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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
186 Results for "
Islet
" in MedChemExpress (MCE) Product Catalog:
Products (186)
186 Results for "Islet" in MCE Product Catalog:
31
Target:
Sitagliptin (MK-0431) is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes .
31
Target:
Sitagliptin (MK-0431) phosphate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes .
31
31 Publications Verification
別名: MK-0431 phosphate monohydrate
Target:
Sitagliptin (MK-0431) phosphate monohydrate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate monohydrate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate monohydrate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate monohydrate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate monohydrate can be used for the study of 1-type and 2-type diabetes .
12
Category:
Infection Ketones, Aldehydes, Acids Phenols Polyphenols Plants Bowdichia virgilioides Compositae Endogenous metabolite Disease Research Fields
Target:
7
7 Cited Publications
Target:
研究分野:
BMS493 is an inverse pan-retinoic acid receptor (RAR) agonist. BMS493 increases nuclear corepressor interaction with RARs. BMS493 also could prevent retinoic acid-induced differentiation . BMS493 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
7
7 Cited Publications
製品番号: HY-16307
CAS 番号: 261365-11-1
Target:
研究分野:
MB05032 is a fructose-1,6-bisphosphatase (FBP1/FBPase) inhibitor with an IC50 value of 16 nM. MB05032 blocks FBP1-mediated glycolysis inhibition in NK cells, restores NK cell glucose uptake, lactate production, degranulation, perforin production, and cytotoxicity against gastric cancer cells. MB05032 elevates ATP/ADP ratios, increases glucose utilization, and enhances insulin secretion in pancreatic β-cells. MB05032 increases neutrophil adhesion, phagocytosis, and mRNA abundance of HKII, ITGA9, CD36 in subclinically hypocalcemic dairy cows. MB05032 inhibits gluconeogenesis in hepatocytes, acts as the active metabolite of prodrug Managlinat dialanetil (MB06322) (HY-14955). MB05032 can be used for the research of gastric cancer, type 2 diabetes, subclinical hypocalcemia, and insulin resistance .
6
6 Cited Publications
別名: Arachidonyl trifluoromethyl ketone
Target:
研究分野:
AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeant trifluoromethyl ketone analog of arachidonic acid. AACOCF3 is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). AACOCF3 blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. AACOCF3 has the potential for the research of cardiovascular disease .
3
3 Cited Publications
製品番号: HY-W030796A
CAS 番号: 150436-68-3
Target:
研究分野:
Lactisole is a canonical antagonist of sweet taste receptor, selectively targeting to T1R3 subunit, a glucose-sensing receptor. Lactisole inhibits insulin secretion induced by glucose in mouse islets .
3
3 Cited Publications
Target:
研究分野:
AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s .
3
3 Cited Publications
製品番号: HY-W030796
CAS 番号: 13794-15-5
Target:
研究分野:
Lactisole free acid is a canonical antagonist of sweet taste receptor, selectively targeting to T1R3 subunit, a glucose-sensing receptor. Lactisole free acid inhibits insulin secretion induced by glucose in mouse islets .
3
研究分野:
Miglitol (BAY-m1099) is an orally active antidiabetic compound that inhibits the breakdown of glycoconjugates into glucose. Miglitol inhibits glycoside hydrolase enzymes called α-glucosidases. Miglitol inhibits oxidative stress-induced apoptosis and mitochondrial ROS over-production in endothelial cells by enhancement of AMP-activated protein kinase. Dietary supplementation with Miglitol from pre-onset stage in OLETF rats delays the onset and development of diabetes and preserves the insulin secretory function of pancreatic islets .
3
3 Cited Publications
製品番号: HY-13967
CAS 番号: 865231-46-5
Target:
研究分野:
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 .
2
Target:
研究分野:
Glipizide (CP 2872; K 4024)?a potent, orally active and sulfonylurea class anti-diabetic agent and can be used for type 2?diabetes mellitus research but not type 1. Glipizide acts by partially blocking ATP-sensitive potassium?(KATP) channels among β cells of pancreatic islets of Langerhans .
2
2 Cited Publications
Target:
研究分野:
BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells .
2
Ligandrol is an orally active, selective androgen receptor (AR) agonist. Ligandrol enhances protein synthesis, inhibits muscle breakdown and oxidative stress, improves muscle cell viability and bone tissue microstructure, and reduces Cisplatin (HY-17394)-induced muscle toxicity and apoptosis. Ligandrol promotes muscle growth, protects bone structure, and has anti-diabetic, anti-apoptotic and antioxidant effects. Ligandrol can antagonize Streptozotocin (HY-13753) damage to pancreatic islets and improve the symptoms of type 2 diabetes .
1
1 Cited Publications
製品番号: HY-W017387
CAS 番号: 4502-00-5
別名: Sodium 4-methyl-2-oxopentanoate; 2-Ketoisocaproic acid sodium salt
研究分野:
Sodium α-ketoisocaproate (Sodium 4-methyl-2-oxopentanoate) is an insulin secretagogue. Sodium α-ketoisocaproate undergoes transamination catalyzed by BCAT and BCATm to produce α-ketoglutarate and leucine; it also binds to the SUR1 site to inhibit KATP channel activity, but does not directly affect the Kir6.2 subunit. Sodium α-ketoisocaproate regulates Ca 2+ influx. Sodium α-ketoisocaproate exerts insulinotropic activity in pancreatic islets and intact mouse pancreata with sufficient BCATm expression. Sodium α-ketoisocaproate can be used in research related to type 2 diabetes .
1
1 Cited Publications
Target:
研究分野:
FKGK18 is a selective group VIA calcium-independent phospholipase A2 (GVIA iPLA2) inhibitor. FKGK18 is a fluoroketone (FK)-based compound with IC50s of 50 nM and 3 μM for iPLA2β and iPLA2γ. FKGK18 can be used for the research of beta-cell apoptosis and diabetes .
Target:
研究分野:
GLP-1R agonist 2 (compound 2) is an effective GLP-1R agonist that exerts its activating effect by forming hydrogen bonds with the Tyr42, Cys71, and Ser84 residues of GLP-1R. GLP-1R agonist 2 has the potential for research in metabolic diseases such as type 2 diabetes and obesity .
Target:
WS6 is an IkB kinase and EBP1 inhibitor, with IC50 values of 0.24 nM, 0.21 nM, and 40.48 nM in MV4-11, MOLM13, and K562 cells, respectively. WS6 promotes the proliferation of alpha and beta cells in the pancreas, has antioxidant and anti-inflammatory activities, and can alleviate depression like behavior in rats [1][2][4].
Target:
研究分野:
Picolinamide (2-Picolinamide) is an inhibitor of Poly(ADP-ribose) synthetase of nuclei from rat pancreatic islet cells .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
