Pirenoxine (Catalin K) is a potent antioxidant. Pirenoxine shows anti-presbyopic activity. Pirenoxine has the potential for the research of cataracts[1][2].
3-Indolepropionic acid is shown to be a powerful antioxidant and has potential in the treatment for Alzheimer’s disease.
ADAMTS-5-IN-3 (Example 37-2) is a potent inhibitor of ADAMTS-5 and ADAMTS-4 with IC50s of 8 and 12 nM, respectively. ADAMTS-5-IN-3 can be used for the research of diseases involving degradation of cartilage or disruption of cartilage homeostasis, in particular osteoarthrosis and/or rheumatoid arthritis[1].
Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist developed for treatment of type 2 diabetes, with an EC50 value of 0.06 nM.
(-)-Gallocatechin, an epimer of (-)-Epigallocatechin (EGC), is contained in various tea products. (-)-Gallocatechin has antioxidant activities[1][2][3].
(Rac)-Sitagliptin is an isoform of Sitagliptin (HY-13749), which is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts[1].
Lithocholic acid-d5 is deuterium labeled Lithocholic acid.
Bisacodyl is a stimulant laxative drug that works directly on the colon to produce a bowel movement.Target: OthersBisacodyl is an organic compound that is used as a stimulant laxative drug. Bisacodyl (20 mg/kg) results in a decrease in AQP3 protein expression and increased mRNA expression level of TNF-α in the colon of rats [1]. Bisacodyl inhibits water absorption in rat jejunum, ileum, and colon, the degree of inhibition is linearly related to the logarithm of the bisacodyl concentration over the range of 0.05 mg to 2.0 mg per 100 mL [2]. Bisacodyl (10 mg/kg, intragastrically) induces a significant decrease in jejunal NOS activity in rats. Bisacodyl (10 mg/kg, intragastrically) increases the distance traveled by the marker in all time periods [3]. Bisacodyl (5.9 mg/kg) decreases significantly jejunal and colonic (Na + K) ATPase activity as compared to saline-treated rats. Bisacodyl (5.9 mg/kg) increases significantly jejunal and colonic PGE2 content and stimulates jejunal and colonic adenyl cyclase activity as compared to those in control rats without affecting cAMP content [4]. Bisacodyl (4.3 mg/kg) coupled with AOM increases the number of crypt per focus, but not the number of tumors in rats. Bisacodyl (43 mg/kg) significantly increases the number of crypt per focus and tumors in rats [5].
Imiloxan hydrochloride is a potent and selective alpha 2B-adrenoceptor antagonist. Imiloxan hydrochloride has the potential for acute kidney injury research[1][2].
Desmosterol is a molecule similar to cholesterol. Desmosterol is the immediate precursor of cholesterol in the Bloch pathway of cholesterol biosynthesis. Desmosterol, as an endogenous metabolite, used to study cholesterol metabolism[1].
Glipizide(K 4024; CP 2872) is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes.Target: Potassium ChannelGlipizide is an oral rapid- and short-acting anti-diabetic drug from the sulfonylurea class. It is classified as a second generation sulfonylurea, which means that it undergoes enterohepatic circulation. Mechanism of action is produced by blocking potassium channels in the beta cells of the islets of Langerhans. By partially blocking the potassium channels, the cell remains depolarized, increasing the time the cell spends in the calcium release stage, which results in signaling leading to calcium influx. The increase in calcium will initiate more insulin release from each beta cell. Sulfonylureas may also cause the decrease of serum glucagon and potentiate the action of insulin at the extrapancreatic tissues [1, 2].
S-Methyl-L-cysteine is a natural product that acts as a substrate in the catalytic antioxidant system mediated by methionine sulfoxide reductase A (MSRA), with antioxidative, neuroprotective, and anti-obesity activities.
Exendin-4, a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM. Sequence: His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2.
IDD388 is a potent aldose reductase (ALR2 or AKR1B1) inhibitor with IC50 of 0.4 uM, shows weak inhibition for AKR1B10 (IC50=4.4 uM).
PF-04937319 is a glucokinase activator (GKA) with EC50 value of 154.4 μM, one of the most promising strategies for the treatment of type 2 diabetes mellitus[1].PF-04937319 is designed to maintain glucose-lowering efficacy while mitigating the risk of hypoglycaemia observed with many other GKAs[2].
2-Methylbenzoxazole is an endogenous metabolite.
11-epi-mogroside V is a mogroside in the fruit of Siraitia grosvenori. 11-epi-mogroside V exhibits considerable bioactivity in promoting glucose uptake in human HepG2 cells in vitro [1].
DL-3-Hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) disodium is a disodium salt compound of HMG-CoA, is a intermediate of terpenes and ketone bodies. DL-3-Hydroxy-3-methylglutaryl coenzyme A disodium also involves in ester metabolism in vivo, as a precursor for cholesterol synthesis, and regulates cholesterol synthesis by coupling LDL receptor[1][2].
Sulfobromophthalein (Bromosulfophthalein) disodium salt is an organic anion dye used in the study of a variety of membrane carriers expressed in animal tissues and involved in transport of drugs and metabolites[1].
Fluazifop-P-butyl, a graminicide from arylophenoxypropionate group, is a acetyl-CoA carboxylase (ACCase) inhibitor[1].
Dextrose, a simple sugar (monosaccharide), is an important carbohydrate in biology.Target: OthersDextrose(D-glucose), a simple sugar (monosaccharide), is an important carbohydrate in biology.
Citric acid monohydrate is a natural preservative and food tartness enhancer. Citric acid monohydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid monohydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid monohydrate causes renal toxicity in mice[1][2][3].
LY2452473 is an orally bioavailable, selective androgen receptor modulator (SARM).
Cytisine is an alkaloid that occurs naturally in several plant genera, such as Laburnum and Cytisus. Cytisine is a partial agonist of α4β2 nAChRs[1], and partial to full agonist at β4 containing receptors and α7 receptors[2]. has been used medically to help with smoking cessation[3].
Insulin peglispro (BIL) is a basal insulin with a flat, prolonged activity profile. Insulin peglispro can exhibit better glycaemic control compared to conventional insulins[1].
C12-Ceramide (N-Lauroyl-D-erythro-sphingosine), a naturally occurring ceramide, is formed by hydrolysis of C12 sphingomyelin. C12-Ceramide can enhance the Doxorubicin toxicity in MDA-MB-231 cells. C12-Ceramide also can be used to diagnose types A and B Niemann-Pick disease[1][1].
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM[1].
D-Glucose-13C-1 (Glucose-13C-1) is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Nordeprenyl is the metabolite of Deprenyl. Deprenyl is a potent, selective and irreversible inhibitor of MAO-B[1].
Diphenyl Phosphate-d10 (DPhP-d10) is the deuterium labled Diphenyl Phosphate (HY-W008151). Diphenyl Phosphate inhibits growth and energy metabolism of zebrafish in a sex-specific manner.