Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect[1][2][3][4][5][6][7].
Ongericimab (JS002) is a humanized anti-PCSK9 monoclonal antibody. Ongericimab has lipid-lowering efficacy. Ongericimab can be used in research of hypercholesteremia and hyperlipidemia[1].
FKGK18 (FKGK18) is a potent, selective inhibitor of iPLA2 (group VIA Ca2+-independent phospholipase A2) with IC50 of 50 nM; displays 195 and >455 times more potent for GVIA iPLA(2) than for GIVA cPLA(2) and GV sPLA(2); inhibits Ca2+-independent PLA2 activity in a concentration-dependent manner, similar to S-BEL, which preferentially inhibits cytosol-associated iPLA2β; FKGK18 a valuable tool to explore the role of GVIA iPLA(2) in cells and in vivo models.
Caprooyl-tetrapeptide-3 acetate is used for fine lines and wrinkle reduction. Caprooyl-tetrapeptide-3 acetate stimulates the expression of collagen VII and laminin-5 in a model of corticoid-induced skin ageing[1].
Dimethyl biphenyl-4,4'-dicarboxylate (Biphenyl dimethyl dicarboxylate) is a hepatoprotectant obtained from Schizandra fructus and may induce a signal transduction similar to that associated with IFN[1].
Pirenoxine (Catalin K) is a potent antioxidant. Pirenoxine shows anti-presbyopic activity. Pirenoxine has the potential for the research of cataracts[1][2].
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.
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].
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.
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].
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].
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].
Eleutheroside D is an active lignan isolated from the root of Eleutherococcus senticosus, has anti-inflammatory and hypoglycemic activities[1]. Eleutheroside D is an optical isomer of Eleutheroside E (HY-N0272)[2].
LS2265 is a taurine derivative of fenofibrate and can induce proliferation of peroxisomes in liver cells of rats.
(2R)-Vildagliptin is the inactive isomer of Vildagliptin (HY-14291), and can be used as an experimental control. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity[1].
ω-Muricholic acid (ω-MCA) is a murine-specific secondary bile acid[1].
Octanoic acid-13C (Caprylic acid-13C) is the 13C labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
7-Methylxanthine, a methyl derivative of xanthine, is one of the purine components in urinary calculi.
Euphol acetate is a triterpene that can be isolated from Euphorbia broteri. Euphol acetate is an inhibitor of hepatic transport proteins organic anion-transporting polypeptide 1/3 (OATP1B1/3)[1][2].
8-NH2-ATP tetrasodium, an inactive form of ATP, is produced by 8-NH2-Ado. 8-NH2-Ado tetrasodium induces apoptosis-related cleavage of poly (ADP-ribose) polymerase[1][2].
Insulin (swine) is a porcine-derived insulin used in diabetes research[1].
(E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) is a potent and selective GSK-3α/β inhibitor, with an IC50 of 10 nM. (E/Z)-BIO-acetoxime shows more than 200-flod selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B (IC50=2.4, 4.3, 63 μM)[1].
3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is a nucleotide analogue that inhibits DNA-dependent RNA polymerases I and II. 3'-Deoxyuridine-5'-triphosphate strongly and competitively inhibits the incorporations of UTP into RNA with a Ki value of 2.0 μM[1].
Xanthine oxidoreductase-IN-3 is an orally active xanthine oxidoreductase (XOR) inhibitor, with an IC50 of 26.3 nM. Xanthine oxidoreductase-IN-3 can be used for the research of acute hyperuricemia[1].
Mogroside I E1, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities[1].
MK204 is an aldose reductase (AR) inhibitor that can be used in diabetes research[1].
Miglitol is an oral anti-diabetic drug that acts by inhibiting the ability of the patient to breakdown complex carbohydrates into glucose.Target: OthersMiglitol is an oral anti-diabetic drug that acts by inhibiting the ability of the patient to breakdown complex carbohydrates into glucose. It is primarily used in diabetes mellitus type 2 for establishing greater glycemic control by preventing the digestion of carbohydrates (such as disaccharides, oligosaccharides, and polysaccharides) into monosaccharides which can be absorbed by the body. Miglitol inhibits glycoside hydrolase enzymes called alpha-glucosidases. Since miglitol works by preventing digestion of carbohydrates, it lowers the degree of postprandial hyperglycemia. It must be taken at the start of main meals to have maximal effect. Its effect will depend on the amount of non-monosaccharide carbohydrates in a person's diet. Dietary supplementation with miglitol from pre-onset stage in OLETF rats delays the onset and development of diabetes and preserves the insulin secretory function of pancreatic islets [1]. Miglitol was orally administered at 40 mg/100 g of high-fat diet containing 45% kcal as fat to 12-week-old rats for 29 days, and age-matched rats without the agent were used as the respective controls [2].
Oxyresveratrol 3'-O-β-D-glucopyranoside is a phenolic compound isolated from Morus nigra root and is an effective tyrosinase inhibitor with an IC50 of 1.64 μM[1].
Phytanic acid is an endogenous metabolite present in Blood that can be used for the research of Zellweger Syndrome, Alpha Methylacyl CoA Racemase Deficiency, Rhizomelic Chondrodysplasia Punctata and Infantile Refsum Disease[1][2][3][4][5].