Acotiamide hydrochloride is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC50 of 1.79 μM. Acotiamide hydrochloride can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide hydrochloride has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory[1][2][3].
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].
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].
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].
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].
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].
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.
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.
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].
SB756050 is a selective TGR5 agonist currently in phase 1clinical trials for the treatment of type 2 diabetes.
4-Prenyloxyresveratrol, an oxyresveratrol derivative, shows potent tyrosinase inhibitory activity with an IC50 of 0.90 μM[1].
SAR629 is a potent monoglyceride lipase (MGL) covalent inhibitor. SAR629 also inhibits 2-Arachidonoylglycerol (2-AG) degradation[1][2].
15-PGDH-IN-1 is a potent and orally active 15-PGDH inhibitior. 15-PGDH-IN-1 has inhibition activity against recombinant human 15-PGDH with an IC50 value of 3 nM. 15-PGDH-IN-1 can be used for the research of tissue repair and regeneration[1].
Pirinixil is a hypolipidemic agent of low toxicity.
(±)-Abscisic acid is an orally active plant hormone that is present also in animals. (±)-Abscisic acid (ABA) contributes to the regulation of glycemia in mammals[1].
Bocidelpar is a modulator of peroxisome proliferator-activated receptor delta (PPAR-δ). Bocidelpar improves mitochondrial biogenesis and function in Duchenne Muscular Dystrophy (DMD) muscle cells (extracted from patent WO2017062468A1, compound 2b)[1].
Retinol, also known as Vitamin A1, has pleiotropic functions including vison, immunity, hematopoiesis, reproduction, cell differentiation/growth, and development.
Sodium Picosulfate inhibits absorption of water and electrolytes, and increases their secretion.Target: OthersSodium Picosulfate displays cytotoxic effects on cultured liver cells. 800 and 1600 mg/mL induces dose-dependently vacuolic and fatty change as well as necrosis combined with a lowered mitotic activity and a slight increase in LDH values of the rapidly growing cultured liver cells of rabbit. Comparable but less severe effects are observed in 4-day old liver cell cultures of rat, while liver cells cultured for 6 to 11 days tolerate 1600 mg/mL Sodium Picosulfate. In human liver cultures the number of cells is slightly lowered at 800 and 1600 mg/mL and the number of nuclei in division is decreased dependent on dose [1]. Sodium Picosulphate has no major influence on ileal and colonic epithelial cell proliferation. In a 12 weeks study, 10 mg/kg Sodium Picosulphate continuously treatment does not influence the labeling index of Brdu (LI) in the ileum and induces no statistically significant increase of the LI when the treated groups are compared with the control group. The proliferative pattern along the crypts remains unchanged with sodium picosulphate treatment throughout the study [2]. Sodium Picosulphate does not induce chronic changes in colonic motility in rats under long-term treatment. 10mg/kg/day Sodium Picosulphate pretreated for 23 weeks does not induce any significant change in the duration of long spike bursts (LSB) which are associated with phasic contractions, or in LSB frequency in the fasted state or after a 3-gram meal [3].
Toltrazuril sulfoxide is a short-lived intermediary metabolite of Toltrazuril (HY-B0175), and then can be metabolized to the reactive toltrazuril sulfone (TZR-SO2) in vivo. Toltrazuril is an antiprotozoal agent that acts upon Coccidia parasites[1].
L-Ornithine-15N2 hydrochloride is the 15N-labeled L-Ornithine hydrochloride. L-Ornithine hydrochloride is a free amino acid that plays a central role in the urea cycle and is also important for the disposal of excess nitrogen.
L-Homoarginine-13C7,15N4 hydrochloride is the 13C- and 15N-labeled H-HomoArg-OH.HCl. H-HomoArg-OH.HCl is an endogenous metabolite.
Suberylglycine is an acyl glycine, which is a normally minor metabolite of fatty acid.
L-ascorbic acid 2-phosphate (2-Phospho-L-ascorbic acid) magnesium hydrate is a long-acting vitamin C derivative that can stimulate collagen formation and expression. L-ascorbic acid 2-phosphate magnesium hydrate can be used as a culture medium supplement for the osteogenic differentiation of human adipose stem cells (hASCs). L-ascorbic acid 2-phosphate magnesium hydrate increases alkaline phosphatase (ALP) activity and expression of runx2A in hASCs during the osteogenic differentiation[1][2][3].
des-Gln14-Ghrelin is a second endogenous ligand for the growth hormone secretagogue receptor. a). des-Gln14-ghrelin potently induces increases in [Ca2+]i in CHO-GHSR62 cells, with an EC50 of 2.4 nM[1].