MMP13-IN-4 (compound 13) is a potent and selective inhibitor of MMP-13 (IC50=14.6 μM)，involved in osteoarthritis (OA)[1].
Canagliflozin is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively.
Otenabant Hydrochloride is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.
2-Thiophenecarboxaldehyde is an endogenous metabolite.
Relamorelin (RM-131), a Ghrelin analog, is a potent ghrelin receptor agonist, with a Ki of 0.42 nM for GHS-1a. Relamorelin can promote food intake and adiposity in mice. Relamorelin can be used for the research of cachexia, gastroparesis, and gastric/intestinal dysmobility disorders[1][2][3].
Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.
TP-004 is a potent, selective METAP2 (Methionine aminopeptidase-2) inhibitor.
RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC)[1][2][3][4].
Tetradecanedioic acid is an endogenous metabolite and belongs to the class of organic compounds known as long-chain fatty acids. Tetradecanedioic acid can act as a candidate biomarker for organic anion-transporting polypeptide mediated drug-drug interactions [1].
Linoleic acid-13C1 is the 13C labeled Linoleic acid. Linoleic acid is a common polyunsaturated (PUFA) found in plant-based oils, nuts and seeds. Linoleic acid is a part of membrane phospholipids, and functions as a structural component to maintain a certain level of membrane fluidity of the transdermal water barrier of the epidermis. Linoleic acid induces red blood cells and hemoglobin damage via oxidative mechanism [1][2].
Lactate-13C-1 (sodium) is the 13C labeled Lactate (sodium)[1]. Lactate (Lactic acid) sodium is the product of glycogenolysis and glycolysis. Lactate (Lactic acid) sodium functions in a variety of biochemical processes[2].
Hesperetin 7-O-glucoside is produced by the enzymatic conversion of Hesperidin. Hesperetin 7-O-glucoside is a potent human HMG-CoA reductase inhibitor and also effectively inhibits the growth of Helicobacter pylori. Antihypertensive effect[1][2].
4'-Methoxychalcone regulates adipocyte differentiation through PPARγ activation. 4'-Methoxychalcone modulates the expression and secretion of various adipokines in adipose tissue that are involved in insulin sensitivity[1].
Icosabutate, a structurally engineered and orally active ω-3 polyunsaturated fatty acid, is an aeicosapentaenoic acid (EPA) derivative. Icosabutate overcomes the drawbacks of unmodified EPA for liver targeting and improves insulin sensitivity, hepatic inflammation and fibrosis[1]. Icosabutate is well tolerated, and efficacious in lowering non-high-density lipoprotein cholesterol (non-HDL-C) levels in persistent hypertriglyceridemia [2].
GIP (3-42), human acts as a glucose-dependent insulinotropic polypeptide (GIP) receptor antagonist, moderating the insulin secreting and metabolic actions of GIP in vivo[1].
Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ[1][2][3][4].
Calcitriol Impurities D is the impurity of Calcitriol, Calcitriol is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).Target: vitamin D receptor
Suvodirsen sodium induces exon 51 skipping and has the potential for study Duchenne muscular dystrophy (DMD)[1].
Benzothiazole is a natural occurring heterocyclic nuclei. Benzothiazole nucleus possesses a number of biological activities such as anticancer, antimicrobial, antidiabetic, anti-inflammatory, antiviral, antileishmanial, and antiviral[1].
1,2-Cyclohexylenedinitrilotetraacetic acid (CDTA) is a chelating agent. 1,2-Cyclohexylenedinitrilotetraacetic acid has an ability to remove manganese from brain and liver (in vivo) and their sub-cellular fractions (in vitro), of rats pretreated with manganese sulphate[1].
COH1 is a ribonucleotide reductase (RR) inhibitor. COH1 can be used in research into cancer, mitochondrial diseases, and neurodegenerative diseases[1].
BMS-191095 is an activators of mitochondrial ATP-sensitive potassium (mitoKATP) channels.Target: potassium channelin vitro: BMS-191095 induces mitochondrial-depolarization and vasodilation. BMS-191095 elicites a dose-dependent vasodilation in endothelium denuded cerebral arteries with 8.1 ± 2.3%, 31.6 ± 2.1%, and 39.5 ± 3.2% relaxation in response to 10, 50, and 100 μM, respectively. in vivo: In normal rats, BMS-191095-induced vasodilation was mediated by mitochondrial depolarization and calcium sparks generation in VSM and was reduced by inhibition of BKCa channels.
JA-ACC (Jasmonyl-ACC) is a derivative of 1-aminocyclopropane-1-carboxylic acid (ACC). ACC is the direct precursor of the plant hormone ethylene. JA-ACC inhibits root growth in Arabidopsis and the inhibition is independent of jasmonic acid (JA) signaling[1].
Endo-β-Galactosidase catalyzes the hydrolysis of internal β1-4 galactose linkages in unbranched, repeating poly-N-acetyllactosamine ([GlcNAc-?(1-3)Gal-?(1-4)]n) structures[1].
AZD1979 is a Melanin-concentrating hormone receptor 1 (MCHr1) antagonist with an IC50 of ~12 nM.
PD 128042 (CI 976) is a potent, orally active, and selective inhibitor of ACAT (acyl coenzyme A:cholesterol acyltransferase) with an IC50s of 73 nM. PD 128042 is also a potent LPAT (lysophospholipid acyltransferase) inhibitor. PD 128042 inhibits Golgi-associated LPAT activity (IC50=15 μM). PD 128042 inhibits multiple membrane trafficking steps, including ones found in the endocytic and secretory pathway[1][2][3].
N,N′-Diferuloylputrescine is a inhibitor of pigmentation with 57% reduction. N,N′-Diferuloylputrescine significantly reduces the protein level of MITF. N,N′-Diferuloylputrescine has strong antioxidant activities as radical scavengers against reactive oxygen species[1].
Tibesaikosaponin V (TKV) is a triterpene diglycoside, which can be isolated from the methanol extract of the roots of Bupleurum chinense DC.. Tibesaikosaponin V inhibits lipid accumulation and triacylglycerol content occurred without cytotoxicity to adipocytes. Tibesaikosaponin V suppresses the mRNA expression of nuclear transcription factors, such as peroxisome proliferator-activated receptor γ (PPARγ) and CCAAT/enhancer binding protein α (C/EBPα). Tibesaikosaponin V inhibits 3T3-L1 preadipocyte differentiation. Tibesaikosaponin V can be used fro research of obesity and its associated metabolic disorders[1].
Decanedioic acid-d4 is the deuterium labeled Decanedioic acid[1]. Decanedioic acid, a normal urinary acid, is found to be associated with carnitine-acylcarnitine translocase deficiency and medium chain acyl-CoA dehydrogenase deficiency[2].
Cetilistat is an inhibitor of pancreatic and gastrointestinal lipases. It has great treatment of obesity in both diabetic and non-diabetic patients.