatory action via multi-level regulation of inflammatory mediators. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways. Rhoifolin also has cytotoxic activity against different cancer cell lines.

Allyl methyl sulfide (Standard) is the analytical standard of Allyl methyl sulfide (HY-128447). This product is intended for research and analytical applications. Allyl methyl sulfide is an orally active organic sulfide. Allyl methyl sulfide is one of the main active ingredients in garlic volatile metabolites. Allyl methyl sulfide can be extracted from garlic. Allyl methyl sulfide enhances SOD activity, inhibits NF-κB signaling pathway, and upregulates pancreatic GLUT2 expression. Allyl methyl sulfide has significant antioxidant, anti-inflammatory and hypoglycemic activities. Allyl methyl sulfide can be used in the research of diabetes and its complications.