Search Result
Results for "
Diabetic model
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-153126
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Biochemical Assay Reagents
Bacterial
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Infection
Metabolic Disease
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Yeast extract is a concentrate of the soluble components of yeast, especially Saccharomyces cerevisiae. Yeast extract is rich in nutritional components such as partially hydrolyzed proteins, free amino acids, B vitamins, and minerals. As a food ingredient, Yeast extract has both nutritional and flavoring properties. Yeast extract can also promote wound healing .
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- HY-111310
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ML351
2 Publications Verification
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Lipoxygenase
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Neurological Disease
Metabolic Disease
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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 .
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- HY-161834
-
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Pyroptosis
Aquaporin
NOD-like Receptor (NLR)
p38 MAPK
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Infection
Metabolic Disease
Inflammation/Immunology
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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 .
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- HY-P3247
-
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Insulin Receptor
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Neurological Disease
Metabolic Disease
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[D-Ala2]-GIP (human) is a GIP receptor agonist (EC50 = 630 pM). [D-Ala2]-GIP (human) improves glucose tolerance. [D-Ala2]-GIP (human) shows neuroprotective activity in MPTP (HY-W114750)-induced Parkinson's disease model. [D-Ala2]-GIP (human) also improves cognitive function and hippocampal synaptic plasticity in obese diabetic rats. [D-Ala2]-GIP (human) can be used for research of type 2 diabetes, Parkinson's disease, etc
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- HY-P99116
-
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RG7716; RO-6867461
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VEGFR
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
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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) .
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- HY-150105
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BMF-219; Menin-MLL inhibitor 21
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Epigenetic Reader Domain
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Metabolic Disease
Inflammation/Immunology
Cancer
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Icovamenib (BMF-219) is a selective, orally active, irreversible Menin inhibitor. Icovamenib forms a stable and irreversible covalent bond with Menin. Icovamenib promotes selective and controlled proliferation of beta cells and improvement of beta cell function in ex vivo human islet cultures. Icovamenib enhances glycemic control in animal diabetic models. Icovamenib induces a dose-dependent enhancement in insulin secretion potentiated by the GLP-1 RA. Icovamenib can be used for the study of multiple hematologic malignancies, solid tumors, and diabetes mellitus, such as diffuse large B-cell lymphoma (DLBCL), multiple myeloma (MM) and chronic lymphocytic leukemia and type 2 diabetes .
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- HY-P2917
-
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GyK
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Nuclear Hormone Receptor 4A/NR4A
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Metabolic Disease
Inflammation/Immunology
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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 .
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- HY-160186
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20-SOLA
1 Publications Verification
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Cytochrome P450
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Cardiovascular Disease
Metabolic Disease
Endocrinology
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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 .
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- HY-B0093A
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- HY-N0837
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NSC17821; NSC23880
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PI3K
Akt
mTOR
Autophagy
Apoptosis
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
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- HY-151500
-
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Amine N-methyltransferase
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Metabolic Disease
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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 .
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- HY-N0761
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- HY-W027553
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NIK-247 free base; Amiridine free base
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Cholinesterase (ChE)
Potassium Channel
Sodium Channel
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Neurological Disease
Metabolic Disease
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Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K + and Na +-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
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- HY-164781
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- HY-101666
-
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Deubiquitinase
Apoptosis
MDM-2/p53
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Metabolic Disease
Cancer
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HBX 41108 is an inhibitor of ubiquitin-specific protease 7 (USP7) with an IC50 of 424 nM. HBX 41108 inhibits USP7-mediated p53 deubiquitination to stabilize p53 and inhibits cancer cell growth. BX 41108 can be used in cancer and diabetes research .
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- HY-76383
-
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COX
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Metabolic Disease
Inflammation/Immunology
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LR-90 is an advanced glycation end product (AGE) inhibitor, inhibits inflammatory responses in human monocytes . LR-90 is also used in the research of diabetic animal model .
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- HY-N4195
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Resveratrol glycoside; trans-Resveratrol 4'-O-β-D-glucopyranoside
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Glycosidase
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Cardiovascular Disease
Metabolic Disease
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Resveratroloside (Resveratrol glycoside) is an orally active competitive inhibitor of α-glucosidase. Resveratroloside has hypoglycemic and cardioprotective effects. Resveratroloside can be used for the research of diabetes and heart system diseases .
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- HY-B0093
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CGS14824A free base
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Angiotensin-converting Enzyme (ACE)
Apoptosis
Reactive Oxygen Species (ROS)
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Cardiovascular Disease
Cancer
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Benazepril (CGS14824A free base) is an orally active angiotensin-converting enzyme (ACE) inhibitor to reduce angiotensin-II production. Benazepril inhibits oxidative stress and inhibits apoptosis by the PI3K/Akt signaling pathway. Benazepril improves diabetic nephropathy and decreases proteinuria. Benazepril can be used in the study of hypertension, heart failure and diabetic nephropathy .
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- HY-B1451
-
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TA-6366
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Angiotensin-converting Enzyme (ACE)
MMP
JNK
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Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Imidapril hydrochloride (TA-6366) is an orally active dual inhibitor of angiotensin-converting enzyme (ACE) and MMP-9. Imidapril hydrochloride inhibits lipopolysaccharide-induced phosphorylation of c-Jun, MKK4 and JNK in monocytes, and downregulates the production of specific inflammatory factors such as TNF-α and IP-10, thereby exerting anti-inflammatory activity. Imidapril hydrochloride also effectively ameliorates mesangial expansion and reduces urinary albumin excretion by inhibiting angiotensin AngII production, lowering glomerular pressure and oxidative stress, thus delaying disease progression. Imidapril hydrochloride can also directly bind to the active site of MMP-9 to inhibit gelatinase activity, and suppress the enlargement of cerebral aneurysms without altering systemic blood pressure. Imidapril hydrochloride is widely applicable to related studies on autoimmune glomerulonephritis, diabetic nephropathy, cerebral aneurysms and other conditions .
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- HY-128442
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Phenyl hydrogen sulfate
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Endogenous Metabolite
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Metabolic Disease
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Phenyl sulfate is an orally active gut microbiota-derived metabolite. Phenyl sulfate induces albuminuria and podocyte damage in experimental models of diabetes. Phenyl sulfate can be used as a disease marker in diabetic kidney disease .
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- HY-W010649
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HSP
Epigenetic Reader Domain
ATP-binding cassette (ABC) transporters
Bacterial
Fungal
Antibiotic
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Infection
Metabolic Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-113089
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H-Glu(H-Lys-OH)-OH; γ-Glu-ε-Lys
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Endogenous Metabolite
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Metabolic Disease
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Epsilon-(gamma-glutamyl)-lysine is an N(6)-acyl-L-lysine derivative. The enzyme tissue transglutaminase (tTg) helps the formation of epsilon-(gamma-glutamyl)lysine bonds between ECM components in some disease, such as non-diabetic kidney, glaucoma filtration .
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- HY-151500B
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Amine N-methyltransferase
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Metabolic Disease
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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 .
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- HY-15195
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Ro 67-0565; SPP-301
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
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Avosentan (Ro 67-0565; SPP-301) is an orally active endothelin (ETA) receptor antagonist. Avosentan can block the ETA receptor, thereby reducing vascular contraction and exerting a renal protective effect. Avosentan inhibits vascular contraction caused by ET-1 and alleviates the reduction in retinal and optic nerve head blood flow induced by it, lowering intraocular pressure in the glaucoma monkey model. Avosentan non-specifically blocks ETB receptors at high doses, inhibiting ETB-mediated diuresis and natriuresis, and may cause fluid retention. Avosentan can be used to reduce proteinuria with diabetic nephropathy, but induces significant fluid overload and congestive heart failure .
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- HY-16421
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(-)-DRF 2725; NNC 61-0029
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PPAR
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Metabolic Disease
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Ragaglitazar is a PPARα and PPARγ agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models. Ragaglitazar improves glycemic control and lipid profile in type 2 diabetic.
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- HY-13967B
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Bacterial
Free Fatty Acid Receptor
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Metabolic Disease
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AMG 837 calcium hydrate is an orally active, selective GPR40/FFA1 agonist with an EC50 of 1.5 nM against human GPR40. AMG 837 calcium hydrate stimulates insulin secretion in a glucose-dependent manner, and effectively improves glycemic control in both normal and diabetic rodent models . AMG 837 calcium hydrate binds to the BacA protein and impairs the survival and replication of Brucella. AMG 837 calcium hydrate can be used in research related to type 2 diabetes and brucellosis .
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- HY-121811
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Lanceolatin C
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Glycosidase
Phosphatase
Interleukin Related
TNF Receptor
COX
Beclin1
GLUT
FAK
Akt
mTOR
p38 MAPK
Keap1-Nrf2
Apoptosis
Amyloid-β
Tau Protein
Autophagy
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Neurological Disease
Inflammation/Immunology
Cancer
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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, Aβ 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 .
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- HY-113089A
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H-Glu(H-Lys-OH)-OH TFA; γ-Glu-ε-Lys TFA
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Endogenous Metabolite
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Metabolic Disease
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Epsilon-(gamma-glutamyl)-lysine (H-Glu(H-Lys-OH)-OH) TFA is an N(6)-acyl-L-lysine derivative. The enzyme tissue transglutaminase (tTg) helps the formation of epsilon-(gamma-glutamyl)lysine bonds between ECM components in some disease, such as non-diabetic kidney, glaucoma filtration .
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- HY-W197205
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Sirtuin
Histone Acetyltransferase
PEPCK
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Metabolic Disease
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SL010110 is an anti-hyperglycemic agent. SL010110 potently inhibits gluconeogenesis by inhibiting SIRT2, activating p300, and subsequently promoting PEPCK1 degradation. SL010110 downregulates the protein level of PEPCK1 without affecting the gene expressions of PEPCK, glucose-6-phosphatase, and fructose-1,6-bisphosphatase. SL010110 significantly improves glucose homeostasis in type 2 diabetic (T2D) mice model. SL010110 can be used for T2D research .
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- HY-116005
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Adenosine Kinase
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Neurological Disease
Inflammation/Immunology
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A-286501 is an orally active and potent carbocyclic nucleoside adenosine kinase inhibitor with an IC50 value of 0.47 nM, which shows analgesic and anti-inflammatory effects. A-286501 reduces nociception in animal models of acute (thermal), inflammatory (formalin and carrageenan) and neuropathic (L5/L6 nerve ligation and streptozotocin-induced diabetic) pain. A-286501 also reduces Carrageenan (HY-125474)-induced paw edema and myeloperoxidase activity in the injured paw. A-286501 is promising for research of analgesic and anti-inflammatory agents .
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- HY-P5396A
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Amino Acid Decarboxylase
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Others
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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 .
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- HY-151500A
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Amine N-methyltransferase
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Metabolic Disease
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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 .
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- HY-179041
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PGE synthase
Prostaglandin Receptor
MDM-2/p53
Amino acid Transporter
Glutathione Peroxidase
Ferroptosis
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Metabolic Disease
Endocrinology
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SZ0232 is a selective mPGES-2 inhibitor. SZ0232 binds to the active site of mPGES-2 via hydrogen bonds and π-π stacking, reduces the production of prostaglandin E2 (PGE2) and blocks the PGE2-EP3 pathway. SZ0232 regulates Ferroptosis by activating the heme-dependent p53/SLC7A11/GPX4 axis, inhibits lipid peroxidation, and protects renal tubules. SZ0232 enhances glucose-stimulated insulin secretion, inhibits β-cell senescence, and improves glucose homeostasis. SZ0232 reduces renal lipid accumulation, alleviates fibrosis, and ameliorates renal dysfunction in diabetic mice. SZ0232 inhibits renal cyst growth in polycystic kidney disease models. SZ0232 exhibits an insulinotropic effect that strengthens with the increase of animal age. SZ0232 can be used in studies related to type 2 diabetes, acute kidney injury, diabetic kidney disease, and autosomal dominant polycystic kidney disease .
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- HY-N0837R
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NSC17821 (Standard); NSC23880 (Standard)
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Reference Standards
PI3K
Akt
mTOR
Autophagy
Apoptosis
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Neurological Disease
Metabolic Disease
Cancer
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Veratramine (NSC17821; NSC23880) (Standard) is the analytical standard of Veratramine (HY-N0837). This product is intended for research and analytical applications. Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
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- HY-106915
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SPR 210
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Aldose Reductase
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Neurological Disease
Metabolic Disease
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SG-210 (SPR 210) is an orally active and selective aldose reductase (AR) inhibitor. SG-210 has IC50 values of 9.5 nM and 10 nM for AR from porcine lens and human placenta, respectively. SG-210 can inhibit sorbitol accumulation and ameliorate diabetic neuropathy and retinopathy in Streptozotocin (HY-13753)-induced diabetic rats. SG-210 can be used in the research of diseases such as diabetes-related complications .
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- HY-178780
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GPR119
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Metabolic Disease
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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 .
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- HY-138007
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ROR
PPAR
LXR
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Metabolic Disease
Inflammation/Immunology
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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 .
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- HY-145559
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KU-596
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HSP
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Metabolic Disease
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Cemdomespib (KU-596) is a highly bioavailable second-generation Hsp90 modulator. Cemdomespib has shown efficacy in improving sensory deficits in models of diabetic peripheral neuropathy. Cemdomespib induces Hsp70 levels and manifest neuroprotective activity through induction of the heat shock response .
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- HY-144289
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Glucokinase
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Metabolic Disease
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BMS-820132 is an orally active and partial glucokinase (GK) activator with a AC50 of 29 nM. BMS-820132 decreases the glucose levels in glucose tolerance test (OGTT) model in normal rats, but not Zucker diabetic fatty (ZDF) rats. BMS-820132 exhibits pharmacological toxicity secondary to strong GK activation .
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- HY-13967
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AMG 837
3 Publications Verification
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Free Fatty Acid Receptor
Bacterial
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Infection
Metabolic Disease
|
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AMG 837 is an orally active, selective GPR40/FFA1 agonist with an EC50 of 1.5 nM against human GPR40. AMG 837 stimulates insulin secretion in a glucose-dependent manner, and effectively improves glycemic control in both normal and diabetic rodent models . AMG 837 binds to the BacA protein and impairs the survival and replication of Brucella. AMG 837 can be used in research related to type 2 diabetes and brucellosis .
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- HY-113089AR
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H-Glu(H-Lys-OH)-OH TFA (Standard); γ-Glu-ε-Lys TFA (Standard)
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Endogenous Metabolite
Reference Standards
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Metabolic Disease
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Epsilon-(gamma-glutamyl)-lysine (TFA) (Standard) is the analytical standard of Epsilon-(gamma-glutamyl)-lysine (TFA). This product is intended for research and analytical applications. Epsilon-(gamma-glutamyl)-lysine (H-Glu(H-Lys-OH)-OH) TFA is an N(6)-acyl-L-lysine derivative. The enzyme tissue transglutaminase (tTg) helps the formation of epsilon-(gamma-glutamyl)lysine bonds between ECM components in some disease, such as non-diabetic kidney, glaucoma filtration .
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- HY-151500C
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Amine N-methyltransferase
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Metabolic Disease
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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 .
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- HY-179578
-
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Enolase
AMPK
Autophagy
Apoptosis
mTOR
Caspase
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Metabolic Disease
Cancer
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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 .
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- HY-14923
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AVE 7688
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Angiotensin-converting Enzyme (ACE)
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Metabolic Disease
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Ilepatril, a dual inhibitor of angiotensin-converting enzyme (ACE) and neutral endopeptidase, has inhibitory effects in the type 2 diabetic nephropathy model in obese Zucker diabetic fatty (ZDF) rats. Ilepatril significantly reduced albuminuria in a dose-dependent manner and may be a strategy distinct from metabolic control to inhibit type 2 diabetic nephropathy .
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- HY-100819
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CCR
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Metabolic Disease
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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 .
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- HY-124483
-
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Arrestin
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Metabolic Disease
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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 .
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- HY-161682
-
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GPR84
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Neurological Disease
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GPR84 antagonist 9 (compound 320) is an orally active GPR84 antagonist with the IC50 of 0.012 μM. GPR84 antagonist 9 can be used for study of inflammatory-driven pain diseases .
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- HY-160602
-
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Free Fatty Acid Receptor
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Metabolic Disease
|
|
CPL207280 is an orally active GPR40/FFA1 agonist with an antidiabetic effect. CPL207280 can effectively enhance glucose-stimulated insulin secretion and improve glucose tolerance in MIN6 pancreatic β-cells as well as in healthy Wistar Han rats and diabetic rat models. CPL207280 can be used for the research of type 2 diabetes .
|
-
-
- HY-12614
-
|
|
Glucokinase
|
Metabolic Disease
|
|
AMG-1694 is a potent glucokinase–glucokinase regulatory protein (GK-GKRP) disruptors and promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, indirectly increasing GK enzymatic activity. AMG-1694 potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation. AMG-1694 normalizes blood glucose levels in several rodent models of diabetes and lowes blood glucose restricted to diabetic and not normoglycaemic animals .
|
-
-
- HY-149837
-
|
|
Fluorescent Dye
|
Inflammation/Immunology
|
|
PRO-F is a photoactivable H2S donor with ROS scavenging ability. PRO-F can be activated by light to produce fluorescent signal, for real-time tracking of released H2S. PRO-F activation doesn’t consume endogenous substances. deliver H2S in an intracellular environment to protect cells from excessive reactive oxygen species (ROS) induced damage. PRO-F shows enhancement on chronic wound healing, researched in diabetic models as well .
|
-
- 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.
|
-
- 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) .
|
-
- HY-134261
-
|
8-Bromoadenosine-5'-O-diphosphoribose
|
TRP Channel
CaMK
|
Metabolic Disease
Cancer
|
|
8-Br-ADPR (8-Bromoadenosine-5'-O-diphosphoribose) is a TRPM2 inhibitor and ADPR signaling pathway antagonist. 8-Br-ADPR inhibits glucagon-mediated nuclear calcium signaling and downstream CaMKII/CREB phosphorylation by blocking ADPR-induced TRPM2 activation. 8-Br-ADPR significantly reduces gluconeogenic gene expression and blood glucose levels in diabetic models. 8-Br-ADPR effectively blocks ADPR-mediated calcium signal transduction in NK cells, inhibits immune synapse formation, granzyme B release and cytolytic activity against melanoma cells. 8-Br-ADPR is widely used in studies related to diseases such as diabetes, melanoma and lymphoma .
|
-
- HY-134261A
-
|
8-Bromoadenosine-5'-O-diphosphoribose disodium
|
CaMK
TRP Channel
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
8-Br-ADPR disodium (8-Bromoadenosine-5'-O-diphosphoribose) is a TRPM2 inhibitor and ADPR signaling pathway antagonist. 8-Br-ADPR disodium inhibits glucagon-mediated nuclear calcium signaling and downstream CaMKII/CREB phosphorylation by blocking ADPR-induced TRPM2 activation. 8-Br-ADPR disodium significantly reduces gluconeogenic gene expression and blood glucose levels in diabetic models. 8-Br-ADPR disodium effectively blocks ADPR-mediated calcium signal transduction in NK cells, inhibits immune synapse formation, granzyme B release and cytolytic activity against melanoma cells. 8-Br-ADPR disodium is widely used in studies related to diseases such as diabetes, melanoma and lymphoma .
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-
- HY-W027553R
-
|
NIK-247 free base (Standard); Amiridine free base (Standard)
|
Reference Standards
Cholinesterase (ChE)
Potassium Channel
Sodium Channel
|
Neurological Disease
Metabolic Disease
|
|
Ipidacrine (Standard) is the analytical reference standard of Ipidacrine. This product is used for research and analytical applications. Ipidacrine is orally active and blood-brain-barrier-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K + and Na +-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
|
-
- HY-175340
-
|
|
Potassium Channel
TSPO
|
Neurological Disease
|
|
Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active Kv7.2/Kv7.3 and TSPO activator. Kv7.2/Kv7.3 activator-3 activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with Ki values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). Kv7.2/Kv7.3 activator-3 prevents motor neuron degeneration in mice and humans conditioned by ALS/FTD astrocytes. Kv7.2/Kv7.3 activator-3 stimulates dorsal root ganglion axonal growth through TSPO and Kv7.2/3 activation. Kv7.2/Kv7.3 activator-3 has anti-epileptic effects in epileptic seizure models. Kv7.2/Kv7.3 activator-3 reduces pain hypersensitivity in patients with diabetic neuropathy, promotes neuronal survival and regeneration after cervical neuropathy in rats, and accelerates the recovery of normal function of sensory and motor neurons .
|
-
- 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 .
|
-
- HY-123409
-
|
|
TGF-β Receptor
|
Metabolic Disease
|
|
Nicousamide is a potent inhibitor of TGF-β RII phosphorylation. Nicousamide can be used to study renal fibrosis in animal models of diabetic nephropathy .
|
-
- 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.
|
-
- HY-128442R
-
|
Phenyl hydrogen sulfate (Standard)
|
Endogenous Metabolite
Reference Standards
|
Metabolic Disease
|
|
Phenyl sulfate (Standard) is the analytical standard of Phenyl sulfate. This product is intended for research and analytical applications. Phenyl sulfate is an orally active gut microbiota-derived metabolite. Phenyl sulfate induces albuminuria and podocyte damage in experimental models of diabetes. Phenyl sulfate can be used as a disease marker in diabetic kidney disease .
|
-
- 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 .
|
-
- HY-168214
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Kv7.2/Kv7.3 agonist 1 (Compound 16) is an orally active agonist for KV7.2/7.3 channel (KCNQ2/3) with an EC50 of 1.03 μM. Kv7.2/Kv7.3 agonist 1 exhibits analgesic efficacy in mice chronic constriction injury (CCI) model and mice Streptozotocin (HY-13753)-induced diabetic peripheral neuropathic pain (DPNP) model, with ED50 of 12.02 and 9.63 mg/kg .
|
-
- 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-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) .
|
-
- 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 .
|
-
- HY-13967A
-
|
|
Bacterial
Free Fatty Acid Receptor
|
Infection
Metabolic Disease
|
|
AMG 837 sodium salt is an orally active, selective GPR40/FFA1 agonist with an EC50 of 1.5 nM against human GPR40. AMG 837 sodium salt stimulates insulin secretion in a glucose-dependent manner, and effectively improves glycemic control in both normal and diabetic rodent models . AMG 837 sodium salt binds to the BacA protein and impairs the survival and replication of Brucella. AMG 837 sodium salt can be used in research related to type 2 diabetes and brucellosis .
|
-
- HY-162639
-
|
|
Glycosidase
Cholinesterase (ChE)
|
Neurological Disease
Metabolic Disease
|
|
α-Glucosidase-IN-68 (Compound 2) is an inhibitor for α-Glucosidase, AChE, and BChE, with IC50 of 0.251, 0.774 and 0.793 μM, respectively. α-Glucosidase-IN-68 exhibits antioxidant efficacy, with IC50 of 0.69 μM and 0.02 μM, in DPPH and ABTS experiments. α-Glucosidase-IN-68 exhibits antidiabetic effect in Streptozotocin (HY-13753)-induced diabetic rat models .
|
-
- 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 .
|
-
- 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 .
|
-
- 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 .
|
-
- HY-170233
-
|
|
NOD-like Receptor (NLR)
Interleukin Related
NF-κB
|
Inflammation/Immunology
|
|
NLRP3-IN-75 is an orally active NLRP3 inhibitor. NLRP3-IN-75 suppresses IL-1β secretion (IC50 = 23 nM). NLRP3-IN-75 selectively inhibits NLRP3 activation by disrupting inflammasome assembly without affecting NLRC4 or AIM2 inflammasomes. NLRP3-IN-75 exhibits superior efficacy in acute peritonitis, diabetic kidney disease and IBD models .
|
-
- 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-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 .
|
-
- 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 .
|
-
- HY-15195R
-
|
Ro 67-0565 (Standard); SPP-301 (Standard)
|
Reference Standards
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Avosentan (Standard) is the analytical standard of Avosentan (HY-15195). This product is intended for research and analytical applications. Avosentan is an orally active endothelin (ETA) receptor antagonist. Avosentan can block the ETA receptor, thereby reducing vascular contraction, and exerting a renal protective effect. Avosentan inhibits vascular contraction caused by ET-1 and alleviates the reduction in retinal and optic nerve head blood flow induced by it, lowering intraocular pressure in the glaucoma monkey model. Avosentan non-specifically blocks ETB receptors at high doses, inhibiting ETB-mediated diuresis and natriuresis, and may cause fluid retention. Avosentan can be used to reduce proteinuria with diabetic nephropathy, but induces significant fluid overload and congestive heart failure.
|
-
- 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 .
|
-
- HY-W027553S1
-
|
NIK-247-d9 free base
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
Potassium Channel
Sodium Channel
|
Metabolic Disease
|
|
Ipidacrine-d9 (NIK-247-d9 (free base)) is the deuterium labeled Ipidacrine (HY-W027553). Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
|
-
- HY-181094
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-110 is a selective and orally active competitive inhibitor of α-Glucosidase with an IC50 of 7.09 μM and a Ki of 6.9 μM. α-Glucosidase-IN-110 can reduce fasting blood glucose levels, improve glucose tolerance, and restore the histomorphology of liver and pancreatic tissues in diabetic rat models. α-Glucosidase-IN-110 can be used for the research of diabetes .
|
-
- 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 .
|
-
- HY-119058
-
|
CP-744809
|
Aldose Reductase
|
Metabolic Disease
|
|
ARI-809 (CP-744809) is a highly selective, orally active aldose reductase inhibitor with an IC50 of 1 nM. ARI-809 blocks excessive glucose flux through the polyol pathway. ARI-809 normalizes elevated sorbitol and fructose levels in sciatic nerve tissues of diabetic rat models, inhibits sorbitol accumulation in lens tissues, and brings elevated urinary albumin excretion close to normal. ARI-809 can be used in diabetes research .
|
-
- 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-173130
-
|
|
Glycosidase
|
Metabolic Disease
Inflammation/Immunology
|
|
α-Glucosidase-IN-86 (Compound A4) is an orally active α-glucosidase inhibitor with an IC50 of 2.72 μM. α-Glucosidase-IN-86 has high safety in mice. α-Glucosidase-IN-86 can reduce fasting blood glucose levels, improve glucose tolerance, regulate blood lipids, and has antioxidant effects in diabetic mice. α-Glucosidase-IN-86 can be used for the research of diabetes .
|
-
- HY-101666R
-
|
|
Deubiquitinase
Reference Standards
Apoptosis
MDM-2/p53
|
Metabolic Disease
Cancer
|
|
HBX 41108 (Standard) is the analytical standard of HBX 41108 (HY-101666). This product is intended for research and analytical applications. HBX 41108 is an inhibitor of ubiquitin-specific protease 7 (USP7) with an IC50 of 424 nM. HBX 41108 inhibits USP7-mediated p53 deubiquitination to stabilize p53 and inhibits cancer cell growth. BX 41108 can be used in cancer and diabetes research .
|
-
- 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 .
|
-
- HY-182438
-
|
|
Drug Intermediate
|
Metabolic Disease
|
|
SDZ 51641 is an orally active fatty acid oxidation inhibitor. By reducing fatty acid oxidation, SDZ 51641 deprives the gluconeogenesis process of required energy and cofactors, thereby lowering blood glucose levels in diabetic models. SDZ 51641 can be used in diabetes research .
|
-
- HY-76383R
-
|
|
COX
|
Metabolic Disease
Inflammation/Immunology
|
|
LR-90 (Standard) is the analytical standard of LR-90. This product is intended for research and analytical applications. LR-90 is an advanced glycation end product (AGE) inhibitor, inhibits inflammatory responses in human monocytes . LR-90 is also used in the research of diabetic animal model .
|
-
- HY-N19615
-
|
|
Keap1-Nrf2
GSK-3
TNF Receptor
Interleukin Related
SOD
|
Inflammation/Immunology
|
|
Isoeucommin A is a lignan compound. Isoeucommin A activates the Nrf2/HO-1 pathway and induces phosphorylation of GSK-3β. Isoeucommin A reduces the levels of pro-inflammatory cytokines TNF-α, IL-1β and IL-6, decreases the oxidative stress marker MDA, increases the antioxidants SOD and GSH, and alleviates oxidative stress in mesangial cells. Isoeucommin A alleviates renal tissue injury, improves impaired renal function and enhances the viability of renal tubular epithelial cells in diabetic nephropathy models. Isoeucommin A can be used in the research of diabetic nephropathy .
|
-
- HY-180528
-
|
|
SGLT
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
SGLT2-IN-6 (Compound 101) is an orally active SGLT2 inhibitor with IC₅₀ values for SGLT2, SGLT1, and DPP4 of 0.8, 6.7, and 72 nM respectively. SGLT2-IN-6 controls blood sugar levels in diabetic rat models and increases the levels of active GLP-1. SGLT2-IN-6 can be used for the study of type 2 diabetes .
|
-
- HY-180527
-
|
|
SGLT
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
SGLT2-IN-5 (Compound 99) is an orally active SGLT2 inhibitor with IC₅₀ values for SGLT2, SGLT1, and DPP4 of 0.8, 23, and 58 nM respectively. SGLT2-IN-5 controls blood sugar levels in diabetic rat models and increases the levels of active GLP-1. SGLT2-IN-5 can be used for the study of type 2 diabetes .
|
-
- 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) .
|
-
- HY-181126
-
|
|
HDAC
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
G194-0712 is a selective histone deacetylase 5 (HDAC5) activator with an EC50 of 7.96 μM and a Kd of 2.53 μM. G194-0712 restores ACTN4-K417 deacetylation and nuclear import, and increases CSTA expression. G194-0712 accelerates wound closure in chronic wound models, reducing wound area and epithelial gap. G194-0712 can be used for the research of chronic skin wounds, such as diabetic wounds, ischemic wounds, radiation injury wounds .
|
-
- 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 .
|
-
- 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 .
|
-
- HY-19689
-
|
NIK-247; Amiridine
|
Cholinesterase (ChE)
Potassium Channel
Sodium Channel
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
|
Ipidacrine (NIK-247; Amiridine) hydrochloride is orally active and blood-brain-barrier-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine hydrochloride has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine hydrochloride is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine hydrochloride is effective in various amnesia models, improves erectile function and inhibits K + and Na +-channels in the neuronal membrane in diabetic rats. Ipidacrine hydrochloride is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
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- HY-118945
-
|
|
Prostaglandin Receptor
Bradykinin Receptor
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
FR191413 is a selective bradykinin B2 receptor agonist that stimulates prostaglandin E2 production in WI-38 cells and activates BK B2 receptor-mediated pathways such as vasodilation and organ protection. FR191413 competitively binds to [ 3H]-BK in guinea pig ileum (GPI) membranes and CHO cells transfected with the human BK B2 receptor, with IC50 values of 20.0 nM and 2.60 nM, respectively. FR191413 can be used in research related to cardiovascular diseases and diabetes, including hypertension, myocardial hypertrophy, myocardial infarction, arrhythmias, and diabetic nephropathy .
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| Cat. No. |
Product Name |
Type |
-
- HY-153126
-
|
|
Biochemical Assay Reagents
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Yeast extract is a concentrate of the soluble components of yeast, especially Saccharomyces cerevisiae. Yeast extract is rich in nutritional components such as partially hydrolyzed proteins, free amino acids, B vitamins, and minerals. As a food ingredient, Yeast extract has both nutritional and flavoring properties. Yeast extract can also promote wound healing .
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3247
-
|
|
Insulin Receptor
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Neurological Disease
Metabolic Disease
|
|
[D-Ala2]-GIP (human) is a GIP receptor agonist (EC50 = 630 pM). [D-Ala2]-GIP (human) improves glucose tolerance. [D-Ala2]-GIP (human) shows neuroprotective activity in MPTP (HY-W114750)-induced Parkinson's disease model. [D-Ala2]-GIP (human) also improves cognitive function and hippocampal synaptic plasticity in obese diabetic rats. [D-Ala2]-GIP (human) can be used for research of type 2 diabetes, Parkinson's disease, etc
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- HY-113089
-
|
H-Glu(H-Lys-OH)-OH; γ-Glu-ε-Lys
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Epsilon-(gamma-glutamyl)-lysine is an N(6)-acyl-L-lysine derivative. The enzyme tissue transglutaminase (tTg) helps the formation of epsilon-(gamma-glutamyl)lysine bonds between ECM components in some disease, such as non-diabetic kidney, glaucoma filtration .
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-
- HY-113089A
-
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H-Glu(H-Lys-OH)-OH TFA; γ-Glu-ε-Lys TFA
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Endogenous Metabolite
|
Metabolic Disease
|
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Epsilon-(gamma-glutamyl)-lysine (H-Glu(H-Lys-OH)-OH) TFA is an N(6)-acyl-L-lysine derivative. The enzyme tissue transglutaminase (tTg) helps the formation of epsilon-(gamma-glutamyl)lysine bonds between ECM components in some disease, such as non-diabetic kidney, glaucoma filtration .
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- HY-P5396A
-
|
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Amino Acid Decarboxylase
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Others
|
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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 .
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-
- HY-P4866
-
|
|
Peptides
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Metabolic Disease
|
|
Q-Peptide is the angiopoietin-1 derived peptide (QHREDGS).Q-Peptide increases keratinocyte migration to improve wound healing, in diabetic mouse model. Q-Peptide accelerates wound closure .
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-
- HY-113089AR
-
|
H-Glu(H-Lys-OH)-OH TFA (Standard); γ-Glu-ε-Lys TFA (Standard)
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Endogenous Metabolite
Reference Standards
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Metabolic Disease
|
|
Epsilon-(gamma-glutamyl)-lysine (TFA) (Standard) is the analytical standard of Epsilon-(gamma-glutamyl)-lysine (TFA). This product is intended for research and analytical applications. Epsilon-(gamma-glutamyl)-lysine (H-Glu(H-Lys-OH)-OH) TFA is an N(6)-acyl-L-lysine derivative. The enzyme tissue transglutaminase (tTg) helps the formation of epsilon-(gamma-glutamyl)lysine bonds between ECM components in some disease, such as non-diabetic kidney, glaucoma filtration .
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-
- 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 .
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-
- 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 .
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-
- 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 .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- 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) .
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-
(5)
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- HY-P991310
-
|
LT3015; LT-3000
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LPL Receptor
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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) .
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-
(5)
-
- 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) .
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-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0837
-
|
NSC17821; NSC23880
|
Alkaloids
Piperidine Alkaloids
Structural Classification
other families
Classification of Application Fields
Plants
Disease Research Fields
Source Classification
Cancer
|
PI3K
Akt
mTOR
Autophagy
Apoptosis
|
|
Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
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-
-
- HY-N0761
-
-
-
- HY-N4195
-
-
-
- HY-B0093
-
-
-
- HY-128442
-
-
-
- HY-113089
-
-
-
- HY-121811
-
|
Lanceolatin C
|
Structural Classification
Pongamia pinnata (L.) Pierre
Leguminosae
Ketones, Aldehydes, Acids
Derris trifoliata Lour.
Plants
Source Classification
|
Glycosidase
Phosphatase
Interleukin Related
TNF Receptor
COX
Beclin1
GLUT
FAK
Akt
mTOR
p38 MAPK
Keap1-Nrf2
Apoptosis
Amyloid-β
Tau Protein
Autophagy
|
|
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, Aβ 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 .
|
-
-
- HY-113089A
-
-
-
- HY-N0837R
-
|
NSC17821 (Standard); NSC23880 (Standard)
|
Alkaloids
Piperidine Alkaloids
Structural Classification
other families
Plants
Source Classification
|
Reference Standards
PI3K
Akt
mTOR
Autophagy
Apoptosis
|
|
Veratramine (NSC17821; NSC23880) (Standard) is the analytical standard of Veratramine (HY-N0837). This product is intended for research and analytical applications. Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
|
-
-
- HY-113089AR
-
|
H-Glu(H-Lys-OH)-OH TFA (Standard); γ-Glu-ε-Lys TFA (Standard)
|
Structural Classification
Natural Products
Endogenous metabolite
Source Classification
|
Endogenous Metabolite
Reference Standards
|
|
Epsilon-(gamma-glutamyl)-lysine (TFA) (Standard) is the analytical standard of Epsilon-(gamma-glutamyl)-lysine (TFA). This product is intended for research and analytical applications. Epsilon-(gamma-glutamyl)-lysine (H-Glu(H-Lys-OH)-OH) TFA is an N(6)-acyl-L-lysine derivative. The enzyme tissue transglutaminase (tTg) helps the formation of epsilon-(gamma-glutamyl)lysine bonds between ECM components in some disease, such as non-diabetic kidney, glaucoma filtration .
|
-
-
- HY-128442R
-
-
-
- HY-N19615
-
-
-
- HY-N17737
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-W027553S1
-
|
|
|
Ipidacrine-d9 (NIK-247-d9 (free base)) is the deuterium labeled Ipidacrine (HY-W027553). Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
|
-
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