PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity[1].
α-L-Fucosidase (EC 3.2.1.51) is an enzyme that catalyzes the chemical reaction. Serum activity of α-L-fucosidase, a lysosomal enzyme present in all mammalian cells, has been proposed as a marker of hepatocellular carcinoma (HCC)[1].
JTC-017, a specific corticotropin-releasing hormone receptor 1 antagonist, attenuates hippocampal noradrenaline release, visceral perception, adrenocorticotropic hormone release, and anxiety after acute colorectal distention in rats. JTC-017 blocks stress-induced changes in colonic motility after chronic colorectal distention in rats[1].
Malate dehydrogenase catalyzes the mutual conversion of oxaloacetate and malate, and is associated with the oxidation/reduction of dinucleotide coenzymes[1].
Retinyl-β-D-glucoside is a naturally occurring and biologically active metabolites of vitamin A, which are found in fish and mammals.IC50 Value: Target: in vitro: Retinyl beta-D-glucoside is a substrate for two broad-specificity mammalian beta-glucosidases, namely the cytosolic and membrane-associated beta-glucosidases of guinea pig liver. However, retinyl beta-D-glucoside is not hydrolysed by placental glucocerebrosidase [1].in vivo: Depending on the mode of administration, retinyl beta-glucose, which is soluble in water, showed 67-100% of the growth-promoting activity of retinyl acetate in vitamin A-deficient rats. In metabolic studies on vitamin A-deficient rats, retinyl beta-glucose was rapidly hydrolyzed to retinol [2].
6β-Hydroxyipolamiide can be isolated from the methanolic extract of S. jamaicensis leaves. 6β-Hydroxyipolamiide has α-glucosidase inhibitory activity with an IC50 of 539.17 μg/mL[1].
AZD7687 is a potent and selective DGAT1 inhibitor with an IC50 value of 80 nM (hDGAT1).IC50 value: 80 nM [1]Target: DGAT1in vitro: Plasma AZD7687 exposure was measured repeatedly. Postprandial serum TAG excursion was measured during 8 h after a standardized mixed meal with fat energy content of 60% (SMM 60%; five cohorts, 1-20 mg), before (baseline) and after dosing, to assess effects on gut DGAT1 activity. AZD7687 markedly reduced postprandial TAG excursion with a steep concentration-effect relationship [2].in vivo: Multiple doses of AZD7687 (1, 2.5, 5, 10 and 20 mg/day, n=6 or n=12 for each) or placebo (n=20) were administered for 1 week. Dose-dependent reductions in postprandial serum TAG were demonstrated with AZD7687 doses ≥5mg compared with placebo (p<0.01). Significant (p<0.001) increases in plasma GLP-1 and PYY levels were seen at these doses, but no clear effect on gastric emptying was demonstrated at the end of treatment. With AZD7687 doses >5 mg/day, gastrointestinal (GI) side effects increased; 11/18 of these participants discontinued treatment owing to diarrhoea [3].
L-Ascorbic acid-d2 is the deuterium labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a colla
Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC50 of 2.27 mM[1], and also inhibits ACE-I activity[2]. Sinapinic acid posssess potent anti-tumor activity, induces apoptosis of tumor cells[1]. Sinapinic acid shows antioxidant and antidiabetic activities[2]. Sinapinic acid reduces total cholesterol, triglyceride, and HOMA-IR index, and also normalizes some serum parameters of antioxidative abilities and oxidative damage in ovariectomized rats[3].
Biotinylated sphingosine (Biotinyl-Sph) is a substrate of sphingosine kinase that can b used to detect the phosphorylation activity of sphingosine kinase 1 (SPHK1) and SPHK2[1].
(Glu20)-Glucagon (1-29) (human, rat, porcine) is the deamidation product of glucagon.
SLC26A3-IN-2 is an orally active inhibitor of anion exchanger protein SLC26A3 (IC50=360 nM). SLC26A3 belongs to solute carrier (SLC) proteins, and the SLC26 family. SLC26 family has broad anion specificity for chloride, bicarbonate, sulfate and oxalate. SLC26A3 down-regulates in adenoma, DRA, involves in in intestinal absorption of chloride and oxalate. The loss of SLC26A3 function mutations is associated with chloride-losing diarrhea[1].
2-γ-Linolenoyl-1,3-dilinoleoyl-sn-glycerol is a triglyceride.
CAY10789 (compound 6) is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist (IC50=2.80 μM) and GPBAR1 (G-protein-coupled bile acid receptor 1) agonist (EC50=3 μM). CAY10789 significantly reduces the adhesion of U937 cells to HAEC, reduces the expression of TNF-α. CAY10789 shows very promising metabolic stability and excellent pharmacokinetics. CAY10789 can be used for the research of colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases[1].
BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor (IC50=0.3 nM). BLU2864 shows anti-tumor activity. BLU2864 can be used in cancer and polycystic kidney disease research[1][2].
2,2-Dihydroxy-1-phenylethan-1-one (compound 2d) is an intermediate of pharmaceutical synthesis with antioxidant property[1].
Metformin D6 hydrochloride is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy[1].
H-Phe-Arg-OH is a dipeptide containing phenylalanine and arginine. H-Phe-Arg-OH can be separated from Bradykinin (HY-P0206) through Angiotensin-converting enzyme (ACE, HY-P2983). H-Phe-Arg-OH can be used for metabolic research[1].
Marstacimab (PF-06741086) is an anti-tissue factor pathway inhibitor (TFPI) monoclonal antibody. Marstacimab can be used for the research of hemophilia[1][2].
Butyl isobutyl phthalate is isolated from the rhizoid of Laminaria japonica. Butyl isobutyl phthalate is a non-competitive α-glucosidase inhibitor with an IC50 value of 38 μM. Butyl isobutyl phthalate shows a hypoglycemic effect and has the potential for diabetes treatment[1].
Glucagon receptor antagonists-2 is a highly potent glucagon receptor antagonist.
UDP-GlcNAc Disodium Salt is a donor substrate of O-GlcNAc transferase (OGT).
Magnoflorine chloride (Magnoflorine chloride), an aporphine alkaloid found in Acoruscalamus, reduces the formation of C. albicans biofilm[1]. Magnoflorine chloride has anti-fungal, anti-antidiabetic and anti-oxidative activity[2].
Andropanoside is a natural product isolated and purified from the herbs of Andrographis paniculata. Andrographis paniculata possesses a protective activity against various liver disorders[1].
AR-A014418-d3 (AR 0133418-d3) is the deuterium labeled AR-A014418. AR-A014418 is a potent, selective, and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM)[1].
Gymnestrogenin is a pentahydroxytriterpene from the leaves of Gymnema sylvestre R.Br[1]. Gymnestrogenin is a LXR antagonist with IC50s of 2.5 and 1.4 μM for LXRα and LXRβ transactivation, respectively. Gymnestrogenin reduces the transcriptional activity of LXR even on its own promoter, thus reducing the mRNA expression[2].
Carboxylesterases (CESs), namely carboxylate hydrolases, are widely distributed in nature, commonly found in mammalian liver, and often used in biochemical research. Carboxylesterase catalyzes the hydrolysis of a variety of endogenous and exogenous substrates, including esters, thioesters, carbamates, and amides, hydrolyzing carboxylic acid esters to the corresponding alcohols and carboxylic acids[1].
SR9238 is a synthetic LXR antagonist with IC50s of 214 nM and 43 nM for LXRα and LXRβ, respectively.
Pneumadin, rat (PNM) is a decapeptide, which possess a potent stimulating effect on arginine-vasopressin (AVP) release. Pneumadin, rat (PNM) exerts a marked antidiuretic effect in animals with functional AVP system[1][2].