Search Result
Results for "
Oral glucose tolerance
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N8518
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Phospholipase
p38 MAPK
Apoptosis
NF-κB
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Metabolic Disease
Inflammation/Immunology
Cancer
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Malabaricone C is an orally active and noncompetitive sphingomyelin synthase (SMS) inhibitor with IC50 values of 3 μM and 1.5 μM for SMS 1 and SMS 2, respectively. Malabaricone C reduces body weight gain, improves glucose tolerance, and decreases lipid accumulation in the liver, showing significant prevention of high fat diet-induced fatty liver in mice. Malabaricone C has anti-inflammatory effects, which is found in the fruits of Myristica cinnamomea King. Malabaricone C is promising for research of obesity and immunological disorders caused due to hyper-activation of T-cells .
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- HY-N2593
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Carnitine Palmitoyltransferase (CPT)
Reactive Oxygen Species (ROS)
Autophagy
Apoptosis
NF-κB
PI3K
Akt
MMP
Keap1-Nrf2
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Metabolic Disease
Inflammation/Immunology
Cancer
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Isorhapontigenin is an orally active dietary polyphenol. Isorhapontigenin acts as a potent antioxidant that reduces the production of reactive oxygen species (ROS). Isorhapontigenin promotes the binding of JUN to the AP-1 site on the SESN2 promoter, induces SESN2 transcription, triggers MAPK8-dependent JUN activation, and upregulates the expression of PPAR-α, PGC-1α and CPT-1A to facilitate fatty acid oxidation. Isorhapontigenin induces autophagy, apoptosis and preadipocyte differentiation; it inhibits tumor growth, cell invasion, NF-κB transcriptional activity, the PI3K/Akt signaling pathway, STAT1 phosphorylation and MMP-2 expression. Isorhapontigenin alleviates oxidative stress, inflammatory cytokine release and triglyceride accumulation; it increases intracellular ATP levels and promotes Nrf2 nuclear translocation. Isorhapontigenin improves insulin sensitivity in adipose tissue and glucose tolerance, and reduces postprandial blood glucose, insulin and free fatty acid levels. Isorhapontigenin is applicable to research on bladder cancer, liver injury, chronic obstructive pulmonary disease, acute lung injury and type 2 diabetes .
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- HY-N0936
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Coixol
1 Publications Verification
6-Methoxy-2-benzoxazolinone; 6-MBOA
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Others
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Inflammation/Immunology
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Coixol (6-Methoxy-2-benzoxazolinone; 6-MBOA) is a potent and orally active anti-inflammatory agent. Coixol decreases the iNOS protein expression. Coixol inhibits the production of TNF-α, IL-6, and IL-1β. Coixol improves glucose tolerance and plasma insulin. Coixol decreases the blood glucose level .
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- HY-N15721
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Trp-CA
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Orphan GPCR
GLP Receptor
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Metabolic Disease
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Tryptophan-cholic acid (Trp-CA) is a microbial amino acid-conjugated bile acid that acts as an endogenous ligand and agonist (EC50=9.6 μM) for the orphan G protein-coupled receptor (GPCR) MRGPRE (Mas-related G protein-coupled receptor family member E). Tryptophan-cholic acid is orally effective but has poor oral absorption and does not cross the blood-brain barrier. Tryptophan-cholic acid promotes the secretion of glucagon-like peptide GLP-1, thereby improving glucose tolerance in diabetic mice. Tryptophan-cholic acid improves glucose tolerance, promotes insulin secretion, and alleviates high-fat diet-induced hepatic steatosis without causing pruritus side effects. Tryptophan-cholic acid is primarily used in research on type 2 diabetes (T2D) .
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- HY-N2486
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Fatty Acid Synthase (FASN)
Apoptosis
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Cancer
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Desoxyrhaponticin is a kind of oral drug that inhibits effective fatty acid synthesis (FASN), and has a fatal effect on cancer cells. Desoxyrhaponticin has the ability to inhibit glucose uptake, improve oral glucose tolerance as a diabetic agent, and possess anti-diabetic effects.
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- HY-164781
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- HY-110197
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6bK TFA
2 Publications Verification
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IDE
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Metabolic Disease
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6bK TFA is a selective insulin-degrading enzyme (IDE) inhibitor with an IC50 of 50 nM. 6bK TFA binds to the distal pocket of IDE, thereby blocking substrate binding, peptide unfolding and cleavage processes, and reducing the degradation of insulin, glucagon and amylin. 6bK TFA improves oral glucose tolerance but impairs intraperitoneal glucose tolerance. 6bK TFA can be used in research related to type 2 diabetes .
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- HY-120565
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G protein-coupled Bile Acid Receptor 1
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Metabolic Disease
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WB403 is an orally active TGR5 activator with an EC50 of 5.5 μM against human TGR5. WB403 activates TGR5 to stimulate downstream signaling pathways, promote GLP-1 secretion, improve glucose tolerance in mice with type 2 diabetes, and reduce levels of fasting blood glucose, postprandial blood glucose and HbA1c. WB403 increases pancreatic β-cell mass and restores the distribution of α-cells and β-cells in islets. WB403 is applicable to the research of type 2 diabetes .
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- HY-108448
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OLDA
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TRP Channel
Lipoxygenase
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Cardiovascular Disease
Neurological Disease
Metabolic Disease
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N-Oleoyldopamine (OLDA) is an orally active TRPV1 activator and 5-LOX inhibitor with blood-brain barrier permeability. N-Oleoyldopamine excites histaminergic neurons in the tuberomammillary nucleus via a dopamine receptor mechanism, a process independent of TRPV1 and cannabinoid receptors. On one hand, N-Oleoyldopamine promotes the release of insulin and glucose-dependent insulinotropic polypeptide through a GPR119-dependent pathway to improve glucose tolerance; on the other hand, N-Oleoyldopamine improves left ventricular function and reduces myocardial infarction size by triggering the release of substance P and calcitonin gene-related peptide. N-Oleoyldopamine is used in studies related to glycemic abnormalities and myocardial ischemia-reperfusion injury .
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- HY-N15135
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Interleukin Related
Toll-like Receptor (TLR)
Fungal
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Metabolic Disease
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Arabinoxylan Medium viscosity is an orally active Dectin-1 splice variant modulator, glucose absorption inhibitor, and chyme viscosity enhancer. Arabinoxylan Medium viscosity inhibits particulate β-glucan-induced Dectin-1A activation and mildly suppresses Dectin-1B activation. In human dendritic cells stimulated with particulate β-glucan, Arabinoxylan Medium viscosity reduces the production of IL-10 and TNF-α, and increases the production of IL-4 and IL-23. Arabinoxylan Medium viscosity also supports antifungal immune responses without activating TLR2, TLR4 or TLR5, and does not induce cytokine production when used to stimulate human dendritic cells alone. Arabinoxylan Medium viscosity increases small intestinal chyme viscosity, gets degraded in the large intestine to produce short-chain fatty acids, reduces glucose absorption and insulin response, and improves glucose homeostasis. Arabinoxylan Medium viscosity supports microbial fermentation and the growth of beneficial microbiota in the gastrointestinal tract, prevents bile acid reabsorption, and delays starch digestion. Arabinoxylan Medium viscosity can be used in research related to type 2 diabetes, impaired glucose tolerance, and metabolic syndrome .
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- HY-111254
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PPAR
NF-κB
JNK
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Inflammation/Immunology
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GQ-16 is an orally active PPARγ partial agonist with an IC50 of 1.84 μM and a Ki of 160 nM against human PPARγ. GQ-16 inhibits Cdk5-mediated Ser-273 phosphorylation. GQ-16 improves insulin sensitivity and glucose tolerance in obese and diabetic mice. GQ-16 also exhibits certain cytotoxicity against tumor cells. GQ-16 can be used in research related to obesity, diabetes and cancer .
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- HY-N2486R
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Reference Standards
Fatty Acid Synthase (FASN)
Apoptosis
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Cancer
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Desoxyrhaponticin (Standard) is the analytical standard of Desoxyrhaponticin. This product is intended for research and analytical applications. Desoxyrhaponticin is a kind of oral drug that inhibits effective fatty acid synthesis (FASN), and has a fatal effect on cancer cells. Desoxyrhaponticin has the ability to inhibit glucose uptake, improve oral glucose tolerance as a diabetic agent, and possess anti-diabetic effects .
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- HY-W003222
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Drug Intermediate
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Metabolic Disease
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N-tert-Boc-cis-4-fluoro-L-proline (Compound 11) is a drug intermediate for the synthesis of 4-fluoropyrrolidine-2-carbonitrile DPP-4 inhibitor. N-tert-Boc-cis-4-fluoro-L-proline can be used to study type 2 diabetes .
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- HY-N11262
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Phosphodiesterase (PDE)
Sirtuin
PGC-1α
p38 MAPK
HSP
TNF Receptor
NO Synthase
Apoptosis
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Metabolic Disease
Inflammation/Immunology
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Sudachitin is an orally active compound that potently inhibits mouse PDE1C and human PDE4B, with IC50 values of 5.0 μM and 15.0 μM, respectively. Sudachitin upregulates Sirt1 and PGC‑1α expression in skeletal muscle to regulate energy metabolism and promote mitochondrial biogenesis. Sudachitin improves lipid metabolism, glucose tolerance, insulin sensitivity, energy expenditure, and fatty acid β‑oxidation. Sudachitin activates p38MAPK signaling, induces HSP27 phosphorylation and caspase‑dependent apoptosis, and blocks EGF‑driven keratinocyte migration and proliferation. Sudachitin suppresses LPS‑induced TNF‑α, NO, and iNOS expression in macrophages and shows potent anti‑inflammatory activity. Sudachitin can be used for the research of metabolic syndrome, type 2 diabetes, and psoriasis. .
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- HY-144289
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Glucokinase
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Metabolic Disease
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BMS-820132 is an orally active and partial glucokinase (GK) activator with a AC50 of 29 nM. BMS-820132 decreases the glucose levels in glucose tolerance test (OGTT) model in normal rats, but not Zucker diabetic fatty (ZDF) rats. BMS-820132 exhibits pharmacological toxicity secondary to strong GK activation .
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- HY-178982
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Apelin Receptor (APJ)
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Metabolic Disease
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Apelin agonist 2 (Compound 35) is an orally active APLNR agonist. Apelin agonist 2 can significantly inhibit the accumulation of cAMP (EC50 = 10 nM). Apelin agonist 2 exhibits a significant improvement in glucose tolerance. Apelin agonist 2 can be used to study metabolic diseases such as diabetes .
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- HY-178447
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PPAR
Glutathione Peroxidase
SOD
TNF Receptor
Interleukin Related
NF-κB
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Infection
Metabolic Disease
Endocrinology
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PPARγ agonist 20 is a potent, orally active PPAR-γ agonist. PPARγ agonist 20 effectively increases antioxidant defenses (SOD, GSH) and reduces lipid peroxidation. PPARγ agonist 20 can upregulate of Pparg, Glut4, and AdipoQ, suppresses of TNF-α, IL-6, and NF-κB p65. PPARγ agonist 20 significantly lowers fasting blood glucose, improving glucose tolerance, and restoring metabolic balance in Streptozotocin (HY-13753)-Nicotinamide (HY-B0150)-induced diabetic rats. PPARγ agonist 20 can be used for the study of type 2 diabetes .
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- HY-14810
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AVE-2268
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SGLT
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Metabolic Disease
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Atigliflozin (AVE-2268) is an orally active and selective SGLT-2 inhibitor, with IC50s of 10 nM and 8.2 μM for hSGLT-2 and hSGLT-1) respectively. Atigliflozin can lower the blood glucose and improve the impaired oral glucose tolerance. Atigliflozin can be used for research of type II diabetes mellitus .
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- HY-124978
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GPR119
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Metabolic Disease
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MK-8282 is a potent, orally active GPR-119 agonist. MK-8282 shows improved glucose tolerance. MK-8282 can be used in the research of type 2 diabetes .
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- HY-160602
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Free Fatty Acid Receptor
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Metabolic Disease
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CPL207280 is an orally active GPR40/FFA1 agonist with an antidiabetic effect. CPL207280 can effectively enhance glucose-stimulated insulin secretion and improve glucose tolerance in MIN6 pancreatic β-cells as well as in healthy Wistar Han rats and diabetic rat models. CPL207280 can be used for the research of type 2 diabetes .
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- HY-177297
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NVP-LCZ960
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Glucokinase
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Metabolic Disease
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LCZ960 is an orally active glucokinase (GK) activator. LCZ960 stimulates GK activity in hepatocytes in vitro and stimulates glucose uptake in vivo through hepatic GK activation. LCZ960 lowers blood glucose in mice with diet-induced obesity (DIO). LCZ960 maintains normoglycemia and improves glucose tolerance in DIO mice and rats. LCZ960 stimulates glycogen synthase flux and increases hepatic glycogen turnover in rats. LCZ960 induces increased hepatic glycogen recycling. LCZ960 can be used to study high-fat diet-induced obesity and type 2 diabetes .
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- HY-178857
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Cannabinoid Receptor
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Metabolic Disease
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CB1 antagonist 6 (Compound 11jE2) is an orally active CB1R antagonist, with an IC50 value of 23 nM. CB1 antagonist 6 significantly reduces food intake and body weight, improves glucose tolerance and insulin resistance, and decreases serum ALT and AST levels in diet-induced obese (DIO) mice, demonstrating hepatoprotective effects. CB1 antagonist 6 can be used for the study of metabolic syndrome (obesity, diabetes) .
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- HY-N0936R
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6-Methoxy-2-benzoxazolinone (Standard); 6-MBOA (Standard)
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Reference Standards
Others
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Inflammation/Immunology
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Coixol (6-Methoxy-2-benzoxazolinone; 6-MBOA) is a potent and orally active anti-inflammatory agent. Coixol decreases the iNOS protein expression. Coixol inhibits the production of TNF-α, IL-6, and IL-1β. Coixol improves glucose tolerance and plasma insulin. Coixol decreases the blood glucose level .
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- HY-173479
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GLP Receptor
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Cardiovascular Disease
Metabolic Disease
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GLP-1R agonist 30 is a selective and orally active GLP-1R agonist with an EC50 of 0.048 nM. GLP-1R has excellent selectivity, with EC50 greater than 20 μM for GLP-2R, GIPR, and GCPR. GLP-1R agonist significantly increases cAMP-stimulating activity while markedly reducing hERG inhibitory activities. GLP-1R agonist has preferable absorption and excellent β-arrestin pathway selectivity. GLP-1R agonist effectively improves glucose tolerance and promoted insulin secretion in B-hGLP1R knock-in mice .
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- HY-162893
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Glycosidase
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Metabolic Disease
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SX29 is an orally active non-competitive α-glucosidase inhibitor with an IC50 value of 2.12 μM. SX29 exhibits hypoglycemic activity, and oral administration of SX29 can reduce blood glucose levels and improve glucose tolerance in diabetic mice .
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- HY-161281
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Glycosidase
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Metabolic Disease
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α-Glucosidase-IN-49 (compound C23) is a potent inhibitor of α-Glucosidase, with IC50 of 0.52 μM. α-Glucosidase-IN-49 has oral bioactivity that can reduce blood glucose and improve glucose tolerance in mice .
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- HY-161892
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FABP
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Metabolic Disease
Inflammation/Immunology
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FABP4-IN-4 (Compound 30) is an orally active inhibitor for FABP, with IC50 of 1.18 μM for FABP 1. FABP4-IN-4 improves the glucose tolerance, reduces the level of blood glucose, plasma lipids and hepatic inflammatory factors, attenuates hepatic steatosis, and exhibits anti-inflammatory effects in mouse diet-induced obesity models .
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- HY-10287A
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Dipeptidyl Peptidase
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Metabolic Disease
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Gosogliptin hydrochloride is the hydrochloride of Gosogliptin (HY-10287). Gosogliptin (PF-00734200) is a potent, orally active, selective, and competitive inhibitor of DPP-IV, the enzyme mainly responsible for the degradation of the incretin peptides GLP-1 and glucose-dependent insulinotropic polypeptide. Gosogliptin demonstrates rapid and reversible inhibition of plasma DPP-4 activity. Gosogliptin stimulates insulin secretion and improves glucose tolerance .
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- HY-155553
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GPR119
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Metabolic Disease
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GPR119 agonist 2 (compound 43) is an orally active GPR119 agonist. GPR119 agonist 2 shows good pharmacokinetic characteristics in rodents and can effectively improve glucose tolerance in mice and rats. GPR119 agonist 2 has the potential to study type 2 diabetes .
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- HY-133559
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PPAR
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Metabolic Disease
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VSP-77 is an orally active PPARγ agonist. VSP-77 selectively upregulates the expression of insulin sensitivity-related genes (Glut4 and Adiponectin) by inhibiting CDK5-mediated phosphorylation of PPARγ at Ser-273. VSP-77 significantly improves glucose tolerance, reduces fasting blood glucose and insulin levels in high-fat diet (HFD)-induced diabetic mouse models. VSP-77 can be used for the study of diabetes .
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- HY-125327
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SGLT
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Metabolic Disease
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YM-543 is a selective SGLT2 inhibitor that effectively reduces hyperglycemia in type 2 diabetic mice through increased urinary glucose excretion. YM-543 demonstrates potent inhibition of both mouse and human SGLT2 activities at nanomolar concentrations. YM-543, when administered orally, significantly improves glucose tolerance in diabetic models and sustains its effects for over 12 hours. YM-543, in combination with other antidiabetic agents like rosiglitazone or metformin, enhances the therapeutic effects on diabetic symptoms. YM-543 does not affect blood glucose levels in normal mice, indicating its specificity for diabetic conditions.
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- HY-147678
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Free Fatty Acid Receptor
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Metabolic Disease
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GPR40 agonist 5 (compound I-14) is an orally active and potent GPR40 (G protein coupled receptor 40) agonist, with an EC50 of 47 nM. GPR40 agonist 5 decreases the levels of blood glucose and improves the glucose tolerance. GPR40 agonist 5 has sufficient effectiveness for the control of hyperglycemia state in type 2 diabetic mice . GPR40 agonist 5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-155967
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AMPK
Cannabinoid Receptor
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Metabolic Disease
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CB1R/AMPK modulator 1 (Compound 38-S) is an orally active CB1R/AMPK modulator, with an Ki of 0.81 nM and an IC50 of 3.9 nM for CB1R. CB1R/AMPK modulator 1 activates AMPK. CB1R/AMPK modulator 1 reduces food intake and body weight, and improves glucose tolerance and insulin sensitivity .
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- HY-10289
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RO-4876904
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Dipeptidyl Peptidase
GLP Receptor
P-glycoprotein
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Metabolic Disease
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Carmegliptin (RO-4876904) is an orally active and potent DPP IV inhibitor with a human DPP IV IC50 of 6.8 nM. Carmegliptin binds to the S1 pocket of DPP IV, blocks the degradation of GLP 1, potentiates endogenous GLP 1, increases plasma insulin levels, alleviates hyperglycemia, improves glucose tolerance. Carmegliptin acts as a substrate for human P glycoprotein without inhibiting the transporter, shows low in vitro cell permeability. Carmegliptin can be used for the research of type 2 diabetes, non insulin dependent diabetes mellitus .
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- HY-N8518R
-
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Reference Standards
Phospholipase
p38 MAPK
Apoptosis
NF-κB
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Metabolic Disease
Inflammation/Immunology
Cancer
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Malabaricone C is an orally active and noncompetitive sphingomyelin synthase (SMS) inhibitor with IC50 values of 3 μM and 1.5 μM for SMS 1 and SMS 2, respectively. Malabaricone C reduces body weight gain, improves glucose tolerance, and decreases lipid accumulation in the liver, showing significant prevention of high fat diet-induced fatty liver in mice. Malabaricone C has anti-inflammatory effects, which is found in the fruits of Myristica cinnamomea King. Malabaricone C is promising for research of obesity and immunological disorders caused due to hyper-activation of T-cells .
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- HY-P4610
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GLP Receptor
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Metabolic Disease
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H-Trp-Tyr-OH is an orally active tryptophan-tyrosine dipeptide with blood-brain barrier permeability. H-Trp-Tyr-OH exerts physiological regulatory effects by stimulating enteroendocrine cells to secrete glucagon-like peptide GLP-1. In mouse models of tauopathies, H-Trp-Tyr-OH inhibits tau phosphorylation, reduces the level of neurofibrillary tangles, increases dopamine turnover, upregulates synapsin expression, and elevates cecal short-chain fatty acid levels, thereby improving behavioral deficits and extending lifespan. H-Trp-Tyr-OH can be used in research related to impaired glucose tolerance and tauopathies .
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- HY-N2593R
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Reference Standards
Carnitine Palmitoyltransferase (CPT)
Reactive Oxygen Species (ROS)
Autophagy
Apoptosis
NF-κB
PI3K
Akt
MMP
Keap1-Nrf2
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Inflammation/Immunology
Cancer
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Isorhapontigenin (Standard) is the analytical standard of Isorhapontigenin (HY-N2593). This product is intended for research and analytical applications. Isorhapontigenin is an orally active dietary polyphenol. Isorhapontigenin acts as a potent antioxidant that reduces the production of reactive oxygen species (ROS). Isorhapontigenin promotes the binding of JUN to the AP-1 site on the SESN2 promoter, induces SESN2 transcription, triggers MAPK8-dependent JUN activation, and upregulates the expression of PPAR-α, PGC-1α and CPT-1A to facilitate fatty acid oxidation. Isorhapontigenin induces autophagy, apoptosis and preadipocyte differentiation; it inhibits tumor growth, cell invasion, NF-κB transcriptional activity, the PI3K/Akt signaling pathway, STAT1 phosphorylation and MMP-2 expression. Isorhapontigenin alleviates oxidative stress, inflammatory cytokine release and triglyceride accumulation; it increases intracellular ATP levels and promotes Nrf2 nuclear translocation. Isorhapontigenin improves insulin sensitivity in adipose tissue and glucose tolerance, and reduces postprandial blood glucose, insulin and free fatty acid levels. Isorhapontigenin is applicable to research on bladder cancer, liver injury, chronic obstructive pulmonary disease, acute lung injury and type 2 diabetes.
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- HY-160156
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Somatostatin Receptor
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Metabolic Disease
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SSTR5 antagonist 4 (compound 1) is a potent, selective and orally active somatostatin subtype 5 (SSTR5) antagonist (hSSTR5 IC50 = 1.3 nM, mSSTR5 IC50 = 1.0 nM). SSTR5 antagonist 4 shows efficacy in mouse oral glucose tolerance test (OGTT) in high fat diet (HFD)-mice. SSTR5 antagonist 4 can be used for type 2 diabetes research .
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- HY-182454
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GPR119
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Metabolic Disease
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GPR119 agonist 4 is a GPR119 agonist and oral glucose-lowering agent with a human GPR119 EC50 of 42 nM.GPR119 agonist 4 activates GPR119.GPR119 agonist 4 reduces blood glucose area under the curve in an oral glucose tolerance test.GPR119 agonist 4 exhibits improved clearance in liver microsomes.GPR119 agonist 4 can be used for the research of type 2 diabetes mellitus .
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- HY-179419
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Glucokinase
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Metabolic Disease
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Glucokinase activator 10, a thiazole-based compound, is a liver-selective and orally active glucokinase activator with an EC50 of 42 nM. Glucokinase activator 10 exhibits significant glucose lowering in acute diet-induced obese mouse oral glucose tolerance (OGTT) test. Glucokinase activator 10 can be used for the study of metabolic disorders .
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- HY-182300
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Dipeptidyl Peptidase
GLP Receptor
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Metabolic Disease
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FE 999011 is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor with IC50 values of 7 nM and 3 nM against human and rat sources, respectively. FE 999011 acts as a glucose tolerance-improving agent and a GLP-1 receptor activator, which reduces blood glucose fluctuation, promotes GLP-1 release and decreases the insulin-glucose ratio. FE 999011 regulates lipid metabolism, delays the onset of diabetes, stabilizes food and water intake, reduces hypertriglyceridemia, prevents the elevation of free fatty acids, and delays the progression of impaired glucose tolerance to disease. FE 999011 can be used in relevant studies of type 2 diabetes .
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- HY-110197A
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IDE
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Metabolic Disease
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6bK formate is a potent and selective insulin degrading enzyme (IDE) inhibitor with an IC50 value of 50 nM. 6bK formate increases circulating insulin in high-fat-fed mice. Acute administration of 6bK formate enhances glucose tolerance to oral glucose, notably to a greater extent in high-fat-fed mice. 6bK formate can be used for type 2 diabetes research .
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- HY-182580
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GPR119
Dipeptidyl Peptidase
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Metabolic Disease
Inflammation/Immunology
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HBK001 is an orally active and selective dual GPR119 agonist and DPP-IV inhibitor. HBK001 triggers cAMP production, PKA activation, CREB phosphorylation, glucose-stimulated insulin secretion, plasma incretin elevation, β-cell proliferation, and β-cell function gene up-regulation. HBK001 reduces blood glucose, ameliorates hyperglycemia, improves glucose tolerance, and enhances islet morphology. HBK001 can be used for the research of type 2 diabetes mellitus .
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- HY-181094
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Glycosidase
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Metabolic Disease
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α-Glucosidase-IN-110 is a selective and orally active competitive inhibitor of α-Glucosidase with an IC50 of 7.09 μM and a Ki of 6.9 μM. α-Glucosidase-IN-110 can reduce fasting blood glucose levels, improve glucose tolerance, and restore the histomorphology of liver and pancreatic tissues in diabetic rat models. α-Glucosidase-IN-110 can be used for the research of diabetes .
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- HY-180415
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11β-HSD
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Metabolic Disease
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UE2316 is an orally active and specific 11βHSD1 inhibitor. UE2316 significantly improves glucose tolerance and insulin sensitivity in uremic rats. UE2316 also exacerbates hepatic fibrosis in mice. UE2316 can be used in the research of diseases such as hepatic fibrosis, uremia and diabetes mellitus .
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- HY-182558
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Drug Derivative
AMPK
IKK
NF-κB
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Metabolic Disease
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Nandinine is an orally active derivative of Berberine (HY-N0716). Nandinine enhances AMPK activity, inhibits the activation of IKKβ/NF-κB, and regulates the phosphorylation of IRS-1. Nandinine reverses the abnormal production of adipokines, promotes insulin-mediated glucose uptake, and alleviates insulin resistance. Nandinine improves glucose tolerance and increases the insulin sensitivity index in mice. Nandinine can be used in studies related to insulin resistance .
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- HY-173130
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Glycosidase
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Metabolic Disease
Inflammation/Immunology
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α-Glucosidase-IN-86 (Compound A4) is an orally active α-glucosidase inhibitor with an IC50 of 2.72 μM. α-Glucosidase-IN-86 has high safety in mice. α-Glucosidase-IN-86 can reduce fasting blood glucose levels, improve glucose tolerance, regulate blood lipids, and has antioxidant effects in diabetic mice. α-Glucosidase-IN-86 can be used for the research of diabetes .
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- HY-125646
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GPR119
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Metabolic Disease
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YH18968 is an orally active GPR119 agonist with an EC50 of 2.8 nM for inducing cAMP accumulation. YH18968 activates GPR119, elevates intracellular cyclic adenosine monophosphate levels, stimulates glucagon-like peptide-1 secretion from intestinal L cells, and triggers glucose-dependent insulin secretion from pancreatic β cells. YH18968 improves glucose tolerance in normal mice and diet-induced obese mice. YH18968 can be used for the research of type 2 diabetes .
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- HY-182250
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FAP
ERK
GLUT
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Metabolic Disease
Inflammation/Immunology
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BR103354 is an orally active, selective fibroblast activation protein (FAP) inhibitor with an IC50 value of 14 nM against hFAP. BR103354 restores the levels of phosphorylated ERK and Glut1 that are reduced by co-treatment with hFGF21 and FAP, decreases non-fasting blood glucose concentrations, improves glucose tolerance, and reduces hepatic triglyceride content. BR103354 ameliorates hepatic steatosis and hepatic fibrosis. BR103354 can be used in the research of type 2 diabetes and non-alcoholic steatohepatitis .
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-
- HY-180936
-
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FBPase
AMPK
mTOR
Ribosomal S6 Kinase (RSK)
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Metabolic Disease
|
|
FBPase-IN-6 (Compound 96) is an orally active FBPase inhibitor with an IC50 value of 1.769 μM. FBPase-IN-6 modulates AMPK/mTORC1/S6K signaling pathways. FBPase-IN-6 improves glucose tolerance, enhances insulin sensitivity, and promotes insulin secretion in type 2 diabetic mice .
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- HY-183489
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Trace Amine-associated Receptor (TAAR)
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Neurological Disease
Metabolic Disease
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TAAR1-agonist-4 is a TAAR1 agonist and oral hypoglycemic agent with an EC50 of 0.0046 μM for TAAR1. TAAR1-agonist-4 alleviates antipsychotic-related metabolic side effects, improves negative and cognitive symptoms, and reduces drug abuse behaviors. TAAR1-agonist-4 is applicable to research on schizophrenia, acute manic episodes associated with bipolar disorder, and glucose intolerance .
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-
- HY-139792
-
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SHR117887
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Endogenous Metabolite
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Metabolic Disease
|
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Besigliptin tosylate (SHR117887) is a DPP-4 inhibitor with activity to improve metabolic control and β-cell function. Besigliptin tosylate can effectively reduce serum DPP-4 activity and improve oral glucose tolerance. Besigliptin tosylate significantly reduces fasting blood glucose levels and improves lipid profiles in a diabetic mouse model. The effect of besigliptin tosylate is comparable to that of the known compound vildagliptin (HY-14291) at the same concentration. Besigliptin tosylate increases insulin staining of pancreatic islet cells in chronic administration, indicating improved β-cell function .
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-
- HY-182280
-
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Insulin Receptor
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Metabolic Disease
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BDM71230 is an orally active inducer of insulin-degrading enzyme (IDE), with an EC50 of 1.9 μM against human IDE. BDM71230 binds to the interface of IDE dimers and enhances the catalytic activity of IDE via steric effects. BDM71230 can potentiate the hydrolytic effect of IDE on insulin and slightly attenuate the hypoglycemic effect of insulin. BDM71230 serves as a pharmacological tool for investigating IDE function and is applicable to studies related to glucose intolerance .
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- HY-181102
-
|
|
G protein-coupled Bile Acid Receptor 1
|
Metabolic Disease
Inflammation/Immunology
|
|
TGR5 agonist 10 is a selective, allosteric and orally active Takeda G protein coupled receptor 5 (TGR5) agonist with EC50s of 0.8 μM and 0.6 μM for human TGR5 and mouse TGR5, respectively. TGR5 agonist 10 demonstrates selectivity for TGR5 over FXR. TGR5 agonist 10 activates hTGR5 and mTGR5 to induce cAMP accumulation, and positively modulates lithocholic acid functional activity and potency at hTGR5, with higher selectivity for cAMP formation over β-arrestin2 recruitment. TGR5 agonist 10 exerts glucose-lowering effects in Mus musculus oral glucose tolerance tests. TGR5 agonist 10 can be used for the research of diabetes .
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- HY-182729
-
|
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Free Fatty Acid Receptor
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Metabolic Disease
|
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FFA2 agonist-2 is a potent agonist of the FFA2 (GPR43) receptor, with a pEC50 of 7.9 for human FFA2, and a pEC50 of 7.3 for murine FFA2. FFA2 agonist-2 acts as an orthosteric agonist and shows no obvious cross‑activity against FFA1, FFA3 and FFA4. FFA2 agonist-2 can be used for FFA2 receptor research in type 2 diabetes and metabolic disorders .
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- HY-10289A
-
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RO-4876904 hydrochloride
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Dipeptidyl Peptidase
GLP Receptor
P-glycoprotein
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Metabolic Disease
|
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Carmegliptin hydrochloride (RO-4876904 hydrochloride) is an orally active and potent DPP‑IV inhibitor with a human DPP‑IV IC50 of 6.8 nM. Carmegliptin hydrochloride binds to the S1 pocket of DPP‑IV, blocks the degradation of GLP‑1, potentiates endogenous GLP‑1, increases plasma insulin levels, alleviates hyperglycemia, improves glucose tolerance. Carmegliptin hydrochloride acts as a substrate for human P‑glycoprotein without inhibiting the transporter, shows low in vitro cell permeability. Carmegliptin hydrochloride can be used for the research of type 2 diabetes, non‑insulin‑dependent diabetes mellitus .
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-
- HY-180845
-
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|
G protein-coupled Bile Acid Receptor 1
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Metabolic Disease
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|
TGR5 agonist 9 is a highly selective and orally active TGR5 allosteric agonist with EC₅₀ values for hTGR5 and mTGR5 of 0.48 and 0.49 μM, respectively. TGR5 agonist 9 can recruit β-arrestin 1 (EC₅₀ = 78.8 μM) and β-arrestin 2 (EC₅₀ = 12.3 μM), and has a higher efficacy in cAMP accumulation (EC₅₀ = 0.48 μM). TGR5 agonist 9 exhibits a significant hypoglycemic effect in the ICR mouse model. TGR5 agonist 9 can be used for research on diabetes .
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- HY-182046
-
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MNK
PPAR
Eukaryotic Initiation Factor (eIF)
Stearoyl-CoA Desaturase (SCD)
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Metabolic Disease
|
|
HD202A is an orally active, selective dual inhibitor of MNK1/MNK2 (with IC50 values of 6.09 nM and 8.06 nM, and Kd values of 1.913 μM and 5.244 μM, respectively) that inhibits the MNK-eIF4E signaling pathway. By downregulating perilipin 2 and SCD1, while upregulating adipose triglyceride lipase and PPARγ coactivator 1α, HD202A enhances mitochondrial fatty acid oxidation and redox homeostasis. HD202A effectively suppresses body weight gain, hepatic lipid accumulation and elevation of serum lipids, significantly improves glucose tolerance and insulin sensitivity of the organism, and ameliorates inflammatory features. With these comprehensive pharmacological activities, HD202A exhibits great application potential in studies of metabolic dysfunction-associated steatotic liver disease .
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-
- HY-182905
-
|
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Somatostatin Receptor
G protein-coupled Bile Acid Receptor 1
|
Metabolic Disease
|
|
SSTR5/TGR5-modulator-1 is an orally active and dual-target small molecule, balanced in vitro activity at human TGR5 and human SSTR5. SSTR5/TGR5-modulator-1 activates human TGR5 to promote cAMP accumulation. SSTR5/TGR5-modulator-1 blocks human SSTR5 to inhibit agonist-induced calcium mobilization. SSTR5/TGR5-modulator-1 improves glucose tolerance in mice. SSTR5/TGR5-modulator-1 alleviates gallbladder filling in mice at pharmacologically relevant doses. SSTR5/TGR5-modulator-1 has suboptimal physicochemical and metabolic properties.SSTR5/TGR5-modulator-1 can be used for the research of type 2 diabetes mellitus .
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-
- HY-182346
-
|
|
FBPase
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Metabolic Disease
|
|
FBPase-IN-7 is a fructose-1,6-bisphosphatase (FBPase) inhibitor with an IC50 of 0.75 μM. FBPase-IN-7 binds to a cryptic allosteric pocket of FBPase, induces conformational rearrangement of key residues, forms a hydrogen-bond network, and disrupts substrate catalysis. FBPase-IN-7 confirms cellular stabilizes HuFBPase in hepatic cells. FBPase-IN-7 has hypoglycemic activity. FBPase-IN-7 can be used for the research of type 2 diabetes .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-W003222
-
|
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Drug Intermediate
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Metabolic Disease
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N-tert-Boc-cis-4-fluoro-L-proline (Compound 11) is a drug intermediate for the synthesis of 4-fluoropyrrolidine-2-carbonitrile DPP-4 inhibitor. N-tert-Boc-cis-4-fluoro-L-proline can be used to study type 2 diabetes .
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- HY-P4610
-
|
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GLP Receptor
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Metabolic Disease
|
|
H-Trp-Tyr-OH is an orally active tryptophan-tyrosine dipeptide with blood-brain barrier permeability. H-Trp-Tyr-OH exerts physiological regulatory effects by stimulating enteroendocrine cells to secrete glucagon-like peptide GLP-1. In mouse models of tauopathies, H-Trp-Tyr-OH inhibits tau phosphorylation, reduces the level of neurofibrillary tangles, increases dopamine turnover, upregulates synapsin expression, and elevates cecal short-chain fatty acid levels, thereby improving behavioral deficits and extending lifespan. H-Trp-Tyr-OH can be used in research related to impaired glucose tolerance and tauopathies .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N8518
-
-
-
- HY-N2593
-
|
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Structural Classification
Stilbenes
Classification of Application Fields
Gnetum cleistostachyum C. Y. Cheng
Phenols
Polyphenols
Gnetaceae
Plants
Inflammation/Immunology
Disease Research Fields
Source Classification
|
Carnitine Palmitoyltransferase (CPT)
Reactive Oxygen Species (ROS)
Autophagy
Apoptosis
NF-κB
PI3K
Akt
MMP
Keap1-Nrf2
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Isorhapontigenin is an orally active dietary polyphenol. Isorhapontigenin acts as a potent antioxidant that reduces the production of reactive oxygen species (ROS). Isorhapontigenin promotes the binding of JUN to the AP-1 site on the SESN2 promoter, induces SESN2 transcription, triggers MAPK8-dependent JUN activation, and upregulates the expression of PPAR-α, PGC-1α and CPT-1A to facilitate fatty acid oxidation. Isorhapontigenin induces autophagy, apoptosis and preadipocyte differentiation; it inhibits tumor growth, cell invasion, NF-κB transcriptional activity, the PI3K/Akt signaling pathway, STAT1 phosphorylation and MMP-2 expression. Isorhapontigenin alleviates oxidative stress, inflammatory cytokine release and triglyceride accumulation; it increases intracellular ATP levels and promotes Nrf2 nuclear translocation. Isorhapontigenin improves insulin sensitivity in adipose tissue and glucose tolerance, and reduces postprandial blood glucose, insulin and free fatty acid levels. Isorhapontigenin is applicable to research on bladder cancer, liver injury, chronic obstructive pulmonary disease, acute lung injury and type 2 diabetes .
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-
-
- HY-N0936
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-
-
- HY-N15721
-
|
Trp-CA
|
Triterpenes
Structural Classification
Terpenoids
Endogenous metabolite
Source Classification
|
Orphan GPCR
GLP Receptor
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|
Tryptophan-cholic acid (Trp-CA) is a microbial amino acid-conjugated bile acid that acts as an endogenous ligand and agonist (EC50=9.6 μM) for the orphan G protein-coupled receptor (GPCR) MRGPRE (Mas-related G protein-coupled receptor family member E). Tryptophan-cholic acid is orally effective but has poor oral absorption and does not cross the blood-brain barrier. Tryptophan-cholic acid promotes the secretion of glucagon-like peptide GLP-1, thereby improving glucose tolerance in diabetic mice. Tryptophan-cholic acid improves glucose tolerance, promotes insulin secretion, and alleviates high-fat diet-induced hepatic steatosis without causing pruritus side effects. Tryptophan-cholic acid is primarily used in research on type 2 diabetes (T2D) .
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-
-
- HY-N2486
-
-
-
- HY-N15135
-
|
|
Structural Classification
Polysaccharides
Antibiotics
Leguminosae
Pisum sativum Linn
Plants
Saccharides
Other Antibiotics
Source Classification
|
Interleukin Related
Toll-like Receptor (TLR)
Fungal
|
|
Arabinoxylan Medium viscosity is an orally active Dectin-1 splice variant modulator, glucose absorption inhibitor, and chyme viscosity enhancer. Arabinoxylan Medium viscosity inhibits particulate β-glucan-induced Dectin-1A activation and mildly suppresses Dectin-1B activation. In human dendritic cells stimulated with particulate β-glucan, Arabinoxylan Medium viscosity reduces the production of IL-10 and TNF-α, and increases the production of IL-4 and IL-23. Arabinoxylan Medium viscosity also supports antifungal immune responses without activating TLR2, TLR4 or TLR5, and does not induce cytokine production when used to stimulate human dendritic cells alone. Arabinoxylan Medium viscosity increases small intestinal chyme viscosity, gets degraded in the large intestine to produce short-chain fatty acids, reduces glucose absorption and insulin response, and improves glucose homeostasis. Arabinoxylan Medium viscosity supports microbial fermentation and the growth of beneficial microbiota in the gastrointestinal tract, prevents bile acid reabsorption, and delays starch digestion. Arabinoxylan Medium viscosity can be used in research related to type 2 diabetes, impaired glucose tolerance, and metabolic syndrome .
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-
-
- HY-N2486R
-
-
-
- HY-N11262
-
|
|
Structural Classification
Flavonoids
Flavones
Rutaceae
Citrus sudachi Hort. ex Shirai.
Plants
Source Classification
|
Phosphodiesterase (PDE)
Sirtuin
PGC-1α
p38 MAPK
HSP
TNF Receptor
NO Synthase
Apoptosis
|
|
Sudachitin is an orally active compound that potently inhibits mouse PDE1C and human PDE4B, with IC50 values of 5.0 μM and 15.0 μM, respectively. Sudachitin upregulates Sirt1 and PGC‑1α expression in skeletal muscle to regulate energy metabolism and promote mitochondrial biogenesis. Sudachitin improves lipid metabolism, glucose tolerance, insulin sensitivity, energy expenditure, and fatty acid β‑oxidation. Sudachitin activates p38MAPK signaling, induces HSP27 phosphorylation and caspase‑dependent apoptosis, and blocks EGF‑driven keratinocyte migration and proliferation. Sudachitin suppresses LPS‑induced TNF‑α, NO, and iNOS expression in macrophages and shows potent anti‑inflammatory activity. Sudachitin can be used for the research of metabolic syndrome, type 2 diabetes, and psoriasis. .
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-
-
- HY-N0936R
-
-
-
- HY-N8518R
-
-
-
- HY-N2593R
-
|
|
Structural Classification
Stilbenes
Gnetum cleistostachyum C. Y. Cheng
Phenols
Polyphenols
Gnetaceae
Plants
Source Classification
|
Reference Standards
Carnitine Palmitoyltransferase (CPT)
Reactive Oxygen Species (ROS)
Autophagy
Apoptosis
NF-κB
PI3K
Akt
MMP
Keap1-Nrf2
|
|
Isorhapontigenin (Standard) is the analytical standard of Isorhapontigenin (HY-N2593). This product is intended for research and analytical applications. Isorhapontigenin is an orally active dietary polyphenol. Isorhapontigenin acts as a potent antioxidant that reduces the production of reactive oxygen species (ROS). Isorhapontigenin promotes the binding of JUN to the AP-1 site on the SESN2 promoter, induces SESN2 transcription, triggers MAPK8-dependent JUN activation, and upregulates the expression of PPAR-α, PGC-1α and CPT-1A to facilitate fatty acid oxidation. Isorhapontigenin induces autophagy, apoptosis and preadipocyte differentiation; it inhibits tumor growth, cell invasion, NF-κB transcriptional activity, the PI3K/Akt signaling pathway, STAT1 phosphorylation and MMP-2 expression. Isorhapontigenin alleviates oxidative stress, inflammatory cytokine release and triglyceride accumulation; it increases intracellular ATP levels and promotes Nrf2 nuclear translocation. Isorhapontigenin improves insulin sensitivity in adipose tissue and glucose tolerance, and reduces postprandial blood glucose, insulin and free fatty acid levels. Isorhapontigenin is applicable to research on bladder cancer, liver injury, chronic obstructive pulmonary disease, acute lung injury and type 2 diabetes.
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