Enteropeptidase (TMPRSS15), a type II transmembrane serine protease and a physiological activator of trypsinogen. Enteropeptidase is associated with the brush border membrane (BBM) of the enterocytes in the upper small intestine. Trypsinogen is the primary substrate for Enteropeptidase. Enteropeptidase is involved in digestion in humans and animals[1].
GLP-1R agonist 10 (Compound 109a) is a GLP-1 agonist with an EC50 of 0.051 nM[1].
Katacalcin is a second potent plasma calcium-lowering peptide.
Myristoyl tetrapeptide-12 directly activates SMAD2 and induces the linking of SMAD3 with DNA. Myristoyl tetrapeptide-12 is capable of stimulating hair growth, especially at the level of eyelashes[1][2].
Gemigliptin tartrate (LC15-0444 tartrate) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin tartrate exhibits potent anti-glycation properties. Gemigliptin tartrate can be used for the research of advanced glycation end products (AGE)-related diabetic complications[1][2].
Cotrimoxazole (Trimethoprim/sulfamethoxazole 1:19), an antimicrobial agent, is a Trimethoprim and Sulfamethoxazole mixture. The ratio of Trimethoprim to Sulfamethoxazole in the combination mixture is 1 : 19[1].
FATP1-IN-2, as an arylpiperazine derivative, is an orally active fatty acid transport protein 1 (FATP1) inhibitor (human IC50=0.43 μM, mouse IC50=0.39 μM)[1].
Lucerastat, the galactose form of Miglustat, is an orally-available inhibitor of glucosylceramide synthase (GCS). Lucerastat has the potential for Fabry disease study[1][2].
Human enteropeptidase-IN-1 (compound 6b) is a highly potent, orally active and low systemic exposure enteropeptidase inhibitor. Human enteropeptidase-IN-1 boosts the increase in fecal protein output, and exhibits potent body weight loss in diet-induced obese (DIO) rat model. Human enteropeptidase-IN-1 can be used for anti-obesity research[1].
Zingerone (Vanillylacetone) is a nontoxic methoxyphenol isolated from Zingiber officinale, with potent anti-inflammatory, antidiabetic, antilipolytic, antidiarrhoeic, antispasmodic and anti-tumor[3] properties[1]. Zingerone alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways[2]. Zingerone acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells[3].
Tofogliflozin(CSG-452) is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2.IC50 value: 2.9/14.9/6.4 nM(human/rat/mouse SGLT2) [1]Target: SGLT2 inhibitorin vitro: Tofogliflozin competitively inhibited SGLT2 in cells overexpressing SGLT2, and K(i) values for human, rat, and mouse SGLT2 inhibition were 2.9, 14.9, and 6.4 nM, respectively. The selectivity of tofogliflozin toward human SGLT2 versus human SGLT1, SGLT6, and sodium/myo-inositol transporter 1 was the highest among the tested SGLT2 inhibitors under clinical development [1]. tofogliflozin was catalyzed to the primary hydroxylated derivative (M4) by CYP2C18, CYP4A11 and CYP4F3B, then M4 was oxidized to M1. 3. Tofogliflozin had no induction potential on CYP1A2 and CYP3A4 [4].in vivo: A single oral gavage of tofogliflozin increased renal glucose clearance and lowered the blood glucose level in Zucker diabetic fatty rats. Tofogliflozin also improved postprandial glucose excursion in a meal tolerance test with GK rats. In db/db mice, 4-week tofogliflozin treatment reduced glycated hemoglobin and improved glucose tolerance in the oral glucose tolerance test 4 days after the final administration [1]. Tofogliflozin (400 ng/ml) induced UGE of about 2 mg·kg?1·min?1 and increased EGP by 1-2 mg·kg?1·min?1, resulting in PG in the normal range [2]. Tofogliflozin suppressed plasma glucose and glycated Hb and preserved pancreatic beta-cell mass and plasma insulin levels. No improvement of glycaemic conditions or insulin level was observed with losartan treatment [3].
H-Abu-OH, one of the three isomers of aminobutyric acid, is elevated in the plasma of children with with Reye's syndrome, tyrosinemia, homocystinuria, nonketotic hyperglycinemia, and ornithine transcarbamylase deficiency.
Nomilin is a limonoid compound obtained from the extracts of citrus fruits. Nomilin is an anti-obesity and anti-hyperglycemic agent [1][2].
Tyrosine decarboxylase (TDC; TyrDC) widely exists in plants, insects and different microorganisms, and is often used in biochemical research. Tyrosine decarboxylase is a pyridoxal 5'-phosphate (PLP)-dependent decarboxylase that catalyzes the removal of carboxyl groups from tyrosine to produce tyramine and carbon dioxide[1].
ALDH1A1-IN-3 (compound 57) is an excellent and selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitor with an IC50 value of 0.379 μM. ALDH1A1-IN-3 can effectively improve glucose consumption in HepG2 cells. ALDH1A1-IN-3 can be used for researching glucose metabolism improvement[1].
Oxyntomodulin, a 37-amino acid peptide hormone, is a glucagon-like peptide 1 (GLP-1) receptor agonist[1].
Furosemide (Lasix) is a loop diuretic inhibitor of Na+/2Cl-/K+ (NKCC) cotransporter of which used in the treatment of congestive heart failure and edema.Target: NKCC Furosemide (INN/BAN) or frusemide is a loop diuretic used in the treatment of congestive heart failure and edema. It is most commonly marketed by Sanofi under the brand name Lasix, and also under the brand names Fusid and Frumex. It has also been used to prevent Thoroughbred and Standardbred race horses from bleeding through the nose during races.Along with some other diuretics, furosemide is also included on the World Anti-Doping Agency's banned drug list due to its alleged use as a masking agent for other drugs.Furosemide, like other loop diuretics, acts by inhibiting NKCC2, the luminal Na-K-2Cl symporter in the thick ascending limb of the loop of Henle. The action on the distal tubules is independent of any inhibitory effect on carbonic anhydrase or aldosterone; it also abolishes the corticomedullary osmotic gradient and blocks negative, as well as positive, free water clearance.Because of the large NaCl absorptive capacity of the loop of Henle, diuresis is not limited by development of acidosis, as it is with the carbonic anhydrase inhibitors. Additionally, furosemide is a noncompetitive subtype-specific blocker of GABA-A receptors. Furosemide has been reported to reversibly antagonize GABA-evoked currents of α6β2γ2 receptors at uM concentrations, but not α1β2γ2 receptors. During development, the α6β2γ2 receptor increases in expression in cerebellar granule neurons, corresponding to increased sensitivity to furosemide
4-(Dimethylamino)phenol increases the extracellular lactate dehydrogenase (LDH) without markedly affecting gluconeogenesis. 4-(Dimethylamino)phenol cannot decreases the ATP content until the membrane becomes permeable to LDH[1].
LY255582 is a pan-opioid antagonist and has high affinity for mu, delta, and kappa receptors (Ki: 0.4 nM, 5.2, 2.0 nM respectively). LY255582 can decrease food intake and body weight. LY255582 can be used for the research of obesity[1][2][3][4].
Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity[1].
Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM.
Kuromanin (chloride), extracted from mulberry leaves, has been shown to improve blood glucose concentrations and lipid homeostasis and to reduce obesity.
pTH-Related Protein (1-34) amide (human, mouse, rat) (Human PTHrP-(1-34)NH2) is a N-terminal fragments of PTHrP. pTH-Related Protein (1-34) amide (human, mouse, rat) induces hypercalcemia, and can be used for research of humoral hypercalcaemia of malignancy[1].
Carbutamide (BZ-55) is an orally active and first-generation sulfonylurea with hypoglycemic activity[1].
TM-25659 is a TAZ modulator. Anti-osteoporotic and anti-obesity activities[1].
BRD3308 is a potent, selective HDAC3 inhibitor with IC50 of 54 nM, displays >20-fold selectivity over HDAC1 and HDAC2, >500-fold selectivity over other HDAC isoforms; attenuates PE-mediated phosphorylation of ERK, but not JNK; also activates HIV-1 transcription in the 2D10 cell line, induces outgrowth of HIV-1 from resting CD4+ T cells isolated from antiretroviral-treated, aviremic HIV+ patients ex vivo and disrupts HIV-1 latency; suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release.
APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively..IC50 value: 2.7 nM (EC50) [1]Target: GPR119Chronic treatment withAPD668 showed for the first time that blood glucose and glycated hemoglobin (HbA1c) levels could be significantly reduced in Zucker Diabetic Fatty (ZDF) rats over several weeks of dosing. APD668 was the ?rst compound with thismechanism of action to be progressed into clinical development for the treatment of diabetes.
Lathosterol is a cholesterol-like molecule. Serum Lathosterol concentration is an indicator of whole-body cholesterol synthesis.
2-Hydroxy-2-methylbutanoic acid, an unusual metabolite, is associated with 2-hydroxyglutaric aciduria and maple syrup urine disease.
Triacylglycerol lipase is an enzyme that preferentially hydrolyzes the outer links of triacylglycerols and acts only on the water-lipid interface. Pancreatic triacylglycerol lipase is the single most important determinant of lipid absorption[1].