OSMI-3 (Compound 2b) is a potent, long-lasting, and cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-3 increases detained intron splicing in cells[1].
BI-2081 is a GPR40 (FFAR1) partial agonist (EC50: 4 nM). BI-2081 induces glucose depending insulin secretion and reduces the plasma glucose concentration. BI-2081 can be used in the research of metabolic diseases, in particular diabetes type 2[1].
4-Chloro-3,5-dimethylphenoxyacetic acid (compound 602 UC) is a product of masked amide bond hydrolysis of auxin analog 602 (compound 602).602 can effectively stimulate hypocotyl growth in wild-type seedlings[1].
Emodin-1-O-β-gentiobioside is an anthraquinone[1][2].
L-Homocystine is the oxidized member of the L-homocysteine. Homocysteine is a pro-thrombotic factor, vasodilation impairing agent, pro-inflammatory factor and endoplasmatic reticulum-stress inducer used to study cardiovascular disease mechanisms.
L-Phenylalanine-3-13C ((S)-2-Amino-3-phenylpropionic acid-3-13C) is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
Valienamine is the alpha-glucosidase inhibitor. Valienamine is the key functional component of many natural glycosidase inhibitors including the crop protectant validamycin A and the antidiabetic agent acarbose[1].
Rosuvastatin Calcium is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM. IC50 Value: 11 nM [1]Target: HMG-CoA reductasein vitro: Rosuvastatin is relatively hydrophilic and is highly selective for hepatic cells; its uptake is mediated by the liver-specific organic anion transporter OATP-C. Rosuvastatin is a high-affinity substrate for OATP-C with apparent association constant of 8.5 μM [2]. Rosuvastatin inhibits cholesterol biosynthesis in rat liver isolated hepatocytes with IC50 of 1.12 nM. Rosuvastatin causes approximately 10 times greater increase of mRNA of LDL receptors than pravastatin [1]. Rosuvastatin (100 μM) decreases the extent of U937 adhesion to TNF-α-stimulated HUVEC. Rosuvastatin inhibits the expressions of ICAM-1, MCP-1, IL-8, IL-6, and COX-2 mRNA and protein levels through inhibition of c-Jun N-terminal kinase and nuclear factor-kB in endothelial cells [3].in vivo: Rosuvastatin (3 mg/kg) daily administration for 14 days decreases plasma cholesterol levels by 26% in male beagle dogs with normal cholesterol levels. In cynomolgus monkeys, Rosuvastatin decreases plasma cholesterol levels by 22% [1]. Rosuvastatin (20 mg/kg/day) administration for 2 weeks, significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin [4]. Rosuvastatin shows antiatherothromhotic effects in vivo. Rosuvastatin (1.25 mg/kg) significantly inhibits thrombin-induced transmigration of monocvtes across mesenteric venules via inhibition of the endothelial cell surface expression of P-selectin, and increases the basal rate of nitric oxide in aortic segments by 2-fold times [5].
Phenoxyacetic acid is an endogenous metabolite.
Kuwanon A is a flavone derivative isolated from the root barks of the mulberry tree (Morus alba L.); inhibits nitric oxide production with an IC50 of 10.5 μM.
STO-609 is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively.
Crovalimab (SKY59; RO7112689) is a novel humanized antibody against C5 in a pH-dependent manner with KDs of 15.2 nM and 16.8 μM at pH 7.4 and 5.8, respectively. Crovalimab binds human FcRn with great affinity (KD: 17 μM at pH 6.0). Crovalimab can block cleavage of C5 by the C5 convertase and inhibite the activity of a C5 variant (p.Arg885His). Crovalimab inhibits C5b-9 formation significantly in all three complement pathways, the classical pathway (CP), lectin pathway (LP), and alternative pathway (AP). Crovalimab has the potential for paroxysmal nocturnal hemoglobinuria (PNH) and complement-mediated diseases research[1][2].
Nicotinic acid riboside is a NAD+ precursor in human cells. Nicotinic acid riboside is an authentic intermediate of human NAD+ metabolism[1][2].
trans-trans-Muconic acid is a urinary metabolite of benzene and has been used as a biomarker of exposure to benzene in humans
1-Hydroxypyrene-d9 is the deuterium labeled 1-Hydroxypyrene[1]. 1-Hydroxypyrene, a biomarker of exposure to polycyclic aromatic hydrocarbons (PAHs), is analyzed in urine samples. 1-Hydroxypyrene is the major biomarker of exposure to pyrenes[2].
Luteinizing Hormone Releasing Hormone (LH-RH), salmon is the hypophysiotropic decapeptide synthesized in the hypothalamus that plays a crucial role in the control of reproductive functions.
CL316243 is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors[1].CL316243 is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate[2]. CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence[3].
L-Tartaric acid (L-(+)-Tartaric acid) diammonium is an endogenous metabolite. L-Tartaric acid diammonium is the primary nonfermentable soluble acid in grapes and the principal acid in wine. L-Tartaric acid diammonium can be used as a flavorant and antioxidant for a range of foods and beverages[1].
Quercetin 3-(6″-caffeoylsophoroside) is an orally active α-amylase inhibitor, with an IC50 of 73.66 μg/mL. Quercetin 3-(6″-caffeoylsophoroside) presents in thehydro-methanolic extract of Cardamine hirsuta Linn. Quercetin 3-(6″-caffeoylsophoroside) shows the antidiabetic activities by oxidative stress reduction and α-amylase inhibition. Quercetin 3-(6″-caffeoylsophoroside) can be used for diabetes mellitus research[1].
Syringic acid-d6 is the deuterium labeled Syringic acid[1]. Syringic acid is correlated with high antioxidant activity and inhibition of LDL oxidation[2][3].
(-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a Ki of 0.73 nM.
PI3Kγ inhibitor 3 is a potent and remarkably selective PI3Kγ inhibitor with pIC50s of 9.1, 5.1, <4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively[1].
2-Acetonaphthone is an endogenous metabolite.
JNJ-40355003 is a potent and selective atty acid amide hydrolase (FAAH) inhibitor[1].
Amylin (1-37) (human) (hIAPP (1-37)) is a peptide hormone, present in pancreatic betacell secretory granules. The C-terminus of Amylin (1-37) (human) is amidated and there is a disulfide bond between cysteine residues 2 and 7[1].
T-863(DGAT-1 inhibitor) is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells.IC50 value:Target: DGAT1T863 causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.
S-(5'-Adenosyl)-L-methionine iodide (S-Adenosyl-L-methionine iodide) is an important methyl donor that is found in all living organisms[1].
Xanthine oxidoreductase-IN-2 (Compound IVa) is a xanthine oxidoreductase (XOR) inhibitor with the IC50 of 7.2 nM. Xanthine oxidoreductase-IN-2 shows hypouricemic effects in mice[1].
Adenosylcobalamin (Coenzyme B12;Cobamamide;AdoCbl) is an active form of Vitamin B12 which is a cofactor for methylmalonyl CoA mutase[1]
Masoprocol (meso-Nordihydroguaiaretic acid) is a potent and orally active lipoxygenase inhibitor. Masoprocol shows antihyperglycemic activity. Masoprocol decreases the glucose concentration and hepatic triglyceride in vivo. Masoprocol has the potential for the research of type II diabetes[1][2][3].