Search Result
Results for "
Insulin Receptor Agonist
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P3375
-
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IBI-362; LY-3305677; OXM-3
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GCGR
GLP Receptor
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Metabolic Disease
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Mazdutide (IBI-362; LY-3305677) is a long-acting synthetic oxyntomodulin analog. Mazdutide is also a co-agonist of glucagon-like peptide (GLP-1R) and glucagon receptor (GCGR). Mazdutide binds human and mouse GCGR (Ki: 17.7 nM and 15.9 nM, respectively) and GLP-1R (Ki: 28.6 nM and 25.1 nM, respectively) and stimulates insulin secretion from mouse islets (EC50: 5.2 nM). Mazdutide is used in studies of obesity and type 2 diabetes (T2D) .
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- HY-14734
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RC-1291; ONO-7643
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GHSR
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Endocrinology
Cancer
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Anamorelin (RC-1291) is an orally active Ghrelin receptor agonist with an EC50 of 0.74 nM. Anamorelin can promote appetite, increase body weight, and stimulate the secretion of growth hormone and insulin-like growth factor-1. Anamorelin can be used in the research of anorexia and cancer cachexia .
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- HY-W040127
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Insulin Receptor
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Metabolic Disease
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Peonidin 3-O-glucoside chloride is an agonist of the free fatty acid receptor FFAR1 and Glucokinase. Peonidin 3-O-glucoside chloride enhances insulin secretion of pancreatic beta cells and increases glucose uptake by liver cells. Peonidin 3-O-glucoside chloride activates FFAR1, promotes the phosphorylation of related proteins in the insulin secretion pathway, and increases the expression of FFAR1. In liver cells, Peonidin 3-O-glucoside chloride activates GK and regulates proteins associated with carbohydrate metabolism. Peonidin 3-O-glucoside chloride can be used in diabetes research .
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- HY-15589
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Free Fatty Acid Receptor
Potassium Channel
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
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GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities .
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- HY-P11274A
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Amycretin sodium; NN 9487 sodium
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Amylin Receptor
Insulin Receptor
GCGR
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Metabolic Disease
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Zenagamtide (Amycretin; NN 9487) sodium is an orally active, blood-brain barrier permeable triple agonist that targets GLP-1, amylin (Amylin Receptor) and calcitonin receptor (Calcitonin Receptor). Zenagamtide sodium is a single peptide consisting of 68 amino acids that can target brain regions regulating food intake, significantly suppress appetite and reduce energy intake. Therefore, Zenagamtide sodium improves body weight, waist circumference, glycated hemoglobin and lipid profile, and also alleviates the histological features of metabolic dysfunction-associated steatotic liver disease (MASLD) and enhances insulin sensitivity. Zenagamtide sodium may cause transient increases in heart rate and fluctuations in serum calcium levels, but it is an important compound for the study of overweight, obesity, insulin resistance and related metabolic diseases .
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- HY-160734
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GSBR-1290
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GLP Receptor
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Metabolic Disease
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Aleniglipron (GSBR-1290) is an orally active glucagon-like peptide-1 receptor (GLP-1R) agonist, with an EC50 value of less than 0.1 nM in HDB cell lines in cAMP stimulation assays. Aleniglipron selectively activates the Gαs-cAMP signaling pathway of GLP-1R without β-arrestin recruitment. Aleniglipron induces insulin release, promotes glucose clearance, reduces food intake and decreases body weight. Aleniglipron is applicable to research related to type 2 diabetes and obesity .
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- HY-14229
-
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CCDC
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G protein-coupled Bile Acid Receptor 1
Calcium Channel
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Metabolic Disease
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TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca 2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity .
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- HY-175701
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RO7795081; RG6652
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Arrestin
GLP Receptor
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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 recruitment of β-arrestin and the internalization of GLP-1R. CT-996 suppresses postprandial blood glucose in mice expressing human GLP-1 receptors and enhances glucose-stimulated insulin secretion (GSIS) in obese monkeys during intravenous glucose challenge. CT-996 can be used for the research of type 2 diabetes (T2D) and obesity .
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- HY-P10959
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LY3532226
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Insulin Receptor
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Metabolic Disease
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Macupatide is a glucose-dependent insulinotropic polypeptide (GIP) receptor agonist. Macupatide improves insulin secretion responses and insulin sensitivity.Macupatide can be used for the research of type 2 diabetes .
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- HY-14734A
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RC-1291 hydrochloride; ONO-7643 hydrochloride
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GHSR
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Endocrinology
Cancer
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Anamorelin (RC-1291) hydrochloride is an orally active Ghrelin receptor agonist with an EC50 of 0.74 nM. Anamorelin hydrochloride can promote appetite, increase body weight, and stimulate the secretion of growth hormone and insulin-like growth factor-1. Anamorelin hydrochloride can be used in the research of anorexia and cancer cachexia .
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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-P99665
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LY-3209590
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Insulin Receptor
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Metabolic Disease
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Insulin efsitora alfa (LY-3209590) is a selective agonist of insulin receptor (IR). Insulin efsitora alfa is a fusion protein composed of human IR agonists fused with the crystallizable (Fc) domain of human immunoglobulin G2 (IgG2) fragment, with a molecular weight of 64.1 kDa. Insulin efsitora alfa is well tolerated and has potential applications in diabetes .
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- HY-112606
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RXFP Receptor
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Others
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ML-290 is a first-in-class and potent relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes, with an EC50 of 94 nM . ML290 is a biased allosteric agonist at the relaxin receptor RXFP1.
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- HY-P11274
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Amycretin; NN 9487
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Amylin Receptor
GCGR
Insulin Receptor
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Metabolic Disease
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Zenagamtide (Amycretin; NN 9487) is an orally active, blood-brain barrier permeable triple agonist that targets GLP-1, amylin (Amylin Receptor) and calcitonin receptor (Calcitonin Receptor). Zenagamtide is a single peptide consisting of 68 amino acids that can target brain regions regulating food intake, significantly suppress appetite and reduce energy intake. Therefore, Zenagamtide improves body weight, waist circumference, glycated hemoglobin and lipid profile, and also alleviates the histological features of metabolic dysfunction-associated steatotic liver disease (MASLD) and enhances insulin sensitivity. Zenagamtide may cause transient increases in heart rate and fluctuations in serum calcium levels, but it is an important compound for the study of overweight, obesity, insulin resistance and related metabolic diseases .
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- HY-134353B
-
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Adenosine 5'-β-thiodiphosphate trilithium
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P2Y Receptor
NF-κB
Interleukin Related
Caspase
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Neurological Disease
Inflammation/Immunology
Cancer
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ADP-β-S (Adenosine 5'-(β-thiodiphosphate)) trilithium is a non-hydrolyzable ADP analog and a P2Y12 receptor agonist. ADP-β-S trilithium activates the P2Y12 receptor in microglia, thereby triggering downstream inflammatory signaling pathways. ADP-β-S trilithium activates P2Y purinergic receptors in rat pancreatic β cells and enhances glucose-induced insulin secretion. ADP-β-S trilithium can be used in the research of diseases such as inflammation and diabetes .
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- HY-P3375A
-
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IBI-362 TFA; LY-3305677 TFA; OXM-3 TFA
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GCGR
GLP Receptor
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Metabolic Disease
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Mazdutide (IBI-362; LY-3305677) TFA is a long-acting synthetic oxyntomodulin analog. Mazdutide is also a co-agonist of glucagon-like peptide (GLP-1R) and glucagon receptor (GCGR). Mazdutide TFA binds human and mouse GCGR (Ki: 17.7 nM and 15.9 nM, respectively) and GLP-1R (Ki: 28.6 nM and 25.1 nM, respectively) and stimulates insulin secretion from mouse islets (EC50: 5.2 nM). Mazdutide TFA is used in studies of obesity and type 2 diabetes (T2D) .
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- HY-10199A
-
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MK-677 free base; MK-0677 free base
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GHSR
Insulin Receptor
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Neurological Disease
Metabolic Disease
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Ibutamoren (MK-677 free base; MK-0677 free base) is an orally active non-peptide growth hormone secretagogue receptor agonist. Ibutamoren activates signal cascades by mimicking endogenous ligands, triggers pulsatile release of growth hormone from the pituitary gland, and increases serum levels of IGF-1 and insulin-like growth factor-binding protein 3. Ibutamoren not only increases the frequency of growth hormone pulses in male individuals, but also promotes elevated bone formation markers in female individuals with postmenopausal osteoporosis. The combination of Ibutamoren with Alendronate sodium hydrate (HY-11101) significantly increases bone mineral density at the femoral neck. However, Ibutamoren may cause mild, reversible adverse reactions such as increased appetite, fluid retention, and elevated fasting blood glucose. Ibutamoren has been widely used in studies related to idiopathic growth hormone deficiency, sarcopenia, Alzheimer's disease, and osteoporosis .
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- HY-107586
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DAQ B1; L-783281; Dimethylasterriquinone
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Insulin Receptor
Akt
NO Synthase
NADPH Oxidase
JAK
STAT
FOXO
DNA/RNA Synthesis
ERK
Flavivirus
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Cardiovascular Disease
Infection
Metabolic Disease
Inflammation/Immunology
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Demethylasterriquinone B1 (DAQ B1; L-783281) is an orally active insulin receptor (insulin receptor) agonist and AKT activator. By activating AKT, Demethylasterriquinone B1 upregulates the expression and activity of eNOS to increase NO production, while downregulating the expression of the NADPH oxidase subunit p22phox to reduce oxidative stress and improve vascular endothelial dysfunction in hypertensive rats. Demethylasterriquinone B1 combind with an AKT inhibitor targets the insulin signaling pathway to activate two antiviral pathways, RNA interference and JAK/STAT, in mosquitoes, thereby reducing Zika virus infection .
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- HY-19995
-
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GSK 137647
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Free Fatty Acid Receptor
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Metabolic Disease
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GSK137647A (GSK 137647) is a potent, selective free fatty acid receptor 4 (FFA4) agonist with pEC50 values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC50 values < 4.5 for all three species for FFA1, FFA2, and FFA3, respectively. GSK137647A has anti-inflammatory activity. GSK137647A induces insulin secretion and inhibits epithelial ion transport, GSK137647A is related to regulation of glucose homeostasis and anti-inflammatory response .
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- HY-U00425
-
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Ligands for Target Protein for PROTAC
Estrogen Receptor/ERR
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Metabolic Disease
Cancer
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PROTAC ERRα ligand 1 is a PROTAC target protein ligand. PROTAC ERRα ligand 1 is an orally active ERRα inverse agonist with IC50 values of 0.6 μM for ERRα. PROTAC ERRα ligand 1 shows no significant activity against a panel of other nuclear receptors, including ERα c, ERRγ, ERβ, PPARα, PPARγ, PPARδ, and RXRα. PROTAC ERRα ligand 1 can provide enhanced insulin sensitivity in vivo. PROTAC ERRα ligand 1 can be used for metabolic diseases research, such as type 2 diabetes and obesity .
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- HY-14234
-
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Glucocorticoid Receptor
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Metabolic Disease
Inflammation/Immunology
Endocrinology
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Glucocorticoid receptor agonist is a Glucocorticoid receptor agonist that acts on Glucocorticoid receptor (GR), progesterone receptor (PR) and mineralocorticoid receptor (MR) with the IC50 values of 2.1 , 1200 and 210 nM, respectively. Glucocorticoid receptor agonist has steroid-like anti-inflammatory properties and may be used to improve metabolism and reduce increased levels of body fat and serum insulin .
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- HY-116819
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GCGR
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Neurological Disease
Metabolic Disease
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VU0453379 is a blood-brain barrier permeable GLP-1R positive allosteric modulator (PAM) with an EC50 value of 1.3 μM. VU0453379 potentiates the actions of endogenous GLP-1 and synthetic peptide agonists, and promotes GLP-1 receptor internalization. VU0453379 stimulates insulin secretion from primary mouse islets. VU0453379 enhances the function of endogenous GLP-1R and reverses catalepsy in animal models. VU0453379 is useful for research on Parkinson's disease and type 2 diabetes .
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- HY-N0910
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- HY-P1072
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CGRP Receptor
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Cardiovascular Disease
Metabolic Disease
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PHM-27 (human) is a human prepro-vasoactive intestinal polypeptide (27 amino acid). PHM-27 (human) is a potent the human calcitonin receptor agonist with an EC50 of 11 nM. PHM-27 (human) efficiently enhances glucose-induced insulin secretion from beta cells by an autocrine mechanism .
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- HY-P0014B
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GLP Receptor
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Metabolic Disease
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Liraglutide (TFA) is an agonist of glucagon-like peptide 1 receptor (GLP-1). Liraglutide (TFA) can activate GLP-1, leading to the release of insulin in the presence of increased glucose concentration. Liraglutide (TFA) also reduces glucagon secretion in a glucose-dependent manner. Liraglutide (TFA) can be studied in research on type 2 diabetes .
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- HY-14363
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Free Fatty Acid Receptor
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Metabolic Disease
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TUG-424 is a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 of 32 nM. TUG-424 significantly increases glucose-stimulated insulin secretion at 100 nM. TUG-424 may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity . TUG-424 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-106103
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MK-678; L-363586
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Somatostatin Receptor
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Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Seglitide (MK-678) is an orally active, selective SSTR2 agonist and somatostatin analog. Seglitide also acts as a competitive Somatostatin receptor antagonist, with pA2 values of 6.50, 6.24 and 6.09 against SS14, SS25 and SS28, respectively. Seglitide produces only weak, transient inhibition of myocardial contractility in isolated right atria of guinea pigs. Seglitide inhibits glucagon secretion and reduces circulating insulin levels. Seglitide causes a sustained, reversible reduction in elevated systolic blood pressure in streptozotocin (HY-13753)-induced diabetic rats, but exerts no effect on spontaneously hypertensive rats. Seglitide induces membrane hyperpolarization and inhibits electrical excitability. Seglitide induces concentration-dependent contraction and significant desensitization in isolated distal colon of rats. Seglitide can be used in research related to hypertension complicated with insulin-dependent diabetes mellitus .
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- HY-P3584A
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(Pro3) Gastric Inhibitory Peptide, human TFA
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Insulin Receptor
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Metabolic Disease
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(Pro3) GIP, human TFA is an efficacious, stable and specific human GIP receptor (hGIPR) full agonist. (Pro3) GIP, human TFA has high binding affinity for human GIPR with Ki/ Kd value of 0.90 nM. (Pro3) GIP, human TFA human can be used for the research of obesity-related diabetes .
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- HY-P10959A
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LY3532226 acetate
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Insulin Receptor
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Metabolic Disease
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Macupatide acetate is a glucose-dependent insulinotropic polypeptide (GIP) receptor agonist. Macupatide acetate improves insulin secretion responses and insulin sensitivity.Macupatide acetate can be used for the research of type 2 diabetes .
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- HY-P4685
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Angiotensin Receptor
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Metabolic Disease
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(Sar1,Ile4,8)-Angiotensin II is a functionally selective angiotensin II type 1 receptor (AT1R) agonist. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated insulin receptor (IR) signaling and glycogen synthesis. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated phosphorylation of Akt and GSK3α/β .
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- HY-P2541A
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Insulin Receptor
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Metabolic Disease
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GIP (1-30) amide, porcine TFA is a full glucose-dependent insulinotropic polypeptide (GIP) receptor agonist with high affinity equal to native GIP(1-42) . GIP (1-30) amide, porcine is a weak inhibitor of gastric acid secretion and potent stimulator of insulin.
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- HY-P10413
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Androgen Receptor
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Metabolic Disease
Endocrinology
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SHBG 141-161 is a GPRC6A receptor agonist. SHBG 141-161 mimics the action of GPRC6A endogenous agonist uncarboxylated osteocalcin by binding to GPRC6A and promoting downstream signaling to increase testosterone and insulin secretion. SHBG 141-161 also reduces the affinity of GPRC6A to GDP protein by binding to the outer cell domain of GPRC6A thus affecting the dynamics of signal transduction. SHBG 141-161 can be used to study GPRC6A in energy metabolism and endocrine regulation .
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- HY-N2452
-
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GLP Receptor
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Cardiovascular Disease
Infection
Metabolic Disease
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Cochinchinenin C is a GLP-1R agonist that binds to the extracellular domain of the receptor via hydrophobic interactions and hydrogen bonds, and promotes glucose-dependent insulin secretion from pancreatic β-cells. Cochinchinenin C also increases intracellular cAMP and ATP levels. At low concentrations, Cochinchinenin C binds to human serum albumin, alters its microenvironment, and induces dominant static fluorescence quenching. Cochinchinenin C shows almost no cytotoxicity to pancreatic β-cells, and exerts a synergistic effect with Loureirin A (HY-N1505) when binding to human serum albumin. Cochinchinenin C has been widely used in studies of type 2 diabetes, Helicobacter pylori infection, thrombotic diseases, and other conditions .
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- HY-151959
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FXR
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
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FXR agonist 4 (compound 10a) is an agonist of farnesoid X receptor (FXR) with an EC50 value of 1.05 μM. FXR agonist 4 effectively improves hyperlipidemia, hepatic steatosis, insulin resistance and hepatic inflammation in DIO mice. FXR agonist 4 can be used for the research of non-alcoholic fatty liver disease (NAFLD) .
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- HY-144035
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GCGR
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Metabolic Disease
Inflammation/Immunology
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GLP-1R agonist 4 is a glucagon-like peptide-1 (GLP-1) receptor agonist. GLP-1 is an intestinal hypoglycemic hormone secreted by L-cells in the lower gastrointestinal tract. GLP-1R agonist 4 can be used for the research of type 2 diabetes mellitus, obesity, non-alcoholic steatohepatitis, insulin resistance and etc .
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- HY-P10965
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ZT002
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GLP Receptor
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Metabolic Disease
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Zovaglutide (ZT002) is a long-acting, selective GLP-1 receptor agonist. Zovaglutide enhances albumin binding capacity via dual fatty acid chain modification. Zovaglutide exerts metabolic effects through central and peripheral GLP-1 pathways, thereby promoting satiety, reducing caloric intake and enhancing glucose-dependent insulin secretion, with no activity against GIP or glucagon receptors. Zovaglutide can be used in research on type 2 diabetes or obesity .
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- HY-P10302
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GLP Receptor
Insulin Receptor
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Metabolic Disease
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GLP-1R/GIPR AgonIST-1 is a double-receptor agonist for GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulin releasing peptide). GLP-1R/GIPR agonist-1 lowers blood sugar by mimicking the action of endogenous hormones GLP-1 and GIP, enhancing insulin secretion while inhibiting glucagon secretion. GLP-1R/GIPR agonist-1 can be used in the study of metabolic diseases such as diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .
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- HY-P3255
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- HY-P11043
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GLP Receptor
Neuropeptide Y Receptor
Arrestin
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Metabolic Disease
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GEP44 is a peptide biased triple agonist targeting Glucagon-like peptide 1 receptor (GLP-1R), neuropeptide Y1 Receptor (Y1-R), and neuropeptide Y2 Receptor (Y2-R). GEP44 induces Y1-R antagonist-controlled, GLP-1R-dependent stimulation of insulin secretion in both rat and human pancreatic islets by counteracting effects of Y1-R and GLP-1R agonism. GEP44 promotes insulin-independent Y1-R-mediated glucose uptake in muscle tissue and significantly reduces food intake and body weight in diet-induced obese rat models. GEP44 can be used for obesity and type 2 diabetes mellitus research .
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- HY-P2090A
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Somatostatin Receptor
Adenylate Cyclase
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Cardiovascular Disease
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Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research .
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- HY-15589R
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Free Fatty Acid Receptor
Potassium Channel
Reference Standards
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
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GW9508 (Standard) is the analytical standard of GW9508. This product is intended for research and analytical applications. GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities .
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- HY-139709
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- HY-139710
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- HY-164040
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Somatostatin Receptor
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Metabolic Disease
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Zavolosotine (Compound 1) is an orally active agonist for somatostatin receptor type 5 (SST5) with EC50 <1 nM. Zavolosotine inhibits insulin and glucagon secretion, increases levels of glucagon in blood in rat model .
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- HY-14229R
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CCDC (Standard)
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G protein-coupled Bile Acid Receptor 1
Calcium Channel
Reference Standards
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Metabolic Disease
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TGR5 Receptor Agonist (Standard) is the analytical standard of TGR5 Receptor Agonist. This product is intended for research and analytical applications. TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity .
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- HY-P2541
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Insulin Receptor
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Metabolic Disease
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GIP (1-30) amide, porcine is a full glucose-dependent insulinotropic polypeptide (GIP) receptor agonist with high affinity equal to native GIP(1-42) . GIP (1-30) amide, porcine is a weak inhibitor of gastric acid secretion and potent stimulator of insulin.
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- HY-P10318
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GLP Receptor
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Endocrinology
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SHR-2042 is a selective agonist of the GLP-1 receptor.SHR-2042 improves glycemic control by activating the GLP-1 receptor, enhancing insulin secretion and inhibiting glucagon secretion. SHR-2042 combined with sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) promotes monomerization through the formation of micelles and improves oral absorption efficiency .
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- HY-176770
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GLP Receptor
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Metabolic Disease
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GLP-1R agonist 34 (Compound 1) is an orally active small molecule glucagon-like peptide-1 receptor (GLP-1R) agonist. GLP-1R agonist 34 promotes insulin secretion, inhibits glucagon release, and delays gastric emptying, thereby effectively lowering blood glucose levels. GLP-1R agonist 34 is promising for research of metabolic diseases, including type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .
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- HY-120287
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Somatostatin Receptor
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Endocrinology
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L-054522 is an agonist for somatostatin receptor subtype 2 with Kd of 0.01 nM. L-054522 inhibits growth hormone release from rat primary pituitary cell (IC50=0.05 nM) and glucagon and insulin release from isolated mouse pancreatic islet cell (IC50=0.05 nM and 12 nM) .
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- HY-134353A
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Adenosine 5'-(β-thiodiphosphate) trisodium
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Interleukin Related
P2Y Receptor
NF-κB
Caspase
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Neurological Disease
Inflammation/Immunology
Cancer
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ADP-β-S (Adenosine 5'-(β-thiodiphosphate)) trilithium is a non-hydrolyzable ADP analog and a P2Y12 receptor agonist. ADP-β-S trilithium activates the P2Y12 receptor in microglia, thereby triggering downstream inflammatory signaling pathways. ADP-β-S trilithium activates P2Y purinergic receptors in rat pancreatic β cells and enhances glucose-induced insulin secretion. ADP-β-S trilithium can be used in the research of diseases such as inflammation and diabetes .
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- HY-106863
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Adrenergic Receptor
|
Metabolic Disease
|
|
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 .
|
-
- HY-120493A
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
AM-6226 is a potent and orally active G protein coupled receptor 40 (GPR40) full agonist with an EC50 of 0.12 μM. AM-6226 can activate the GPR40 receptors on pancreatic β cells and enteroendocrine L cells, promote insulin secretion in a glucose-dependent manner and also increase the release of incretin hormones (GLP-1, GIP), thereby avoiding the risk of hypoglycemia. AM-6226 can be used for the research of metabolic disease, such as diabetes .
|
-
- HY-108020
-
|
|
Free Fatty Acid Receptor
|
Endocrinology
|
|
LY2881835 is a potent and selective agonist of G protein-coupled receptor 40 (GPR40). LY2881835 has efficacious and durable dose-dependent reductions in glucose levels along with significant increases in insulin and GLP-1 secretion. LY2881835 has the potential for the research of type 2 diabetes mellitus . LY2881835 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-171850
-
|
|
GLP Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
GLP-1R modulator-1 (Compound 384) is an orally active, potent selective glucagon-like peptide-1 receptor (GLP-1R) agonist. GLP-1R modulator-1 activates G-protein coupled signaling, elevates intracellular cAMP levels, promotes insulin secretion, delays gastric emptying and suppresses appetite. GLP-1R modulator-1 is promising for research of type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .
|
-
- HY-169066
-
|
|
Insulin Receptor
|
Metabolic Disease
|
INSR agonist 1 is an insulin receptor (INSR) agonist. INSR agonist 1 can increase INSR pY1355/1361 levels and works synergistically with insulin .
|
-
- HY-118141
-
|
|
Adrenergic Receptor
|
Metabolic Disease
|
|
BMS-194449 is a beta 3 receptor agonist with the Ki value of 160 nM. BMS-194449 can be used for study of obesity and non-insulin dependent diabetes .
|
-
- HY-162136
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
GPR40 agonist 7 (Compound 1) is an orally active G protein-coupled receptor 40 (GPR40) agonist. GPR40 agonist 7 can significantly increase insulin and GLP-1 secretion, and has a hypoglycemic effect in vivo with an ED50 of 0.58 mg/kg
|
-
- HY-109692
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
GPR120 Agonist 5 (compound 12) is an agonist targeting GPR120 (EC50=1.2 μM). GPR120 Agonist 5 promotes the release of glucagon-like 1 (GLP-1) by binding to the GPR120 receptor, which in turn binds to its receptors on pancreatic beta cells, increasing insulin secretion and thereby lowering blood sugar levels. GPR120 Agonist 5 also helps reduce chronic low-grade inflammation, which plays an important role in the pathogenesis of obesity, insulin resistance, and type 2 diabetes. GPR120 Agonist 5 can be used to investigate the mechanism of action of GPR120 in metabolic and inflammatory diseases .
|
-
- HY-101637
-
|
JT 501
|
PPAR
|
Metabolic Disease
|
|
Reglitazar is an agonist for peroxisome proliferator-activated receptor α and β (PPAR α and PPAR β), which enhances insulin sensitivity, lowers blood glucose and regulates blood lipid levels .
|
-
- HY-108664
-
|
|
P2Y Receptor
|
Metabolic Disease
|
|
MRS2957 is a P2Y6 receptor agonist that activates AMPK in pancreatic β-cells, promoting insulin secretion and reducing apoptosis, thereby holding potential as a therapeutic target for type 2 diabetes.
|
-
- HY-106181A
-
|
R-106056 hydrochloride
|
PPAR
|
Metabolic Disease
|
|
Rivoglitazone hydrochloride (R-106056 hydrochloride) is a peroxisome proliferator-activated receptor-γ (PPAR-γ) agonist. Rivoglitazone hydrochloride (R-106056 hydrochloride) exerts its anti-diabetic effect by activating PPARγ to regulate the expression of a large number of genes related to lipid and glucose metabolism. Rivoglitazone hydrochloride (R-106056 hydrochloride) can be used to study insulin secretion and insulin resistance in animal models of diabetes .
|
-
- HY-14734B
-
|
RC-1291 Fumarate; ONO-7643 Fumarate
|
GHSR
|
Endocrinology
Cancer
|
|
Anamorelin (RC-1291) Fumarate is an orally active Ghrelin receptor agonist with an EC50 of 0.74 nM. Anamorelin Fumarate can promote appetite, increase body weight, and stimulate the secretion of growth hormone and insulin-like growth factor-1. Anamorelin Fumarate can be used in the research of anorexia and cancer cachexia .
|
-
- HY-129707
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium inhibits specific [ 3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents .
|
-
- HY-19310
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
AMP-579 is an adenosine receptor agonist that primarily targets adenosine A1 and A2A receptors (with Ki values of 1.7 and 4.5 nM for the A1 receptor in rat brain and adipocytes, and a Ki value of 56 nM for the A2A receptor in rat brain). AMP-579 inhibits lipolysis, restores insulin-dependent glucose transport, and reduces heart rate through the activation of A1 receptors, while it induces vasodilation, particularly in coronary arteries, through the activation of A2A receptors (with an IC50 of 0.3 μM in porcine coronary arterial rings). AMP 579 shows potential for application in cardioprotection and the treatment of acute myocardial infarction .
|
-
- HY-14734R
-
|
RC-1291 (Standard); ONO-7643 (Standard)
|
Reference Standards
GHSR
|
Endocrinology
Cancer
|
|
Anamorelin (Standard) (RC-1291 (Standard)) is the analytical standard of Anamorelin (HY-14734). This product is intended for research and analytical applications. Anamorelin (RC-1291) is an orally active Ghrelin receptor agonist with an EC50 of 0.74 nM. Anamorelin can promote appetite, increase body weight, and stimulate the secretion of growth hormone and insulin-like growth factor-1. Anamorelin can be used in the research of anorexia and cancer cachexia .
|
-
- HY-P2090
-
|
|
Somatostatin Receptor
Adenylate Cyclase
|
Cardiovascular Disease
|
|
Angiopeptin, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin has the potential for coronary atherosclerosis research .
|
-
- HY-12976
-
|
|
G Protein-coupled Receptor Kinase (GRK)
|
Metabolic Disease
|
|
DS-1558 is an orally active small molecule G protein-coupled receptor 40 agonist. DS-1558 not only increases the glucose-stimulated insulin secretion by glucagon like peptide-1 (GLP-1) but also potentiated the maximum insulinogenic effects of GLP-1 after an intravenous glucose injection in normal Sprague Dawley rats. DS-1558 is promising for research of type 2 diabetes .
|
-
- HY-P1128
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
Galanin (swine), a neuropeptide, consists of 29 amino acids and contains a C-terminal amidated glycine. Galanin (swine) inhibits basal and stimulated insulin secretion both in vivo and in vitro under a variety of experimental conditions. Galanin (swine) is a galanin receptor agonist with pKis of 9.63, 9.49, 9.02, 8.98, 8.01 and 8.14 at human GAL1, rat GAL1, human GAL2, rat GAL2, human GAL3 and rat GAL3 respectively .
|
-
- HY-P1128A
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
Galanin (swine) TFA, a neuropeptide, consists of 29 amino acids and contains a C-terminal amidated glycine. Galanin (swine) inhibits basal and stimulated insulin secretion both in vivo and in vitro under a variety of experimental conditions. Galanin (swine) TFA is a galanin receptor agonist with pKis of 9.63, 9.49, 9.02, 8.98, 8.01 and 8.14 at human GAL1, rat GAL1, human GAL2, rat GAL2, human GAL3 and rat GAL3 respectively .
|
-
- HY-P0165B
-
|
ITM077 acetate; R1583 acetate; BIM51077 acetate
|
GLP Receptor
|
Metabolic Disease
|
|
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 .
|
-
- HY-113513
-
|
|
Others
|
Cancer
|
|
5(S)-HEPE is an active metabolite of eicosapentaenoic acid. It is formed from EPA by 5-lipoxygenase (5-LO). 5(S)-HEPE is an agonist of G protein-coupled receptor 119 (GPR119). It increases cAMP accumulation in CHO-K1 cells expressing human GPR119 when used at a concentration of 10 μM. 5(S)-HEPE increases glucose-induced insulin secretion from MING6 insulinoma pancreatic islets and glucagon-like peptide 1 (GLP-1) secretion from HuTu 80 adenocarcinoma cells when used at a concentration of 10 μM. Serum levels of 5(S)-HEPE are elevated in patients with hyperlipidemia.
|
-
- HY-P11075
-
|
|
Neurokinin Receptor
|
Metabolic Disease
|
|
[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) (ID 305) is a selective NK2R agonist with an EC50 of 3.7 nM for hNK2R. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) significantly inhibits weight loss in diet-induced obese (DIO) mice model and improves Loperamide (HY-156131)-induced dysfunctional voiding in wild-type mice. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) can be used for neurokinin receptor mediated disorders, such as obesity, insulin resistance and type 2 diabetes research .
|
-
- HY-180210
-
|
|
GHSR
GHR
IGF-1R
|
Inflammation/Immunology
Cancer
|
|
Ghrelin receptor full agonist-3 (Compound 22) is a selective, potent and orally active ghrelin receptor full agonist with an EC50 of 1.8 nM. Ghrelin receptor full agonist-3 can stimulate pulsatile secretion of growth hormone (GH), significantly increasing the frequency and duration of GH secretion, thereby inducing a sustained increase in insulin-like growth factor-1 (IGF-1) levels. Ghrelin receptor full agonist-3 can be used for the researches of cancer and chronic obstructive pulmonary disease .
|
-
- HY-P11610
-
|
|
Amylin Receptor
CGRP Receptor
|
Metabolic Disease
|
|
KBP-089 is a dual Amylin and Calcitonin Receptor agonist. KBP-089 reduces body weight, decreases adipose tissue mass and improves glucose tolerance in obese rats. KBP-089 also eliminates lipid accumulation in the liver and muscle, and ameliorates glycemic homeostasis and insulin sensitivity. KBP-089 is applicable to the research of diseases such as obesity and type 2 diabetes .
|
-
- HY-19002
-
|
|
Adrenergic Receptor
|
Metabolic Disease
|
|
BRL-26830A is a β-adrenergic receptor agonist. BRL-26830A reduces body weight and increases metabolic rate in obese mouse models. BRL-26830A stimulates insulin release and significantly reduces blood glucose levels in ICR mouse models. BRL-26830A can be used to study endocrine and metabolic diseases such as obesity and diabetes .
|
-
- HY-P11584
-
|
|
Amylin Receptor
CGRP Receptor
|
Metabolic Disease
|
|
KBP-066A is a long-acting dual amylin and calcitonin receptor agonist. KBP-066A can activate the CTR and AMY-R potently, with no off-target activity. KBP-066A reduces fasting blood glucose levels, fasting insulin levels, and body weight in diabetic rat models. KBP-066A can be used for the research of type 2 diabetes mellitus, obesity .
|
-
- HY-P11629
-
|
|
Amylin Receptor
CGRP Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
KBP-336 is a dual amylin and calcitonin receptor agonist (DACRA). KBP-336 exhibits antidiabetic and insulin-sensitizing properties, improves glucose levels, spatial learning, and memory in diabetic rats, and reduces blood glucose. KBP-336 also alleviates pain-like symptoms in osteoarthritis rats. KBP-336 also promotes weight and fat reduction. KBP-336 is useful for research on diabetes, obesity, and arthritis .
|
-
- HY-120493
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
(rel)-AM-6226 is the relative stereoisomer of AM-6226 (HY-120493A). AM-6226 is a potent, orally active full agonist of G protein-coupled receptor 40 (GPR40) with an EC50 value of 0.12 μM. AM-6226 activates GPR40 receptors on pancreatic β-cells and enteroendocrine L-cells, promotes insulin secretion in a glucose-dependent manner, and increases the release of incretin hormones (GLP-1, GIP), thus avoiding the risk of hypoglycemia. AM-6226 can be used in the research of metabolic diseases such as diabetes .
|
-
- HY-P992108
-
|
RELAX10
|
RXFP Receptor
Akt
NO Synthase
VEGFR
|
Cardiovascular Disease
|
|
Efadirelaxin alfa (RELAX10) is a highly selective agonist of relaxin/insulin-like family peptide receptor RXFP1. After subcutaneous administration in animal experiments, Efadirelaxin alfa exhibits a significantly prolonged terminal half-life (7 days in mice, 3.75 days in rats), and shows no activity against related receptors such as RXFP2 and RXFP3. Efadirelaxin alfa has significant anti-cardiac hypertrophy and anti-fibrotic effects. Efadirelaxin alfa effectively attenuates and reverses cardiac hypertrophy and collagen deposition by regulating the TGF-β1/Smad2 and AKT/eNOS signaling pathways. Efadirelaxin alfa improves cardiac systolic function without causing fluctuations in blood pressure or heart rate, demonstrating favorable safety. Efadirelaxin alfa is currently mainly used in studies related to heart failure .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3375
-
|
IBI-362; LY-3305677; OXM-3
|
GCGR
GLP Receptor
|
Metabolic Disease
|
|
Mazdutide (IBI-362; LY-3305677) is a long-acting synthetic oxyntomodulin analog. Mazdutide is also a co-agonist of glucagon-like peptide (GLP-1R) and glucagon receptor (GCGR). Mazdutide binds human and mouse GCGR (Ki: 17.7 nM and 15.9 nM, respectively) and GLP-1R (Ki: 28.6 nM and 25.1 nM, respectively) and stimulates insulin secretion from mouse islets (EC50: 5.2 nM). Mazdutide is used in studies of obesity and type 2 diabetes (T2D) .
|
-
- HY-P11274A
-
|
Amycretin sodium; NN 9487 sodium
|
Amylin Receptor
Insulin Receptor
GCGR
|
Metabolic Disease
|
Zenagamtide (Amycretin; NN 9487) sodium is an orally active, blood-brain barrier permeable triple agonist that targets GLP-1, amylin (Amylin Receptor) and calcitonin receptor (Calcitonin Receptor). Zenagamtide sodium is a single peptide consisting of 68 amino acids that can target brain regions regulating food intake, significantly suppress appetite and reduce energy intake. Therefore, Zenagamtide sodium improves body weight, waist circumference, glycated hemoglobin and lipid profile, and also alleviates the histological features of metabolic dysfunction-associated steatotic liver disease (MASLD) and enhances insulin sensitivity. Zenagamtide sodium may cause transient increases in heart rate and fluctuations in serum calcium levels, but it is an important compound for the study of overweight, obesity, insulin resistance and related metabolic diseases .
|
-
- HY-P10959
-
|
LY3532226
|
Insulin Receptor
|
Metabolic Disease
|
|
Macupatide is a glucose-dependent insulinotropic polypeptide (GIP) receptor agonist. Macupatide improves insulin secretion responses and insulin sensitivity.Macupatide can be used for the research of type 2 diabetes .
|
-
- HY-P11274
-
|
Amycretin; NN 9487
|
Amylin Receptor
GCGR
Insulin Receptor
|
Metabolic Disease
|
Zenagamtide (Amycretin; NN 9487) is an orally active, blood-brain barrier permeable triple agonist that targets GLP-1, amylin (Amylin Receptor) and calcitonin receptor (Calcitonin Receptor). Zenagamtide is a single peptide consisting of 68 amino acids that can target brain regions regulating food intake, significantly suppress appetite and reduce energy intake. Therefore, Zenagamtide improves body weight, waist circumference, glycated hemoglobin and lipid profile, and also alleviates the histological features of metabolic dysfunction-associated steatotic liver disease (MASLD) and enhances insulin sensitivity. Zenagamtide may cause transient increases in heart rate and fluctuations in serum calcium levels, but it is an important compound for the study of overweight, obesity, insulin resistance and related metabolic diseases .
|
-
- HY-P3375A
-
|
IBI-362 TFA; LY-3305677 TFA; OXM-3 TFA
|
GCGR
GLP Receptor
|
Metabolic Disease
|
|
Mazdutide (IBI-362; LY-3305677) TFA is a long-acting synthetic oxyntomodulin analog. Mazdutide is also a co-agonist of glucagon-like peptide (GLP-1R) and glucagon receptor (GCGR). Mazdutide TFA binds human and mouse GCGR (Ki: 17.7 nM and 15.9 nM, respectively) and GLP-1R (Ki: 28.6 nM and 25.1 nM, respectively) and stimulates insulin secretion from mouse islets (EC50: 5.2 nM). Mazdutide TFA is used in studies of obesity and type 2 diabetes (T2D) .
|
-
- HY-P1072
-
|
|
CGRP Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
PHM-27 (human) is a human prepro-vasoactive intestinal polypeptide (27 amino acid). PHM-27 (human) is a potent the human calcitonin receptor agonist with an EC50 of 11 nM. PHM-27 (human) efficiently enhances glucose-induced insulin secretion from beta cells by an autocrine mechanism .
|
-
- HY-P0014B
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
Liraglutide (TFA) is an agonist of glucagon-like peptide 1 receptor (GLP-1). Liraglutide (TFA) can activate GLP-1, leading to the release of insulin in the presence of increased glucose concentration. Liraglutide (TFA) also reduces glucagon secretion in a glucose-dependent manner. Liraglutide (TFA) can be studied in research on type 2 diabetes .
|
-
- HY-106103
-
|
MK-678; L-363586
|
Somatostatin Receptor
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Seglitide (MK-678) is an orally active, selective SSTR2 agonist and somatostatin analog. Seglitide also acts as a competitive Somatostatin receptor antagonist, with pA2 values of 6.50, 6.24 and 6.09 against SS14, SS25 and SS28, respectively. Seglitide produces only weak, transient inhibition of myocardial contractility in isolated right atria of guinea pigs. Seglitide inhibits glucagon secretion and reduces circulating insulin levels. Seglitide causes a sustained, reversible reduction in elevated systolic blood pressure in streptozotocin (HY-13753)-induced diabetic rats, but exerts no effect on spontaneously hypertensive rats. Seglitide induces membrane hyperpolarization and inhibits electrical excitability. Seglitide induces concentration-dependent contraction and significant desensitization in isolated distal colon of rats. Seglitide can be used in research related to hypertension complicated with insulin-dependent diabetes mellitus .
|
-
- HY-P3584A
-
|
(Pro3) Gastric Inhibitory Peptide, human TFA
|
Insulin Receptor
|
Metabolic Disease
|
|
(Pro3) GIP, human TFA is an efficacious, stable and specific human GIP receptor (hGIPR) full agonist. (Pro3) GIP, human TFA has high binding affinity for human GIPR with Ki/ Kd value of 0.90 nM. (Pro3) GIP, human TFA human can be used for the research of obesity-related diabetes .
|
-
- HY-P10959A
-
|
LY3532226 acetate
|
Insulin Receptor
|
Metabolic Disease
|
|
Macupatide acetate is a glucose-dependent insulinotropic polypeptide (GIP) receptor agonist. Macupatide acetate improves insulin secretion responses and insulin sensitivity.Macupatide acetate can be used for the research of type 2 diabetes .
|
-
- HY-P4685
-
|
|
Angiotensin Receptor
|
Metabolic Disease
|
|
(Sar1,Ile4,8)-Angiotensin II is a functionally selective angiotensin II type 1 receptor (AT1R) agonist. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated insulin receptor (IR) signaling and glycogen synthesis. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated phosphorylation of Akt and GSK3α/β .
|
-
- HY-P2541A
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide, porcine TFA is a full glucose-dependent insulinotropic polypeptide (GIP) receptor agonist with high affinity equal to native GIP(1-42) . GIP (1-30) amide, porcine is a weak inhibitor of gastric acid secretion and potent stimulator of insulin.
|
-
- HY-P10413
-
|
|
Androgen Receptor
|
Metabolic Disease
Endocrinology
|
|
SHBG 141-161 is a GPRC6A receptor agonist. SHBG 141-161 mimics the action of GPRC6A endogenous agonist uncarboxylated osteocalcin by binding to GPRC6A and promoting downstream signaling to increase testosterone and insulin secretion. SHBG 141-161 also reduces the affinity of GPRC6A to GDP protein by binding to the outer cell domain of GPRC6A thus affecting the dynamics of signal transduction. SHBG 141-161 can be used to study GPRC6A in energy metabolism and endocrine regulation .
|
-
- HY-P10965
-
|
ZT002
|
GLP Receptor
|
Metabolic Disease
|
|
Zovaglutide (ZT002) is a long-acting, selective GLP-1 receptor agonist. Zovaglutide enhances albumin binding capacity via dual fatty acid chain modification. Zovaglutide exerts metabolic effects through central and peripheral GLP-1 pathways, thereby promoting satiety, reducing caloric intake and enhancing glucose-dependent insulin secretion, with no activity against GIP or glucagon receptors. Zovaglutide can be used in research on type 2 diabetes or obesity .
|
-
- HY-P10302
-
|
|
GLP Receptor
Insulin Receptor
|
Metabolic Disease
|
|
GLP-1R/GIPR AgonIST-1 is a double-receptor agonist for GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulin releasing peptide). GLP-1R/GIPR agonist-1 lowers blood sugar by mimicking the action of endogenous hormones GLP-1 and GIP, enhancing insulin secretion while inhibiting glucagon secretion. GLP-1R/GIPR agonist-1 can be used in the study of metabolic diseases such as diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .
|
-
- HY-P3255
-
-
- HY-P11043
-
|
|
GLP Receptor
Neuropeptide Y Receptor
Arrestin
|
Metabolic Disease
|
|
GEP44 is a peptide biased triple agonist targeting Glucagon-like peptide 1 receptor (GLP-1R), neuropeptide Y1 Receptor (Y1-R), and neuropeptide Y2 Receptor (Y2-R). GEP44 induces Y1-R antagonist-controlled, GLP-1R-dependent stimulation of insulin secretion in both rat and human pancreatic islets by counteracting effects of Y1-R and GLP-1R agonism. GEP44 promotes insulin-independent Y1-R-mediated glucose uptake in muscle tissue and significantly reduces food intake and body weight in diet-induced obese rat models. GEP44 can be used for obesity and type 2 diabetes mellitus research .
|
-
- HY-P2090A
-
|
|
Somatostatin Receptor
Adenylate Cyclase
|
Cardiovascular Disease
|
|
Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research .
|
-
- HY-P2541
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide, porcine is a full glucose-dependent insulinotropic polypeptide (GIP) receptor agonist with high affinity equal to native GIP(1-42) . GIP (1-30) amide, porcine is a weak inhibitor of gastric acid secretion and potent stimulator of insulin.
|
-
- HY-P10318
-
|
|
GLP Receptor
|
Endocrinology
|
|
SHR-2042 is a selective agonist of the GLP-1 receptor.SHR-2042 improves glycemic control by activating the GLP-1 receptor, enhancing insulin secretion and inhibiting glucagon secretion. SHR-2042 combined with sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) promotes monomerization through the formation of micelles and improves oral absorption efficiency .
|
-
- HY-P2090
-
|
|
Somatostatin Receptor
Adenylate Cyclase
|
Cardiovascular Disease
|
|
Angiopeptin, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin has the potential for coronary atherosclerosis research .
|
-
- HY-P1128
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
Galanin (swine), a neuropeptide, consists of 29 amino acids and contains a C-terminal amidated glycine. Galanin (swine) inhibits basal and stimulated insulin secretion both in vivo and in vitro under a variety of experimental conditions. Galanin (swine) is a galanin receptor agonist with pKis of 9.63, 9.49, 9.02, 8.98, 8.01 and 8.14 at human GAL1, rat GAL1, human GAL2, rat GAL2, human GAL3 and rat GAL3 respectively .
|
-
- HY-P1128A
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
Galanin (swine) TFA, a neuropeptide, consists of 29 amino acids and contains a C-terminal amidated glycine. Galanin (swine) inhibits basal and stimulated insulin secretion both in vivo and in vitro under a variety of experimental conditions. Galanin (swine) TFA is a galanin receptor agonist with pKis of 9.63, 9.49, 9.02, 8.98, 8.01 and 8.14 at human GAL1, rat GAL1, human GAL2, rat GAL2, human GAL3 and rat GAL3 respectively .
|
-
- HY-P0165B
-
|
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-P11075
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Neurokinin Receptor
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Metabolic Disease
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[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) (ID 305) is a selective NK2R agonist with an EC50 of 3.7 nM for hNK2R. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) significantly inhibits weight loss in diet-induced obese (DIO) mice model and improves Loperamide (HY-156131)-induced dysfunctional voiding in wild-type mice. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) can be used for neurokinin receptor mediated disorders, such as obesity, insulin resistance and type 2 diabetes research .
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- HY-P11610
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Amylin Receptor
CGRP Receptor
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Metabolic Disease
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KBP-089 is a dual Amylin and Calcitonin Receptor agonist. KBP-089 reduces body weight, decreases adipose tissue mass and improves glucose tolerance in obese rats. KBP-089 also eliminates lipid accumulation in the liver and muscle, and ameliorates glycemic homeostasis and insulin sensitivity. KBP-089 is applicable to the research of diseases such as obesity and type 2 diabetes .
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- HY-P11584
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Amylin Receptor
CGRP Receptor
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Metabolic Disease
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KBP-066A is a long-acting dual amylin and calcitonin receptor agonist. KBP-066A can activate the CTR and AMY-R potently, with no off-target activity. KBP-066A reduces fasting blood glucose levels, fasting insulin levels, and body weight in diabetic rat models. KBP-066A can be used for the research of type 2 diabetes mellitus, obesity .
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- HY-P11629
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Amylin Receptor
CGRP Receptor
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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KBP-336 is a dual amylin and calcitonin receptor agonist (DACRA). KBP-336 exhibits antidiabetic and insulin-sensitizing properties, improves glucose levels, spatial learning, and memory in diabetic rats, and reduces blood glucose. KBP-336 also alleviates pain-like symptoms in osteoarthritis rats. KBP-336 also promotes weight and fat reduction. KBP-336 is useful for research on diabetes, obesity, and arthritis .
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Target |
Research Area |
Image |
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- HY-P99665
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LY-3209590
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Insulin Receptor
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Metabolic Disease
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Insulin efsitora alfa (LY-3209590) is a selective agonist of insulin receptor (IR). Insulin efsitora alfa is a fusion protein composed of human IR agonists fused with the crystallizable (Fc) domain of human immunoglobulin G2 (IgG2) fragment, with a molecular weight of 64.1 kDa. Insulin efsitora alfa is well tolerated and has potential applications in diabetes .
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(5)
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- HY-P992108
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RELAX10
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RXFP Receptor
Akt
NO Synthase
VEGFR
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Cardiovascular Disease
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Efadirelaxin alfa (RELAX10) is a highly selective agonist of relaxin/insulin-like family peptide receptor RXFP1. After subcutaneous administration in animal experiments, Efadirelaxin alfa exhibits a significantly prolonged terminal half-life (7 days in mice, 3.75 days in rats), and shows no activity against related receptors such as RXFP2 and RXFP3. Efadirelaxin alfa has significant anti-cardiac hypertrophy and anti-fibrotic effects. Efadirelaxin alfa effectively attenuates and reverses cardiac hypertrophy and collagen deposition by regulating the TGF-β1/Smad2 and AKT/eNOS signaling pathways. Efadirelaxin alfa improves cardiac systolic function without causing fluctuations in blood pressure or heart rate, demonstrating favorable safety. Efadirelaxin alfa is currently mainly used in studies related to heart failure .
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(5)
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Product Name |
Category |
Target |
Chemical Structure |
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- HY-W040127
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- HY-N15721
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Trp-CA
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Triterpenes
Structural Classification
Terpenoids
Endogenous metabolite
Source Classification
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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-N0910
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- HY-N2452
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other families
Classification of Application Fields
Phenols
Polyphenols
Metabolic Disease
Plants
Disease Research Fields
Source Classification
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GLP Receptor
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Cochinchinenin C is a GLP-1R agonist that binds to the extracellular domain of the receptor via hydrophobic interactions and hydrogen bonds, and promotes glucose-dependent insulin secretion from pancreatic β-cells. Cochinchinenin C also increases intracellular cAMP and ATP levels. At low concentrations, Cochinchinenin C binds to human serum albumin, alters its microenvironment, and induces dominant static fluorescence quenching. Cochinchinenin C shows almost no cytotoxicity to pancreatic β-cells, and exerts a synergistic effect with Loureirin A (HY-N1505) when binding to human serum albumin. Cochinchinenin C has been widely used in studies of type 2 diabetes, Helicobacter pylori infection, thrombotic diseases, and other conditions .
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- HY-113513
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Microorganisms
Source Classification
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Others
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5(S)-HEPE is an active metabolite of eicosapentaenoic acid. It is formed from EPA by 5-lipoxygenase (5-LO). 5(S)-HEPE is an agonist of G protein-coupled receptor 119 (GPR119). It increases cAMP accumulation in CHO-K1 cells expressing human GPR119 when used at a concentration of 10 μM. 5(S)-HEPE increases glucose-induced insulin secretion from MING6 insulinoma pancreatic islets and glucagon-like peptide 1 (GLP-1) secretion from HuTu 80 adenocarcinoma cells when used at a concentration of 10 μM. Serum levels of 5(S)-HEPE are elevated in patients with hyperlipidemia.
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