Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects[1].
Pegapamodutide (LY-2944876) is a glucagon-GLP-1 receptor agonist, and can be used in type 2 diabetes and obesity research[1].
α-GLU stands for α-glucosidase. α-GLU hydrolyzes starch and disaccharides via targeting to terminal, non-reducing (1→4)-linked α-D-glucose residues to produce α-glucose. α-GLU is substrate selective[1].
L-Phenylalanine-13C9 ((S)-2-Amino-3-phenylpropionic acid-13C9) is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
NVP-DPP728 is a potent, reversible and nitrile-dependent dipeptidyl peptidase IV (DPP-IV) inhibitor. NVP-DPP728 can inhibit human DPP-IV amidolytic activity with a Ki of 11 nM. NVP-DPP728 inhibits degradation of glucagon-like peptide-1 (GLP-1) and thereby potentiates insulin release in response to glucose intake. NVP-DPP728 can be used for researching diabetes[1].
Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone.Leriglitazone (Hydroxypioglitazone) PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy.Leriglitazone (Hydroxypioglitazone) binds to the PPARγ C-terminal ligand-binding domain (LBD) with Ki of 1.2 μM，induces transcriptional efficacy of the PPARγ (LBD) with EC50 of 680 nM[1].
Mogroside III, 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].
N-Benzyloleamide is a maccamide isolated from Lepidium meyenii (Maca). N-Benzyloleamide irreversibly inhibits fatty acid amide hydrolase (FAAH). N-benzyloleamide influences the energy metabolism and reveals antioxidant and antifatigue activities[1][2].
Cholecystokinin is a peptide hormone. Cholecystokinin, as a hunger suppressant, inhibits food intake and stimulates the digestion of fat and protein. Cholecystokinin can be used for the research of gastrointestinal system[1][2][3].
SREBP/SCAP-IN-2(compound 13) is a selectiveSREBP/SCAPinhibitor[1].
D-(+)-Sorbose, an active enantiomer of D-Sorbose, which inhibits disaccharidase activity and demonstrates suppressive action on postprandial blood levels of glucose and insulin in the rat. D-sorbose acts as a sweetener may contribute to the prevention of lifestyle-related diseases, such as type 2 diabetes mellitus[1].
Adenosine-3′-13C is the 13C labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiolo
Rosiglitazone-d3 (BRL 49653-d3) is the deuterium labeled Rosiglitazone. Rosiglitazone (BRL 49653) is a selective, orally active PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively. Rosiglitazone binds to PPARγ with a Kd of approximately 40 nM. Rosiglitazone is also an activator of TRPC5 (EC50=~30 μM) and an inhibitor of TRPM3[1][2][3][4].
CP-319340 free base is a microsomal triglyceride transfer protein (MTP) inhibitor.
Trimethylammonium chloride-d10 is the deuterium labeled Trimethylammonium chloride[1]. Trimethylammonium chloride is an endogenous metabolite.
Mozavaptan hydrochloride (OPC-31260 hydrochloride) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan hydrochloride shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan hydrochloride has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment[1][2].
Abietic acid, a diterpene isolated from Pimenta racemosa var. grissea, possesses antiproliferative, antibacterial, and anti-obesity properties. Abietic acid inhibits lipoxygenase activity for allergy treatment[1][2].
3,3-Dimethylglutaric acid, a member of methyl-branched fatty acids, is a endogenous metabolite occasionally found in human urine[1].
3-Methylglutaconic acid is the major metabolites accumulating in 3-Methylglutaconic aciduria (MGTA). 3-Methylglutaconic acid can induce lipid oxidative damage and protein oxidative. 3-Methylglutaconic acid decreases the non-enzymatic antioxidant defenses in cerebral cortex supernatants to elicit oxidative stress in the cerebral cortex. 3-Methylglutaconic acid can be used for brain damage disease research[1].
SBI-993 is an analog of SBI-477 that shows improved potency and suitable pharmacokinetic properties for in vivo bioavailability; reduces Txnip and Arrdc4 expression to a degree similar to that seen with SBI-477 in human myotubes; reduces muscle and liver TAG levels, enhances insulin signaling, and improved glucose tolerance in mice fed a high-fat diet.
Apelin-13 is the endogenous ligand of the orphan G protein-coupled receptor APJ, activates APJ receptor with an EC50 value of 0.37 nM in CHO cells[1][2].
8-Aminooctanoic acid is an omega-amino fatty acid that is octanoic acid which carries an amino group at position 8. 8-aminooctanoic acid has a role as a human metabolite[1].
Cicrotoic acid is an unsaturated fatty acid that increases bile flow and changes lipid composition[1].
SJ000063181 is a potent BMP signaling activator with an EC50 ≤1 µM. SJ000063181 can be used as chemical probes to interrogate BMP signaling due to it can penetrate zebrafish embryos[1].
L-796568 is a β(3)-adrenergic receptor agonist. L-796568 can be used for the research of obesity[1].
PF 03716556 is a potent, and selective acid pump (H+,K+ ATPase) antagonist, with pIC50 value of 6.009.IC50 value:6.009 (pIC50)Target: H+,K+ ATPasePF-03716556 inhibited the activity of H+, K+-ATPase with pIC50 of 6.026 ± 0.112, 6.038 ± 0.039 and 6.009 ± 0.209 at pH 6.4 for porcine, canine and human ion-leaky membrane vesicles, respectively. PF-03716556 (PF03716556) is useful for treatment of gastroesophageal reflux disease.
Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive and orally active pan-PTP (protein tyrosine phosphatases) inhibitor. Bis(maltolato)oxovanadium(IV) inhibits HCPTPA, PTP1B, HPTPβ and SHP2 with IC50s of 126 nM, 109 nM, 26 nM and 201 nM, respectively. Bis(maltolato)oxovanadium(IV) is a potent insulin sensitizer[1][2].
WAY-362450 is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM.
Crotonyl-CoA is an intermediate in the fermentation of butyric acid, and in the metabolism of lysine and tryptophan. Crotonyl-CoA is important in the metabolism of fatty acids and amino acids[1].
Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.