Search Result
Results for "
glucose tolerance
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N8522
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Others
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Metabolic Disease
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9,10-Dihydroxystearic acid is an oxidation product of oleic acid. 9,10-Dihydroxystearic acid can improve glucose tolerance and insulin sensitivity in KKAy mice .
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- HY-123297
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Free Fatty Acid Receptor
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Metabolic Disease
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TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes .
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- HY-N9410
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1-Linoleoyl-2-Hydroxy-sn-glycero-3-PC; LPC(18:2/0:0); LysoPC(18:2)
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Endogenous Metabolite
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Metabolic Disease
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Lysophosphatidylcholine 18:2 (1-Linoleoyl-2-Hydroxy-sn-glycero-3-PC), a lysophospholipid, is a potential biomarker identified from insulin resistance (IR) polycystic ovary syndrome (PCOS). Low plasma Lysophosphatidylcholine 18:2 also has been shown to predict impaired glucose tolerance, insulin resistance, type 2 diabetes, coronary artery disease, and memory impairment .
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- HY-N7515
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2',4',6'-Trihydroxychalcone
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Bacterial
AMPK
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Infection
Metabolic Disease
Inflammation/Immunology
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Pinocembrin chalcone (2',4',6'-Trihydroxychalcone) is an antibacterial compound from Helichrysum Trilineatum. Pinocembrin chalcone facilitates AMP-activated protein kinase (AMPK) activation, improves glucose tolerance, increases muscle FAO and reduces fat accumulation in the liver and skeletal muscles in high-fat diet-induced (HFD) diabetic mice. Pinocembrin chalcone is promising for research of gastric ulcers and diabetes .
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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-178982
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Apelin Receptor (APJ)
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Metabolic Disease
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Apelin agonist 2 is an orally effective 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-N0936R
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6-Methoxy-2-benzoxazolinone (Standard); 6-MBOA (Standard)
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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-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-17538A
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PGC-1α
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Metabolic Disease
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ZLN005 (hydrochloride) is a peroxisome proliferator-activated receptor-g coactivator-1a (PGC-1α) activator. ZLN005 (hydrochloride) can stimulate the expression of PGC-1α and downstream genes in skeletal muscle cells, improve glucose utilization and fatty acid oxidation. ZLN005 (hydrochloride) can increase the transcription of PGC-1α and downstream genes in skeletal muscle of diabetic db/db mice, increase fat oxidation and improve glucose tolerance, pyruvate tolerance and insulin sensitivity .
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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-170874
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PPAR
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Metabolic Disease
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PPARγ modulator-2 (Compound (R)-2n) is the reversible modulator for PPARγ that inhibits PPARγ ligand-binding domain (LBD) with an IC50 of 41 nM. PPARγ modulator-2 reduces blood glucose, improves the glucose tolerance and insulin tolerance, and exhibits anti-diabetic efficacy in db/db mouse models .
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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-150012
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- HY-117830
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Phosphatase
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Endocrinology
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CX08005 is a competitive PTP1B inhibitor. CX08005 can directly enhance the action of insulin in vivo and in vitro and improve insulin resistance .
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- HY-N13082
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Others
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Metabolic Disease
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Deacetylescin Ia (compound 12) is a deacetylated compound with anti-hyperglycemic effects that can be extracted from the debittered Aesculus and deacetylated at the C-22 position. Deacetylescin Ia (100 mg/kg) can inhibit blood glucose elevation in mouse glucose tolerance tests .
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- HY-164781
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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-117446
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GPR119
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Metabolic Disease
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AS-1669058 is a GPR119 agonist and a potential inhibitor of type 2 diabetes. AS-1669058 induces insulin secretion in response to high blood glucose levels in vitro and in vivo and increases insulin promoter activity. In animal studies, AS-1669058 improved glucose tolerance and reduced blood glucose levels in db/db mice .
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- HY-125025
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- HY-117446A
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GPR119
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Metabolic Disease
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AS-1669058 free base is a GPR119 agonist and a potential inhibitor of type 2 diabetes. AS-1669058 free base induces insulin secretion induced by high blood glucose levels in vitro and in vivo and increases insulin promoter activity. In animal studies, AS-1669058 free base improved glucose tolerance and reduced blood glucose levels in db/db mice.
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- HY-110197
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6bK TFA
1 Publications Verification
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Others
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Metabolic Disease
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6bK TFA is a potent and selective insulin degrading enzyme (IDE) inhibitor with an IC50 value of 50 nM. 6bK TFA increases circulating insulin in high-fat-fed mice. Acute administration of 6bK TFA enhances glucose tolerance to oral glucose, notably to a greater extent in high-fat-fed mice .
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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-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-W709961
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1-(3-Carboxypropyl)tetradecyl (9Z)-9-octadecenoate
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Endogenous Metabolite
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Metabolic Disease
Inflammation/Immunology
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5-OAHSA (1-(3-Carboxypropyl)tetradecyl (9Z)-9-octadecenoate) is a endogenous lipid. 5-OAHSA reduces the level of blood glucose, improves the glucose tolerance, and stimulates the the secretion of GLP-1 and insulin. 5-OAHSA exhibits potential in regulating metabolic and inflammatory responses .
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- HY-169411
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Glycosidase
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Metabolic Disease
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α-Glucosidase-IN-77 (Compound H7) is a non-competitive inhibitor for α-glucosidase with an IC50 of 1.25 μM. α-Glucosidase-IN-77 lowers blood glucose levels, improves glucose tolerance, regulates intestinal microbiota, and exhibits hepatoprotective effect in mouse type 2 diabetes model .
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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-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 polyphenol extracted from coix (Coix lachryma-jobi L.var.ma-yuen Stapf) with antimicrobial and antitumor activities .
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- HY-129736A
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Dipeptidyl Peptidase
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Metabolic Disease
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P32/98 a potent inhibitor of dipeptidyl peptidase IV with a Ki value of 130 nM. P32/98 improves glucose tolerance, insulin sensitivity and β-cell responsiveness in fatty Zucker rat model .
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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-131334
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AMPK
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Metabolic Disease
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AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect .
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- HY-129736
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Dipeptidyl Peptidase
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Metabolic Disease
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P32/98 hemifumarateis a potent inhibitor of dipeptidyl peptidase IV with a Ki value of 130 nM. P32/98 hemifumarate improves glucose tolerance, insulin sensitivity and β-cell responsiveness in fatty Zucker rat model .
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- HY-150012R
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Endogenous Metabolite
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Metabolic Disease
Endocrinology
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N-Lactoyl-Phenylalanine (Standard) is the analytical standard of N-Lactoyl-Phenylalanine. This product is intended for research and analytical applications. N-Lactoyl-Phenylalanine is a blood-derived signaling metabolite that can be induced by exercise. N-Lactoyl-Phenylalanine can reduce obesity and improve glucose tolerance .
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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-133180
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Wnt
β-catenin
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Metabolic Disease
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YW1128 (compound 3a) is a potent Wnt/β-Catenin inhibitor. YW1128 induces the proteasome degradation of β-catenin and subsequent inhibits the Wnt/β-catenin signaling in cells. YW1128 significantly decreases hepatic lipid accumulation. YW1128 improves glucose tolerance of high fat diet-fed mice without noticeable toxicity. YW1128 down regulates the genes involved in the glucose and fatty acid anabolism .
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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-117459
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PPAR
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Metabolic Disease
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E-3030 free acid is a potent dual activator of peroxisome proliferator-activated receptor (PPAR) alpha and PPARgamma, exhibiting significant antidiabetic and lipid-modulating effects. E-3030 decreases blood glucose, triglyceride, non-esterified fatty acids, and insulin levels, while increasing blood adiponectin levels. E-3030 improves glucose tolerance and shows remarkable triglyceride- and non-high-density lipoprotein cholesterol-lowering effects in animal models.
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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-150012S1
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- HY-P1434
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Insulin Receptor
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Metabolic Disease
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[Pro3]-GIP (mouse) is a GIP receptor antagonist (IC50: 2.6 μM). [Pro3]-GIP (mouse) improves glucose tolerance and insulin sensitivity in ob/ob mice. [Pro3]-GIP (mouse) can be used for research of type 2 diabetes .
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- HY-175701
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RO7795081; RG6652
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GLP Receptor
Arrestin
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Metabolic Disease
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CT-996 is an orally active GLP-1RA agonist, with an EC50 of 0.49 nM. CT-996 reduces the β-arrestin recruitment and GLP-1R internalization. CT-996 suppresses postprandial blood glucose following a mixed meal tolerance test (MMTT) in mice expressing the human GLP-1 receptor and enhances glucose stimulated insulin secretion (GSIS) during an intravenous glucose challenge in obese monkeys. CT-996 can be used for the study of type 2 diabetes (T2D) and obesity .
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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-146725
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FBPase
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Metabolic Disease
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FBPase-IN-1 is a potent FBPase (Fructose-1,6-bisphosphatase) inhibitor for Type 2 diabetes (T2D) study with an IC50 of 0.22 μM. FBPase-IN-1 can reduce blood glucose levels and ameliorate glucose tolerance. FBPase-IN-1 modifies the C128 site, regulates the N125-S124-S123 allosteric pathway of FBPase and affects the catalytic activity of FBPase .
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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-P0165B
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ITM077 acetate; R1583 acetate; BIM51077 acetate
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GLP Receptor
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Metabolic Disease
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Taspoglutide (R1583) acetate is an agonist of the glucagon-like peptide 1 receptor (GLP-1R) with an Ki value of 1.1 nM. Taspoglutide acetate induces cAMP accumulation in CHO-K1 cells expressing human GLP-1R (EC50 = 0.06 nM). Taspoglutide acetate decreases blood levels of glucose and increases blood levels of insulin in a glucose tolerance test in Zucker diabetic obese rats. Taspoglutide acetate reduces blood levels of gastric inhibitory polypeptide (GIP), plasma levels of triglycerides, and body weight in the same model .
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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-106863
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Adrenergic Receptor
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Metabolic Disease
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BRL 35135 is a potent and selective β3-adrenergic receptor agonist. BRL 35135 can dose dependently increase energy expenditure, reduce weight, and only reduce fat without reducing muscle protein. BRL 35135 can significantly improve glucose tolerance and insulin sensitivity. BRL 35135 can be used to study metabolic conditions such as obesity and diabetes .
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- HY-13991A
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Ras
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Metabolic Disease
Cancer
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(S)-CCG-1423 is an inhibitor of Rho signaling that blocks the nuclear import of MRTF-A. (S)-CCG-1423 reduces the nuclear accumulation of MRTF-A and improves glucose uptake and tolerance in insulin-resistance mice in vivo. (S)-CCG-1423 exhibits higher inhibition activity than the SR- and the R-isomers of CCG-1423 (HY-13991). (S)-CCG-1423 can be used for the research of cancer and 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-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-N15721
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Trp-CA
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Orphan GPCR
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Metabolic Disease
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Tryptophan-cholic acid (Trp-CA) is a microbial amino-acid-conjugated bile acid, serving as an endogenous ligand and agonist of the orphan G protein-coupled receptor (GPCR) MRGPRE. Tryptophan-cholic acid activates MRGPRE, promoting the secretion of glucagon-like peptide-1 (GLP-1) through the Gs-cAMP and β-arrestin-1-ALDOA signaling pathways, thereby improving glucose tolerance in diabetic mice. Tryptophan-cholic acid is promising for research of type 2 diabetes .
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- HY-13991R
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Ras
Apoptosis
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Cancer
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CCG-1423 (Standard) is the analytical standard of CCG-1423. This product is intended for research and analytical applications. CCG-1423 is an inhibitor of Rho/MRTF/SRF pathway. CCG-1423 shows activities in several cancer cells. CCG-1423 is a promising lead compound for the development of novel pharmacologic tools, and it can be used for the research of cancer and diabetes .
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- HY-13991
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Ras
Apoptosis
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Cancer
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CCG-1423 is an inhibitor of Rho/MRTF/SRF pathway. CCG-1423 shows activities in several cancer cells. CCG-1423 is a promising lead compound for the development of novel pharmacologic tools, and it can be used for the research of cancer and diabetes .
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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-121744
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PS10
5 Publications Verification
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PDHK
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Inflammation/Immunology
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PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM) . PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy .PDK: pyruvate dehydrogenase kinase
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- HY-N8518R
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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-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-12443
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Casein Kinase
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Neurological Disease
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PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid agent-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner . PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity .
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- HY-P3247
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Insulin Receptor
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Neurological Disease
Metabolic Disease
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[D-Ala2]-GIP (human) is a GIP receptor agonist (EC50 = 630 pM). [D-Ala2]-GIP (human) improves glucose tolerance. [D-Ala2]-GIP (human) shows neuroprotective activity in MPTP (HY-W114750)-induced Parkinson's disease model. [D-Ala2]-GIP (human) also improves cognitive function and hippocampal synaptic plasticity in obese diabetic rats. [D-Ala2]-GIP (human) can be used for research of type 2 diabetes, Parkinson's disease, etc
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- HY-128578
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PDHK
NO Synthase
Interleukin Related
HIF/HIF Prolyl-Hydroxylase
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Metabolic Disease
Inflammation/Immunology
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KPLH1130 is a pyruvate dehydrogenase kinase (PDK) inhibitor. KPLH1130 potently inhibits M1 macrophage polarization by reducing the expression of pro-inflammatory cytokines, decreasing the levels of M1 phenotype markers (HIF-1α, iNOS) and nitric oxide (NO) production. KPLH1130 prevents the reduction of mitochondrial oxygen consumption rate (OCR) induced by inflammatory stimuli (LPS ((HY-D1056) + IFN-γ) in various macrophage types. KPLH1130 improves glucose tolerance in HFD-fed mice. KPLH1130 can be used for the study of obesity-associated metabolic disorders and other inflammatory conditions .
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- HY-155156
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Endogenous Metabolite
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Cardiovascular Disease
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PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC50=19 nM). PF-07238025 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice .
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- HY-155157
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Endogenous Metabolite
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Cardiovascular Disease
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PF-07247685 is a BCKDC kinase (BDK) inhibitor (EC50=2.2 nM). PF-07247685 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07247685 improved cardiometabolic endpoints and improves glucose tolerance in mice .
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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-126855
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7-Sulfocholic acid
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G protein-coupled Bile Acid Receptor 1
MHC
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Metabolic Disease
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Cholic acid 7-sulfate (7-Sulfocholic acid) is a selective agonist targeting TGR5 (EC50=0.17 μM) and a ligand for MHC class I-related protein (MR1). As a gut-restricted TGR5 agonist, cholic acid 7-sulfate binds to TGR5 on enteroendocrine L cells, induces GLP-1 secretion, and improves glucose tolerance in a TGR5-dependent manner. Cholic acid 7-sulfate also acts as an endogenous ligand for MR1, promoting the survival of mucosal-associated invariant T cells MAIT and the expression of homeostatic gene signatures, affecting MAIT cell development and function. Cholic acid 7-sulfate is mainly used in the research of diabetes and MAIT cell-related immune regulation .
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- HY-126855S
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7-Sulfocholic acid-d4
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Isotope-Labeled Compounds
G protein-coupled Bile Acid Receptor 1
MHC
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Metabolic Disease
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Cholic acid 7-sulfate-d4 (7-Sulfocholic acid-d4) is the deuterium labeled Cholic acid 7-sulfate (HY-126855). Cholic acid 7-sulfate is a selective agonist targeting TGR5 (EC50=0.17 μM) and a ligand for MHC class I-related protein (MR1). As a gut-restricted TGR5 agonist, cholic acid 7-sulfate binds to TGR5 on enteroendocrine L cells, induces GLP-1 secretion, and improves glucose tolerance in a TGR5-dependent manner. Cholic acid 7-sulfate also acts as an endogenous ligand for MR1, promoting the survival of mucosal-associated invariant T cells MAIT and the expression of homeostatic gene signatures, affecting MAIT cell development and function. Cholic acid 7-sulfate is mainly used in the research of diabetes and MAIT cell-related immune regulation .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1434
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Insulin Receptor
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Metabolic Disease
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[Pro3]-GIP (mouse) is a GIP receptor antagonist (IC50: 2.6 μM). [Pro3]-GIP (mouse) improves glucose tolerance and insulin sensitivity in ob/ob mice. [Pro3]-GIP (mouse) can be used for research of type 2 diabetes .
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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-P3247
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Insulin Receptor
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Neurological Disease
Metabolic Disease
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[D-Ala2]-GIP (human) is a GIP receptor agonist (EC50 = 630 pM). [D-Ala2]-GIP (human) improves glucose tolerance. [D-Ala2]-GIP (human) shows neuroprotective activity in MPTP (HY-W114750)-induced Parkinson's disease model. [D-Ala2]-GIP (human) also improves cognitive function and hippocampal synaptic plasticity in obese diabetic rats. [D-Ala2]-GIP (human) can be used for research of type 2 diabetes, Parkinson's disease, etc
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- HY-P0165B
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ITM077 acetate; R1583 acetate; BIM51077 acetate
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GLP Receptor
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Metabolic Disease
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Taspoglutide (R1583) acetate is an agonist of the glucagon-like peptide 1 receptor (GLP-1R) with an Ki value of 1.1 nM. Taspoglutide acetate induces cAMP accumulation in CHO-K1 cells expressing human GLP-1R (EC50 = 0.06 nM). Taspoglutide acetate decreases blood levels of glucose and increases blood levels of insulin in a glucose tolerance test in Zucker diabetic obese rats. Taspoglutide acetate reduces blood levels of gastric inhibitory polypeptide (GIP), plasma levels of triglycerides, and body weight in the same model .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N8522
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- HY-N9410
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- HY-N7515
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- HY-N2486
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- HY-150012
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- HY-N2486R
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- HY-N0936
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- HY-N0936R
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- HY-N13082
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- HY-150012R
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- HY-N15721
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Trp-CA
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Triterpenes
Terpenoids
Source classification
Endogenous metabolite
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Orphan GPCR
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Tryptophan-cholic acid (Trp-CA) is a microbial amino-acid-conjugated bile acid, serving as an endogenous ligand and agonist of the orphan G protein-coupled receptor (GPCR) MRGPRE. Tryptophan-cholic acid activates MRGPRE, promoting the secretion of glucagon-like peptide-1 (GLP-1) through the Gs-cAMP and β-arrestin-1-ALDOA signaling pathways, thereby improving glucose tolerance in diabetic mice. Tryptophan-cholic acid is promising for research of type 2 diabetes .
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- HY-N8518R
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Source classification
Phenols
Polyphenols
Myristicaceae
Plants
Myristica fragrans Houtt.
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Phospholipase
p38 MAPK
Apoptosis
NF-κB
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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-N8518
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- HY-155156
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Cardiovascular Disease
Classification of Application Fields
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
Disease Research Fields
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Endogenous Metabolite
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PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC50=19 nM). PF-07238025 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice .
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- HY-155157
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Cardiovascular Disease
Natural Products
Classification of Application Fields
Source classification
Endogenous metabolite
Disease Research Fields
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Endogenous Metabolite
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PF-07247685 is a BCKDC kinase (BDK) inhibitor (EC50=2.2 nM). PF-07247685 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07247685 improved cardiometabolic endpoints and improves glucose tolerance in mice .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-150012S1
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N-Lactoyl-Phenylalanine- 13C6 (Lac-Phe- 13C6) is 13C labeled N-Lactoyl-Phenylalanine. N-Lactoyl-Phenylalanine is a blood-derived signaling metabolite that can be induced by exercise. N-Lactoyl-Phenylalanine can reduce obesity and improve glucose tolerance .
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-
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- HY-126855S
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Cholic acid 7-sulfate-d4 (7-Sulfocholic acid-d4) is the deuterium labeled Cholic acid 7-sulfate (HY-126855). Cholic acid 7-sulfate is a selective agonist targeting TGR5 (EC50=0.17 μM) and a ligand for MHC class I-related protein (MR1). As a gut-restricted TGR5 agonist, cholic acid 7-sulfate binds to TGR5 on enteroendocrine L cells, induces GLP-1 secretion, and improves glucose tolerance in a TGR5-dependent manner. Cholic acid 7-sulfate also acts as an endogenous ligand for MR1, promoting the survival of mucosal-associated invariant T cells MAIT and the expression of homeostatic gene signatures, affecting MAIT cell development and function. Cholic acid 7-sulfate is mainly used in the research of diabetes and MAIT cell-related immune regulation .
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