glucose concentration

By Targets:	GLUT (2) SGLT (2) Autophagy (1) Endogenous Metabolite (1) Free Fatty Acid Receptor (1) GCGR (1) Lipoxygenase (1) PPAR (1) Somatostatin Receptor (1) Topoisomerase (1)
By Research Areas:	Cancer (4) Endocrinology (1) Metabolic Disease (7)

Targets Recommended: GLUT SGLT

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-109500

Masoprocol meso-Nordihydroguaiaretic acid; meso-NDGA	Lipoxygenase	Metabolic Disease
Masoprocol (meso-Nordihydroguaiaretic acid) is a potent and orally active lipoxygenase inhibitor. Masoprocol shows antihyperglycemic activity. Masoprocol decreases the glucose concentration and hepatic triglyceride in vivo. Masoprocol has the potential for the research of type II diabetes .

HY-109018A

Velagliflozin proline 1 Publications Verification	SGLT	Metabolic Disease
Velagliflozin proline is an oral *sodium-glucose* cotransporter 2 (SGLT2*) inhibitor with antidiabetic activity. Velagliflozin proline reduces renal glucose* reabsorption and stimulates glycosuria, which lowers blood sugar and insulin concentrations .

HY-109018B

Velagliflozin proline hydrate	SGLT	Metabolic Disease
Velagliflozin proline hydrate is the clinical form of Velagliflozin (HY-109018). Velagliflozin is an oral *sodium-glucose* cotransporter 2 (SGLT2*) inhibitor with antidiabetic activity. Velagliflozin reduces renal glucose* reabsorption and stimulates glycosuria, which lowers blood sugar and insulin concentrations .

HY-148247

BI-2081	Free Fatty Acid Receptor	Metabolic Disease
BI-2081 is a GPR40 (FFAR1) partial agonist (EC₅₀: 4 nM). BI-2081 induces glucose depending insulin secretion and reduces the plasma glucose concentration. BI-2081 can be used in the research of metabolic diseases, in particular diabetes type 2 .

HY-P3621

Biotinyl-Glucagon (1-29), human, bovine, porcine	GCGR	Metabolic Disease
Biotinyl-Glucagon (1-29), human, bovine, porcine is a biotinylated glucagon. Glucagon is a peptide hormone, produced by α-cells of the pancreas, can increase concentration of glucose and fatty acids in the bloodstream .

HY-155034

Antitumor agent-102	Topoisomerase GLUT	Cancer
Antitumor agent-102 (compound 10) is a conjugate of Topoisomerase I inhibitor SN38 and glucose transporter inhibitor, targeting to colorectal cancer. Antitumor agent-102 induces higher concentrations of free SN38 in tumor tissues than Irinotecan (HY-16562) .

HY-19824

3PO Maximum Cited Publications 19 Publications Verification	Autophagy	Cancer
3PO is an inhibitor of PFKFB3. 3PO attenuates the proliferation of several cancer cell lines with IC₅₀s of 1.4-24 μmol/L. 3PO suppresses glucose uptake and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD ⁺ and NADH. 3PO can be used for the research of cancer .

HY-108615

CP-316819 GPi 819	Others	Endocrinology
CP 316819 is a potent glycogen phosphorylase (GPase) inhibitor with antihyperglycemic effect (IC₅₀ values are 17 and 34 nM against human skeletal muscle glycogen phosphorylase (huSMGPa) and liver glycogen phosphorylase (huLGPa) respectively).CP 316819 causes glycogen accumulation under normoglycemic conditions but permits glycogen utilization when glucose concentrations are low.CP-316819 prevents neuronal cell death and maintains brain electrical currents .

HY-P3954

Somatostatin-28 (sheep, human rat mouse)	Somatostatin Receptor	Metabolic Disease
Somatostatin-28 (sheep, human rat mouse) is a biologically active polypeptide, synthesised in the proximal intestinal epithelial cells. Somatostatin-28 (sheep, human rat mouse) suppresses glucose-stimulated insulin secretion without affecting circulating basal insulin concentration. Somatostatin-28 (sheep, human rat mouse) also targets to somatostatin receptor subtype 5 (SSTR5) to regulate GLP-1 secretion .

HY-113513

5-HEPE	Others	Cancer
5(S)-HEPE is an active metabolite of eicosapentaenoic acid. It is formed from EPA by 5-lipoxygenase (5-LO). 5(S)-HEPE is an agonist of G protein-coupled receptor 119 (GPR119). It increases cAMP accumulation in CHO-K1 cells expressing human GPR119 when used at a concentration of 10 μM. 5(S)-HEPE increases glucose-induced insulin secretion from MING6 insulinoma pancreatic islets and glucagon-like peptide 1 (GLP-1) secretion from HuTu 80 adenocarcinoma cells when used at a concentration of 10 μM. Serum levels of 5(S)-HEPE are elevated in patients with hyperlipidemia.

HY-151486

GLUT1-IN-1	GLUT	Cancer
GLUT1-IN-1 is a glucose transporter 1 (GLUT1) inhibitor and has a GLUT1-specific inactivation ability. GLUT1-IN-1 exhibits concentration-dependent cytotoxicity for HeLa, A549 and HepG2 cells with IC₅₀ values of 5.49 μM, 11.14 μM, and 8.73 μM, respectively. GLUT1-IN-1 can be used for the research of photodynamic therapy (PDT) and severals cancer .

HY-124399

N-Octadecyl-N'-propyl-sulfamide	Endogenous Metabolite PPAR	Metabolic Disease
Peroxisome proliferator-activated receptors (PPARs) play an important role in regulating lipid and glucose metabolism, and oleoylethanolamide (OEA) is a natural ligand for PPARα. N-Octadecyl-N'-propyl-sulfamide is an analog of OEA and a potent activator of PPARα, with selective binding affinity for PPARα (EC50=100 nM, compared to 120 nM for OEA). N-Octadecyl-N'-propyl-sulfamide (10 mg/kg; ip) inhibits food intake and reduces body weight gain in rats. At a dose of 1 mg/kg, N-Octadecyl-N'-propyl-sulfamide induces satiety, thereby reducing food intake, body weight, and plasma triglyceride concentrations in free-feeding Wistar rats and obese Zucker (fa/fa) rats.

Cat. No.	Product Name

HY-L045

Oxygen Sensing Compound Library	2,572 compounds
Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression. Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival. HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O₂ concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation. MCE offers a unique collection of 2,572 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

Oxygen Sensing Compound Library

2,572 compounds

Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression.

Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival.

HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O₂ concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation.

MCE offers a unique collection of 2,572 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

Cat. No.	Product Name	Target	Research Area

HY-P3954

Somatostatin-28 (sheep, human rat mouse)	Somatostatin Receptor	Metabolic Disease
Somatostatin-28 (sheep, human rat mouse) is a biologically active polypeptide, synthesised in the proximal intestinal epithelial cells. Somatostatin-28 (sheep, human rat mouse) suppresses glucose-stimulated insulin secretion without affecting circulating basal insulin concentration. Somatostatin-28 (sheep, human rat mouse) also targets to somatostatin receptor subtype 5 (SSTR5) to regulate GLP-1 secretion .

HY-P3621

Biotinyl-Glucagon (1-29), human, bovine, porcine	GCGR	Metabolic Disease
Biotinyl-Glucagon (1-29), human, bovine, porcine is a biotinylated glucagon. Glucagon is a peptide hormone, produced by α-cells of the pancreas, can increase concentration of glucose and fatty acids in the bloodstream .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-109500

Masoprocol meso-Nordihydroguaiaretic acid; meso-NDGA	other families Classification of Application Fields Source classification Phenols Polyphenols Metabolic Disease Plants Disease Research Fields	Lipoxygenase
Masoprocol (meso-Nordihydroguaiaretic acid) is a potent and orally active lipoxygenase inhibitor. Masoprocol shows antihyperglycemic activity. Masoprocol decreases the glucose concentration and hepatic triglyceride in vivo. Masoprocol has the potential for the research of type II diabetes .

HY-113513

5-HEPE	Microorganisms Source classification	Others
5(S)-HEPE is an active metabolite of eicosapentaenoic acid. It is formed from EPA by 5-lipoxygenase (5-LO). 5(S)-HEPE is an agonist of G protein-coupled receptor 119 (GPR119). It increases cAMP accumulation in CHO-K1 cells expressing human GPR119 when used at a concentration of 10 μM. 5(S)-HEPE increases glucose-induced insulin secretion from MING6 insulinoma pancreatic islets and glucagon-like peptide 1 (GLP-1) secretion from HuTu 80 adenocarcinoma cells when used at a concentration of 10 μM. Serum levels of 5(S)-HEPE are elevated in patients with hyperlipidemia.

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