5-Octyl hydrogen L-glutamate is cell-permeable molecule and can be used for synthesizing 5-octyl ester derivatives (5-octyl α-ketoglutarate)[1].
PF-249 is a potent, selective AMPK β1-containing complexes activator; increases the phosphorylation of the AMPK substrate ACC at S79 with EC50 of 296 nM, potently inhibits de novo lipogenesis (IC50=15 nM) in primary rat hepatocytes.
MK-3903 is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM.
Fmoc-Ala-OH-13C3 is a 13C-labeled Fmoc-leucine. 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-ind
Villocarine A is a natural vasorelaxant indole alkaloid[1].
L-Threonic acid magnesium salt is the enantiomer of Threonic acid and a metabolite of vitamin C. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent[1].
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].
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].
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].
Oxyntomodulin, a 37-amino acid peptide hormone, is a glucagon-like peptide 1 (GLP-1) receptor agonist[1].
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].
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].
Mebeverine metabolite O-desmethyl Mebeverine alcohol is a metabolite of Mebeverine, which is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract.
Syringic acid is correlated with high antioxidant activity and inhibition of LDL oxidation.
Pseudobaptigenin is a flavonoid. Pseudobaptigenin shows very good anticataract activity. Pseudobaptigenin has good binding affinity for the inhibition of glycation against γ-crystallin protein. Pseudobaptigenin also has good ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity) property[1].
Vildagliptin (LAF-237; NVP-LAF 237) inhibits DPP-4 with IC50 of 2.3 nM.IC50 Value: 2.3 nM[1]Target: DPP-4in vitro: Vildagliptin is an N-substituted glycyl-2-cyanopyrrolidine (figure 2). It is a potent competitive and reversible inhibitor of human and rodent DPP-4 in vitro, with a median inhibitory concentration (IC50) ~2-3 nmol/L. Importantly, vildagliptin inhibits DPP-4 with high specificity relative to other similar peptidases where its IC50 exceeds 200 mol/L [1].in vivo: Compared to age-, gender-, BMI-matched subjects with normal renal function, the mean AUC of vildagliptin after 14 days in patients with mild, moderate, and severe RI increased by 40%, 71%, and 100%, respectively [2]. The treatment was effective in modulating stress in pancreatic tissue, both by reducing levels of stress markers as well as by increasing activity of SOD and catalase. After analyzing the pancreatic histology, we found that vildagliptin was also able to preserve islets and pancreatic β-cells, especially at the concentration of 5 mg/kg [3].Clinical trial: FDA approved drug.
Clofarabine(Clolar; Clofarex) inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase.IC50 Value: 65 nMTarget: in vitro: Clofarabine is a second generation purine nucleoside analog with antineoplastic activity. It is phosphorylated intracellularly, which inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase, resulting in inhibition of DNA repair and synthesis of DNA and RNA. This nucleoside analog also disrupts mitochondrial function and membrane integrity, resulting in the release of pre-apoptotic factors, including cytochrome C and apoptotic-inducing factor, which activate apoptosis.in vivo: Clofarabine is used for treating relapsed or refractory acute lymphoblastic leukaemia (ALL) in children, after at least two other types of treatment have failed.
Cinnamyl Alcohol is an active component from chestnut flower, inhibits increased PPARγ expression, with anti-obesity activity[1].
SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.
β-Tocopherol-d3 is the deuterium labeled β-Tocopherol. β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol[1][2][3].
TGR5 Receptor Agonist 4 is an agonist of Bile Acid Receptor (TGR5), with EC50 for hTGR5 and mTGR5 of 2 nM and 3 nM, respectively. TGR5 Receptor Agonist plays important roles in hypoglycemic and weight loss[1].
Dihydrouracil-13C4,15N2 is the 13C and 15N labeled Dihydrouracil[1]. Dihydrouracil (5,6-Dihydrouracil), a metabolite of Uracil, can be used as a marker for identification of dihydropyrimidine dehydrogenase (DPD)-deficient[2][3].
Octapeptide-2 is a bioactive peptide with promotion of hair growth effect and has been reported used as a cosmetic ingredient[1].
PCSK9-IN-22 (compound 29) is an orally active inhibitor of PCSK9. PCSK9-IN-22 inhibits the interaction of the protein with LDLR in vivo[1].
Tyrphostin 8 is a tyrosine kinase, with an IC50 of 560 μM for EGFR kinase. Tyrphostin 8 is also a GTPase inhibitor. Tyrphostin 8 can inhibit the protein serine/threonine phosphatase calcineurin (IC50=21 μM)[1][2][3].
GCGR antagonist 2, a Furan-2-carbohydrazide, is an orally active glucagon receptor antagonist. GCGR antagonist 2 binds to hGluR with an Kd value of 2.3 nM, and inhibits rat receptor with an IC50 value of 0.43 nM. GCGR antagonist 2 inhibits glucagon-stimulated glycogenolysis[1][2].
L162441 is an Angiotensin type 1 receptor antagonist.
m-Anisaldehyde is an endogenous metabolite.
S-(2,4-Dinitrophenyl)glutathione is a substrate for glutathione-S-transferase. (2,4-Dinitrophenyl)glutathione can be used as an irreversible glutathione reductase inhibitor with an Ki value of 30 µM[1][2].
Gentianine, an active metabolite of Swertiamarin, has anti-diabetic effect and anti-inflammatory property[1][2].