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diabetic mouse models

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36

Inhibitors & Agonists

3

Peptides

3

Inhibitory Antibodies

2

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-111310
    ML351
    2 Publications Verification

    Lipoxygenase Neurological Disease Metabolic Disease
    ML351 is a potent and highly specific 15-LOX-1 inhibitor with an IC50 of 200 nM. ML351 shows excellent selectivity (>250-fold) versus the related isozymes, 5-LOX, platelet 12-LOX, 15-LOX-2, ovine COX-1, and human COX-2 . ML351 prevents dysglycemia and reduces β-cell oxidative stress in nonobese diabetic mouse model of T1D .
    ML351
  • HY-161834
    RG100204
    1 Publications Verification

    Pyroptosis Aquaporin NOD-like Receptor (NLR) p38 MAPK Infection Metabolic Disease Inflammation/Immunology
    RG100204 is a selective, orally available inhibitor of the aquaporin AQP9. RG100204 directly inhibits AQP9 channel function, preventing the transmembrane transport of water, glycerol, and H 2O 2. RG100204 reduces the activation of the NLRP3 inflammasome and p38 MAPK signaling pathways, thereby alleviating inflammation and pyroptosis. RG100204 reduces multi-organ dysfunction in a mouse sepsis model and shows glucose-regulating effects in diabetic db/db mice .
    RG100204
  • HY-P99116

    RG7716; RO-6867461

    VEGFR Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    Faricimab, an overall good safety and tolerability profile, is a bispecific antibody targeting Angiopoietin-2 (Ang-2) and vascular endothelial growth factor-A (VEGF-A). Faricimab prevents retinal vascular leakage, cell death and inflammation in retinal ischemia/reperfusion (I/R) injury and sCNV mouse models. Faricimab demonstrates statistically superior visual acuity gains versus Ranibizumab (HY-P9951). Faricimab can be used for retinal diseases, such as age-related macular degeneration (w-AMD), diabetic macular edema (DME) and macular edema following retinal vein occlusion (RVO) .
    Faricimab
  • HY-P2917

    GyK

    Nuclear Hormone Receptor 4A/NR4A Metabolic Disease Inflammation/Immunology
    Glycerol kinase, microorganism (GyK) acts as a NR4A1 inhibitor with enzymatic activity. It directly binds to and inhibits the transcription factor NR4A1, thereby negatively regulating hepatic gluconeogenesis and reducing blood glucose levels. Glycerol kinase, microorganism positively regulates UCP1 expression via partial dependence on the β-adrenergic receptor-cAMP-CREB pathway, promotes browning of white adipose tissue and thermogenesis, and further modulates intracellular fatty acid composition and energy metabolism. In diabetic mouse models, overexpression of Glycerol kinase effectively antagonizes NR4A1-induced hyperglycemia, demonstrating potential for improving glucose homeostasis. Glycerol kinase, microorganism can be used for studies on diabetes and obesity .
    Glycerol kinase, microorganism
  • HY-160186
    20-SOLA
    1 Publications Verification

    Cytochrome P450 Cardiovascular Disease Metabolic Disease Endocrinology
    20-SOLA is an orally active 20-HETE antagonist. 20-SOLA greatly ameliorates changes in blood pressure and renal injury associated with a Streptozotocin (STZ) (HY-13753)-diabetic mouse model. 20-SOLA facilitates the restoration of coronary collateral growth (CCG) after ischemic injury. 20-SOLA can be studied for research in cardiovascular diseases and diabetes .
    20-SOLA
  • HY-151500

    Amine N-methyltransferase Metabolic Disease
    JBSNF-00002 free base is an orally active small molecule inhibitor of the tricyclic nicotinamide N-methyltransferase (NNMT) with IC50 values for human, mouse and monkey sources of NNMT of 33, 210 and 190 nM respectively. JBSNF-00002 free base can reduce endogenous MNA levels in U2OS osteosarcoma cells, with its EC50 being 2.5 μM. JBSNF-00002 free base exhibits significant anti-obesity and anti-diabetic activities in the diet-induced obesity (DIO) model. JBSNF-00002 free base can be used for the study of metabolic diseases such as obesity, type 2 diabetes and non-alcoholic fatty liver disease .
    JBSNF-000028 free base
  • HY-164781
    KOTX1
    1 Publications Verification

    MBE1

    Aldehyde Dehydrogenase (ALDH) Metabolic Disease
    KOTX1 is an orally active and selective ALDH1A3 inhibitor. KOTX1 improves glucose tolerance, insulin secretion and blood sugar levels in diabetic mouse models .
    KOTX1
  • HY-W010649

    HSP Epigenetic Reader Domain ATP-binding cassette (ABC) transporters Bacterial Fungal Antibiotic Infection Metabolic Disease Inflammation/Immunology Cancer
    Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve β-cell function in a diabetic mouse model. Isoxazole and its derivatives exhibit broad biological activities (such as antimicrobial, antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, immunomodulatory, analgesic, anti-tuberculosis, and anti-diabetic effects). For example, the bicyclic Isoxazole can act as an HSP90 inhibitor, and the tricyclic Isoxazole is promising as a selective multidrug resistance protein (MRP1) inhibitor​ .
    Isoxazole
  • HY-151500B

    Amine N-methyltransferase Metabolic Disease
    JBSNF-00002 hydrochloride is an orally active small molecule inhibitor of the tricyclic nicotinamide N-methyltransferase (NNMT) with IC50 values for human, mouse and monkey sources of NNMT of 33, 210 and 190 nM respectively. JBSNF-00002 hydrochloride can reduce endogenous MNA levels in U2OS osteosarcoma cells, with its EC50 being 2.5 μM. JBSNF-00002 hydrochloride exhibits significant anti-obesity and anti-diabetic activities in the diet-induced obesity (DIO) model. JBSNF-00002 hydrochloride can be used for the study of metabolic diseases such as obesity, type 2 diabetes and non-alcoholic fatty liver disease .
    JBSNF-000028 hydrochloride
  • HY-121811

    Lanceolatin C

    Glycosidase Phosphatase Interleukin Related TNF Receptor COX Beclin1 GLUT FAK Akt mTOR p38 MAPK Keap1-Nrf2 Apoptosis Amyloid-β Tau Protein Autophagy Neurological Disease Inflammation/Immunology Cancer
    Pongamol is an orally active flavonoid with an IC50 of 75 μM and a Ki of 58 μM against PTPase-1B, and an IC50 of 103.5 μM against intestinal α-Glycosidase. Pongamol reduces the release of IL‑1β, TNF‑α, COX‑2 and iNOS in cells, reverses the nuclear translocation of NF‑κB, and upregulates the levels of Beclin 1 and LC3 Ⅱ/LC3 Ⅰ. Pongamol promotes glucose uptake by increasing the level of GLUT4 on the surface of skeletal muscle cells. Pongamol inhibits epithelial-mesenchymal transition by suppressing the FAK/Akt-mTOR signaling pathway. Pongamol inhibits neuronal cytotoxicity, suppresses cell apoptosis and extends the lifespan of Caenorhabditis elegans by activating the MAPKs/Nrf2 signaling pathway. Pongamol exerts hypoglycemic effects in diabetic mouse models. Pongamol alleviates oxidative stress, neuroinflammation, deposition and excessive phosphorylation of Tau Protein, and restores autophagy function in Alzheimer's disease mouse models by inhibiting the Akt/mTOR signaling pathway. Pongamol is applicable to research related to Alzheimer's disease, type 2 diabetes, non-small cell lung cancer and postprandial hyperglycemia .
    Pongamol
  • HY-P5396A

    Amino Acid Decarboxylase Others
    GAD65 (524-543) acetate is a biological active peptide with amino acids 524 to 543 fragment of glutamic acid decarboxylase 65 (GAD65). GAD65 (524-543) acetate is one of the first fragments of the islet antigen to induce proliferative T cell responses in the non-obese diabetic (NOD) mouse model of spontaneous autoimmune diabetes. GAD65 (524-543) acetate is a specific, possibly low affinity, stimulus for the spontaneously arising diabetogenic T cell clone BDC2.5. Immunization with GAD65 (524-543) acetate increases the susceptibility of the NOD mice to type 1 diabetes induced by the adoptive transfer of BDC2.5 T cells .
    GAD65 (524-543) acetate
  • HY-151500A

    Amine N-methyltransferase Metabolic Disease
    JBSNF-00002 TFA is an orally active small molecule inhibitor of the tricyclic nicotinamide N-methyltransferase (NNMT) with IC50 values for human, mouse and monkey sources of NNMT of 33, 210 and 190 nM respectively. JBSNF-00002 TFA can reduce endogenous MNA levels in U2OS osteosarcoma cells, with its EC50 being 2.5 μM. JBSNF-00002 TFA exhibits significant anti-obesity and anti-diabetic activities in the diet-induced obesity (DIO) model. JBSNF-00002 TFA can be used for the study of metabolic diseases such as obesity, type 2 diabetes and non-alcoholic fatty liver disease .
    JBSNF-000028 TFA
  • HY-178780

    GPR119 Metabolic Disease
    MKP10241 is an orally active GPR119 agonist. MKP10241 elevates cAMP levels in the GPR119 expressing cell line (EC50: 3.7 nM). MKP10241 reduces blood glucose levels and HbA1c in acute models and a chronic diabetic mouse model. MKP10241 also demonstrates excellent preclinical efficacy in acute as well as chronic rodent models of obesity, and MASH .
    MKP10241
  • HY-138007

    ROR PPAR LXR Metabolic Disease Inflammation/Immunology
    SR-1903 is an inverse agonist of RORγ and PPARγ (IC50 of ∼100 nM and 209 nM for RORγ and PPARγ, respectively) and a LXR agonist. SR-1903 exhibits anti-inflammatory and anti-diabetic efficacy in collagen-induced arthritis and diet-induced obesity mouse models .
    SR-1903
  • HY-151500C

    Amine N-methyltransferase Metabolic Disease
    JBSNF-00002 is an orally active small molecule inhibitor of the tricyclic nicotinamide N-methyltransferase (NNMT) with IC50 values for human, mouse and monkey sources of NNMT of 33, 210 and 190 nM respectively. JBSNF-00002 can reduce endogenous MNA levels in U2OS osteosarcoma cells, with its EC50 being 2.5 μM. JBSNF-00002 exhibits significant anti-obesity and anti-diabetic activities in the diet-induced obesity (DIO) model. JBSNF-00002 can be used for the study of metabolic diseases such as obesity, type 2 diabetes and non-alcoholic fatty liver disease .
    JBSNF-000028
  • HY-179578

    Enolase AMPK Autophagy Apoptosis mTOR Caspase Metabolic Disease Cancer
    SU212 is a podophyllotoxin-derived ENO1 inhibitor and AMPK activator. SU212 can selectively induce oxidative phosphorylation, reduce glycolysis activity and glucose uptake in tumor cells, and directly bind to ENO1 without affecting these pathways in normal cells. SU212 induces apoptosis and promotes ENO1 degradation via proteasomal and autophagic pathways without inhibiting the catalytic activity. SU212 leads to mitotic arrest and apoptosis in TNBC (triple-negative breast cancer) cells by activating AMPK, demonstrating potent anti-tumor activity in vitro. SU212 inhibits tumor growth and metastasis in syngeneic, xenograft, and diabetic mouse models, exhibiting an excellent safety profile. SU212 can be used in research on t TNBC, diabetes, and fatty liver disease .
    SU212
  • HY-100819

    CCR Metabolic Disease
    RO5234444 is an orally active CCR2 antagonist, with IC50s of 22nM for human CCR2 and 161 nM for mouse CCR2. RO5234444 alleviates glomerulosclerosis, reduces albuminuria, and significantly improves the glomerular filtration rate (GFR) in the uninephrectomized (1K) type 2 diabetic db/db mouse model. RO5234444 can be used for the study of type 2 diabetic nephropathy .
    RO5234444
  • HY-124483

    Arrestin Metabolic Disease
    W2476 is a regulator of thioredocin-interacting protein signaling pathway. W2476 promotes competitive binding of forkhead box O1 transcription factor (FOXO1). W2476 can ameliorate β-cell dysfunction and enhance insulin secretion in diabetic mouse model .
    W2476
  • HY-145549

    N-eicosanoyl-D-erythro-Sphingosylphosphorylcholine; SM(d18:1/20:0)

    Endogenous Metabolite Endocrinology
    C20 Sphingomyelin (d18:1/20:0) (N-eicosanoyl-D-erythro-Sphingosylphosphorylcholine; SM(d18:1/20:0)) is a naturally occurring sphingolipid. C20 Sphingomyelin (d18:1/20:0) levels are upregulated in the hippocampus of streptozotocin (HY-13753)-induced diabetic rats and in human plasma, positively correlating with insulin resistance in obese humans. C20 Sphingomyelin (d18:1/20:0) is also upregulated in the liver of a mouse model of Niemann-Pick C1 disease, a neurodegenerative cholesterol sphingolipid lysosomal storage disorder.
    C20 Sphingomyelin (d18:1/20:0)
  • HY-Z15823

    Dexverapamil

    Calcium Channel Potassium Channel Somatostatin Receptor Arrestin Apoptosis P-glycoprotein Metabolic Disease Inflammation/Immunology
    (R)-Verapamil (Dexverapamil) is an optically enantiomer of the oral-active Verapamil (HY-14275). (R)-Verapamil has a relatively low affinity for L-type calcium channels (Cav1.2) (IC50 > 300 μM), and its IC50 for sodium channels (sodium channel) is 3.19 μM. (R)-Verapamil exhibits SSTR2 agonistic activity, with an EC50 of 1.3 μM. (R)-Verapamil significantly downregulates the expression of TXNIP protein in diabetic mouse models and significantly inhibits β-cell apoptosis (apoptosis), effectively controlling blood sugar. (R)-Verapamil can be used as a PET tracer for the function of P-glycoprotein (P-gp) .
    (R)-Verapamil
  • HY-122120

    AJ‐9677

    Adrenergic Receptor Metabolic Disease
    Rafabegron (AJ-9677) is a specific beta3-adrenoceptor agonist. Rafabegron can reduce blood glucose, insulin, FFA, and triglyceride levels in diabetic and obese mouse models .
    Rafabegron
  • HY-125327

    SGLT Metabolic Disease
    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.
    YM-543
  • HY-170874

    PPAR Metabolic Disease
    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 .
    PPARγ modulator-2
  • HY-P991310

    LT3015; LT-3000

    LPL Receptor Neurological Disease Cancer
    Lpathomab (LT3015; LT-3000) is a human IgG1 monoclonal antibody (mAb) targeting LPA. Lpathomab reduces the release of IL-8 and IL-6 cytokines in SKOV3 cells and blocks LPA-triggered tumor cell migration. Lpathomab reduces neovascularization in Matrigel plug and CNV models. Lpathomab inhibits brain injury in the CCI mouse model. Lpathomab can be used in the study of brain injury, ovarian cancer, diabetic neuropathy, and spinal cord injury. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
    Lpathomab
  • HY-171793

    PPAR Metabolic Disease
    DN-108, a thiazolidinedione derivative, is an orally active peroxisome proliferator-activated receptor γ (PPARγ) agonist with antidiabetic effects. DN-108 improves hyperglycemia, hypertriglyceridemia and hyperinsulinemia in diabetic mouse models. DN-108 enhances tissue glucose uptake (e.g., increasing 2-deoxyglucose uptake in L6 muscle cells) and inhibits fatty acid synthase activity. DN-108 is promising for research of type 2 diabetes .
    DN-108
  • HY-126969

    PPAR Metabolic Disease
    C333H is a selective PPARγ modulator with insulin-sensitizing and hypoglycemic activities. C333H exhibits similar insulin-sensitizing effects to thiazolidinediones (TZDs) in diabetic mouse models without significantly increasing body weight or adipose tissue weight. C333H increases circulating high molecular weight adiponectin isoform levels in diabetic db/db mice, reduces serine phosphorylation of PPARγ 273 in brown adipose tissue, and selectively modulates the expression of specific PPARγ target genes in adipose tissue. Express. C333H exhibits weak recruitment of co-activators and weak dissociation of co-repressors in vitro. These properties suggest that C333H may be a potential inhibitor of type 2 diabetes .
    C333H
  • HY-159962

    Glutaminase Metabolic Disease
    TGase2-IN-1 (Compound 22) is an orally active inhibitor for TGase2 with an IC50 of 1.12 μM. TGase2-IN-1 inhibits TGase2 in human retinal microvascular endothelial cells with an IC50 of 0.07 μM. TGase2-IN-1 exhibits 74.6% oral bioavailability. TGase2-IN-1 inhibits retinal vascular leakage in mouse Streptozotocin (HY-13753)-induced diabetic model .
    TGase2-IN-1
  • HY-133559

    PPAR Metabolic Disease
    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 .
    VSP-77
  • HY-162578

    PPAR Metabolic Disease
    PPARα/γ agonist 4 (Compound (S)-7) is an orally active dual potent agonist of PPARα and PPARγ, with EC50 values of 0.061 μM and 1.42 μM respectively. PPARα/γ agonist 4 acts through an insulin-independent mechanism and exhibits mitochondrial pyruvate carrier inhibition and anti-diabetic properties. PPARα/γ agonist 4 is expected to be used in research for dyslipidemic type 2 diabetes .
    PPARα/γ agonist 4
  • HY-P5396

    Amino Acid Decarboxylase Others
    GAD65 (524-543) is a biological active peptide with amino acids 524 to 543 fragment of glutamic acid decarboxylase 65 (GAD65). GAD65 (524-543) is one of the first fragments of islet antigen to induce proliferative T cell responses in the non-obese diabetic (NOD) mouse model of spontaneous autoimmune diabetes. GAD65 (524-543) is a specific, possibly low affinity, stimulus for the spontaneously arising diabetogenic T cell clone BDC2.5. Immunization with GAD65 (524-543) increases the susceptibility of the NOD mice to type 1 diabetes induced by the adoptive transfer of BDC2.5 T cells .
    GAD65 (524-543)
  • HY-120974

    GLUT Metabolic Disease
    α-Lipoic Acid Derivative 1 (Compound AN-7) is an α-lipoic acid derivative that enhances glucose transport in skeletal muscle by releasing active α-lipoic acid (LA), significantly improving glucose metabolism. In L6 skeletal muscle cells, α-Lipoic Acid Derivative 1 significantly increases glucose transport rates, approximately 12 times more potent than the parent compound α-lipoic acid (HY-N0492). In a mild diabetic mouse model, 10 mg/kg of α-Lipoic Acid Derivative 1 administered for two weeks significantly reduced blood glucose levels by 39%. α-Lipoic Acid Derivative 1 shows significant potential in research related to glucose metabolism in diabetes .
    α-lipoic acid derivative 1
  • HY-133806

    MetAP VEGFR Cardiovascular Disease Neurological Disease Metabolic Disease Cancer
    Fumarranol, a Fumagillin (HY-B0751) analogue, is a selective type 2 methionine aminopeptidase (MetAP2) inhibitor with a human IC50 of 3.2 μM. Fumarranol inhibits proliferation of bovine aortic endothelial cells and inhibits angiogenesis in a mouse matrigel plug model. Fumarranol can be used for the researches of cancer, diabetic retinopathy, age-related macular degeneration .
    Fumarranol
  • HY-123974

    PPAR Metabolic Disease
    BR101549 is a non-TZD agonist of PPARγ. BR101549 activates PPARγ to the level of Pioglitazone in vitro. BR101549 can control blood glucose level in mouse model. BR101549 can be studied in anti-diabetic research .
    BR101549
  • HY-139792

    SHR117887

    Endogenous Metabolite Metabolic Disease
    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 .
    Besigliptin tosylate
  • HY-P992410

    PAI-1 TGF-beta/Smad Inflammation/Immunology
    MEDI-579 is a fully human monoclonal antibody against PAI-1, with a KD value of 6 pM for human PAI-1 and 105 pM for rat PAI-1. MEDI-579 restores renal plasmin activity and inhibits PAI-1-mediated intracellular signal transduction. MEDI-579 reduces albuminuria, glomerulosclerosis severity, TGF-β1 expression level, and phosphorylated Smad2 level induced in diabetic mice. MEDI-579 decreases the levels of active PAI-1 in plasma and kidneys, and increases plasma plasmin level in a mouse model of lupus nephritis. MEDI-579 can be used in research related to diabetic nephropathy and lupus nephritis. The recommended isotype control is human IgG1 kappa (HY-P99001) .
    MEDI-579
  • HY-N17737

    Fatty Acid Synthase (FASN) Cytochrome P450 Metabolic Disease Inflammation/Immunology
    Floramanoside F is a type of flavonol glycoside compound. Floramanoside F has a moderate free radical scavenging effect, with a SC₅₀ value of 25.1 μM. Floramanoside F has a relatively weak inhibitory activity on aldose reductase, with a IC₅₀ value greater than 100 μM. Floramanoside F has strong binding affinity with key target enzymes of type 1 diabetic nephropathy (T1DN) (Fasn, Cyp2e1, Cyp4a32), and can inhibit lipid accumulation and oxidative stress, thereby alleviating renal inflammation and fibrosis. Floramanoside F can be used to study type 1 diabetic nephropathy and diabetic complications .
    Floramanoside F

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