glucose tolerance

CCG-1423, a selective RhoA pathway inhibitor, suppresses SRF-mediated transcription.

AMPK activator 4 is a potent and selective AMPK activator that does not inhibit mitochondrial complex I. It selectively activates AMPK in muscle tissue, dose-dependently improves glucose tolerance in normal mice, significantly reduces fasting glucose levels, and improves insulin resistance in db/db diabetic mice. [AMPK activator 4 has hypoglycemic effects.]

Phanginin A, a natural product discovered in Caesalpinia sappan Linn, activates SIK1 and inhibits gluconeogenesis in mouse primary hepatocytes. Phanginin A increases PDE4 activity and suppresses the hepatic cAMP/PKA/CREB pathway, improving metabolic disorders in ob/ob mice. It may be used in studies of type 2 diabetes.

trans-Cinnamic acid (Myricitrine) exerts anti-diabetic activity by improving glucose tolerance in vivo and by stimulating insulin secretion in vitro.

Oxfenicine (4-Hydroxy-L-phenylglycine) is a carnitine palmitoyltransferase-1 inhibitor. Oxfenicine improves whole-body glucose tolerance and insulin sensitivity in high-fat diet-induced obese mouse with insulin resistance.

HWL-088 is a potent free fatty acid receptor 1 (FFA1/GPR40) agonist. HWL-088 significantly improves glucose tolerance in normal and diabetic models.

KPLH1130, a specific pyruvate dehydrogenase kinase (PDK) inhibitor, enhances glucose tolerance in mice fed a high-fat diet (HFD). It effectively hinders macrophage polarization and mitigates proinflammatory reactions.

PF-5006739 is an effective and selective inhibitor of CK1δ/ε (IC50s: 3.9 nM and 17.0 nM, respectively). PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selecti

SX29 is a non-competitive α-glucosidase inhibitor with oral activity, exhibiting an IC50 of 2.12 μM. It possesses hypoglycemic properties; oral administration of SX29 reduces blood glucose levels and enhances glucose tolerance in diabetic mice.

YH18968, a GPR119 agonist, improves glucose tolerance and enhances blood glucose-lowering effects. When combined with dipeptidyl peptidase-4 (DPP-4) inhibitors, YH18968 increases the plasma levels of active GLP-1 in normal mice.

KOTX1 is an orally active and selective inhibitor of ALDH1A3. In a diabetic mouse model, KOTX1 improves glucose tolerance, insulin secretion, and blood glucose levels.

α-Glucosidase-IN-77 (Compound H7) is a non-competitive α-glucosidase inhibitor with an IC50 of 1.25 μM. It reduces blood glucose levels, improves glucose tolerance, regulates gut microbiota, and exhibits hepatoprotective effects in a mouse model of type 2 diabetes.

PPARγmodulator-2 (Compound (R)-2n) is a reversible modulator of PPARγ, inhibiting the PPARγ ligand-binding domain (LBD) with an IC50 of 41 nM. It helps lower blood glucose levels, improves glucose tolerance and insulin sensitivity, and demonstrates antidiabetic activity in db/db mouse models.

α-Glucosidase-IN-86 (Compound A4) is an orally active α-glucosidase inhibitor with an IC50 of 2.72 μM. In mice, it demonstrates high safety and effectively reduces fasting blood glucose levels, improves glucose tolerance, regulates blood lipids, and exhibits antioxidant properties in diabetic models. α-Glucosidase-IN-86 is suitable for diabetes research.

GLP-1R agonist 30 is an orally active, selective GLP-1R agonist with an EC50 of 0.048 nM. It exhibits outstanding selectivity, with EC50 values exceeding 20 μM for GLP-2R, GIPR, and GCPR. GLP-1R agonist 30 significantly enhances cAMP stimulation and reduces hERG inhibition. The compound has good absorption and excellent β-arrestin pathway selectivity. Additionally, GLP-1R agonist 30 improves glucose tolerance and promotes insulin secretion in B-hGLP1R gene knock-in mice.

ZP3022 is a dual agonist targeting the glucagon-like peptide 1 receptor (GLP-1R) and cholecystokinin 2 (CCK2) receptor. It selectively enhances cAMP accumulation or ERK phosphorylation in HEK293 cells with GLP-1R or CCK2 receptor expression, compared to ERK phosphorylation in cells with the CCK1 receptor (EC50s: 0.02, 10.3, and >1,000 nM for human receptors, respectively). At 40 nM, ZP3022 promotes proliferation of rat neonatal β-cells in vitro. It also boosts glucose-induced insulin secretion (GSIS) in rat pancreatic islets at 10 and 100 nM concentrations and decreases body weight in rats at 40 nmol/kg doses twice daily. Administered at 100 nmol/kg daily, ZP3022 enhances β-cell and total pancreatic mass and improves glucose tolerance in db/db mice, while reducing food intake but not body weight in these mice.

Tryptophan-cholic acid (Trp-CA) is a microbial amino acid-binding bile acid (MABA), serving as an endogenous ligand and agonist for MRGPRE (Mas-related GPCR family member E), thereby inducing GLP-1 secretion. Tryptophan-cholic acid improves glucose tolerance in diabetic mice and may be utilised for studies on type 2 diabetes.

α-Glucosidase-IN-49 (compound C23) is a potent inhibitor of α-Glucosidase, with an IC50 of 0.52 μM. This compound exhibits oral bioactivity, effectively lowering blood glucose levels and enhancing glucose tolerance in mice.

ZLN005 (hydrochloride) is an activator of the peroxisome proliferator-activated receptor-gamma coactivator 1-alpha (PGC-1α). It enhances the expression of PGC-1α and downstream genes in skeletal muscle cells, leading to improved glucose utilization and fatty acid oxidation. In diabetic db/db mice, ZLN005 (hydrochloride) elevates the transcription of PGC-1α and downstream genes in skeletal muscle, boosts fat oxidation, and enhances glucose tolerance, pyruvate tolerance, and insulin sensitivity.

LCZ960 is an orally active glucokinase (GK) activator that stimulates GK activity in liver cells in vitro and enhances glucose uptake in vivo by activating hepatic GK. It effectively lowers blood glucose levels in diet-induced obesity (DIO) in mice. LCZ960 maintains normal blood sugar and improves glucose tolerance in DIO mice and rats. Additionally, LCZ960 stimulates glycogen synthase flux and increases glycogen turnover in the liver of rats, inducing an increase in hepatic glycogen cycling. This compound is useful for research on obesity and type 2 diabetes induced by high-fat diets.

Linogliride is a guanidine-based inhibitor of insulin secretion and a structural analog of pirogliride with hypoglycemic activity. It blocks ATP-sensitive potassium channels in the pancreatic beta cell membrane, thereby stimulating insulin secretion and improving glucose tolerance.

Linogliride fumarate is the fumarate salt of Linogliride. Linogliride is a guanidine-based inhibitor of insulin secretion and a structural analog of pirogliride with hypoglycemic activity. It blocks ATP-sensitive potassium channels in the pancreatic beta cell membrane, thereby stimulating insulin secretion and improving glucose tolerance.

SIRT6-IN-1, a novel SIRT6 inhibitor, reduces glycemia and improves oral glucose tolerance in unfed wild-type mice.

WB403 is a TGR5 activator. WB403 significantly decreases fasting blood glucose, postprandial blood glucose and HbA1c, improves glucose tolerance in type 2 diabetic mice. WB403 increases pancreatic β-cells and restores the normal distribution pattern of α-