Oxindole (Indolin-2-one) is an aromatic heterocyclic building block. 2-indolinone derivatives have become lead compounds in the research of kinase inhibitors.
Chlorazanil is a triazine derivative and also a new nonmercurial diuretic agent.
Apigenin 4′-O-β-D-glucopyranoside is a flavonoid that can be found in caledonian guioa villosa[1].
Alogliptin 13CD3 (SYR-322 13CD3) is the deuterium labeled Alogliptin. Alogliptin is a potent and selective inhibitor of DPP-4.
YM348 is a potent and orally active 5-HT2C receptor agonist, which shows a high affinity for cloned human 5-HT2C receptor (Ki: 0.89 nM).
L-Leucine-1-13C,15N is the 13C- and 15N-labeled L-Leucine. L-Leucine is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway[1].
Dentonin (AC-100) is a synthetic fragment derived from MEPE. Dentonin enhances osteogenesis by promoting osteoprogenitor adhesion and facilitates immature adherent cells survival. Dentonin has no significant effect to mature osteoblasts. Dentonin can be used for the research of phosphate homeostasis and bone metabolism[1].
SSAO inhibitor-3 (Compound 2) is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor with IC50s of <10 nM, and 0.1-10 μM for human SSAO and AOC1, respectively. SSAO inhibitor-3 can be used for the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, multiple sclerosis, etc[1].
Hymeglusin, as a fungal β-lactone antibiotic, is a HMG-CoA synthase inhibitor (IC50 = 0.12 μM). Hymeglusin covalently modifies the active Cys129 residue of the enzyme[2][3].
Adrenocorticotropic Hormone (ACTH) (1-39), rat is a potent melanocortin 2 (MC2) receptor agonist.
KL001 is a cryptochrome protein (CRY) stabilizer which specifically interacts with CRY1 and CRY2. KL001 prevents ubiquitin-dependent degradation of CRY, resulting in lengthening of the circadian period. KL001 has the potential to control fasting hormone-induced gluconeogenesis[1][2].
Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ[1][2].
2-Acetamido-2,4-dideoxy-4-fluoro-α-D-glucopyranose (compound 13) is a hepatic glycosaminoglycan biosynthesis inhibitor[1].
(±)-Carnitine chloride exists in two isomers, known as D and L. L-carnitine plays an essential role in the β-oxidation of fatty acids and also shows antioxidant, and anti-inflammatory activities.
Acetyl-(D-Phe2,Lys15,Arg16,Leu27)-VIP (1-7)-GRF (8-27), a vasoactive intestinal peptide (VIP), is a VIP1 antagonist[1].
Taurolithocholic Acid-d5 sodium salt is the deuterium labeled Taurolithocholic acid sodium salt. Taurolithocholic acid sodium salt, a potent cholestatic agent, is a potent Ca2+ agonist[1][2].
Isomaltose is composed of two glucose units and suitable as a non-cariogenic sucrose replacement and is favorable in products for diabetics and prediabetic dispositions.
Lumiracoxib-d6 (COX-189-d6) is the deuterium labeled Lumiracoxib. Lumiracoxib is a potent,selective and orally active COX-2 inhibitor with a Ki value of 0.06 μM[1]. Lumiracoxib acts as a nonselective NSAID with anti-inflammatory, analgesic and antipyretic activities. Lumiracoxib can be used for osteoarthritis and bone cancer research[1][2].
DGAT-1 inhibitor 2 is an effective inhibitor of DGAT-1;antiobesity agents.IC50 value:Target: DGAT-1Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) is one of two known DGAT enzymes that catalyze the final step in triglyceride synthesis. Findings from genetically modified mice as well as pharmacological studies suggest that inhibition of DGAT1 is a promising strategy for the treatment of obesity and type 2 diabetes.
α-Amylase-IN-3 (Compound 4) is a none-competitive type of α-Amylase inhibitor with an IC50 value of 18.04 μM, which also has radical scavenging activities (DPPH and ABTS) with IC50 values of 16.04 μM (DPPH) and 16.99 μM (ABTS), respectively. α-Amylase-IN-3 has good protein–ligand interactions profile against α-Amylase. α-Amylase-IN-3 may have pharmacological activities such as anti-oxidative, anti-inflammatory inhibitory, which is helpful for the development of diabetes and oxidative stress associated disease[1].
4'-Hydroxyflavanone is an inhibitor of SREBP maturation and lipid synthesis. 4'-Hydroxyflavanone is a synthetic analogue of flavanone, has potential for hepatic steatosis and dyslipidemia research[1].
Meliasendanin D (Compound 4) is a lignin.Meliasendanin D is isolated from the natural Melia toosendan fruit. Meliasendanin D has antioxidant activity[1].
CTP inhibitor is a potent and selective CTP inhibitor. CTP inhibitor inhibits the plasma membrane citrate transporter (PMCT)[1].
NHE3-IN-3 (Compound 1) is a Na+/H+ exchanger isoform 3 (NHE3) inhibitor with pIC50 of 6.2 and 6.6 against human and rat NHE3, respectively. NHE3-IN-3 shows high (98%) oral bioavailability in Sprague–Dawley rats[1].
Tubulin polymerization-IN-21 (compound 9a) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-21 exhibits anti-cancer activity through disrupting cellular integrity and affecting glucose metabolism[1].
GS 389 ((±)-O,O-Dimethylcoclaurine) is a tetrahydroisoquinoline. GS-389 inhibites Cyclic AMP and cyclic AMP dependent phosphodiesterases from rat atrial and ventricular tissue. GS-389 relaxes the contraction induced by phenylephrine and high K+ in rat aortic rings[1].
Cazpaullone is a glycogen synthase kinase-3 (GSK-3) inhibitor. Cazpaullone can activate pancreatic beta cell protection and replication. Cazpaullone can be used for the research of diabetes[1].
Pregnenolone 16α-carbonitrile is an orally active prototypical and effective rodent-PXR activator. Pregnenolone 16α-carbonitrile, a synthetic steroid, induces cytochrome P4503A expression. Pregnenolone 16α-carbonitrile exhibits increased resistance to subsequent stressful insults[1][2][3].
KU14R is a new I(3)-R antagonist, which selectively blocks the insulin secretory response to imidazolines.IC50 Value:Target: Insulin ReceptorA new I(3)-R antagonist, KU14R (2 (2-ethyl 2,3-dihydro-2-benzofuranyl)-2-imidazole), which selectively blocks the insulin secretory response to imidazolines. KU14R partially attenuated responses to Imidazole-4-acetic acid-ribotide (IAA-RP). The effects of KU14R on stimulus secretion-coupling in normal mouse islets and beta cells was compared by measuring KATP channel activity, plasma membrane potential, cytosolic calcium concentration ([Ca2+]c) and dynamic insulin secretion. In the presence of 10 mmol/l but not of 5 mmol/l glucose, KU14R (30, 100 or 300 micromol/l) was ineffective. KATP channel was blocked by KU14R (IC50 31.9 micromol/l, Hill slope -1.5). KU14R does not act as an antagonist of either efaroxan or S22068 at an imidazoline site in vivo.
2-Hydroxyestradiol, a metabolite of 17β-estradiol with minimal estrogenic activity, possesses antioxidant effects and reacts with DNA to form stable adducts and exerts genotoxicity[1][3].