CL316243 is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors[1].CL316243 is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate[2]. CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence[3].
MK196 (MK-196) is an investigational diuretic which has pronounced saluretic activity in the rat and dog as well as both uricosuric and saluretic activity in the chimpanzee.
L-Tartaric acid (L-(+)-Tartaric acid) diammonium is an endogenous metabolite. L-Tartaric acid diammonium is the primary nonfermentable soluble acid in grapes and the principal acid in wine. L-Tartaric acid diammonium can be used as a flavorant and antioxidant for a range of foods and beverages[1].
Deoxycholic acid (cholanoic acid) sodium hydrate，a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5[1][2].
Quercetin 3-(6″-caffeoylsophoroside) is an orally active α-amylase inhibitor, with an IC50 of 73.66 μg/mL. Quercetin 3-(6″-caffeoylsophoroside) presents in thehydro-methanolic extract of Cardamine hirsuta Linn. Quercetin 3-(6″-caffeoylsophoroside) shows the antidiabetic activities by oxidative stress reduction and α-amylase inhibition. Quercetin 3-(6″-caffeoylsophoroside) can be used for diabetes mellitus research[1].
Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling[1].
Syringic acid-d6 is the deuterium labeled Syringic acid[1]. Syringic acid is correlated with high antioxidant activity and inhibition of LDL oxidation[2][3].
Ferric citrate (Iron(III) citrate), an orally active iron supplement, is an efficacious phosphate binder. Ferric citratee can be used for iron deficiency anemia and chronic kidney disease (CKD) research.
(-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a Ki of 0.73 nM.
PI3Kγ inhibitor 3 is a potent and remarkably selective PI3Kγ inhibitor with pIC50s of 9.1, 5.1, <4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively[1].
2-Acetonaphthone is an endogenous metabolite.
Pitavastatin Calcium is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells.
JNJ-40355003 is a potent and selective atty acid amide hydrolase (FAAH) inhibitor[1].
HNMPA is a membrane impermeable insulin receptor tyrosine kinase inhibitor. HNMPA inhibits serine and tyrosine autophosphorylation by the human insulin receptor. HNMPA has no effect on protein kinase C or cyclic AMP-dependent protein kinase activities[1][2]
(R)-ND-336 is a potent and selective MMP-9 inhibitor with a Ki of 19 nM. (R)-ND-336 inhibits MMP-2 (Ki=127 nM) and MMP-14 (Ki=119 nM). (R)-ND-336 has the potential for diabetic foot ulcers (DFUs) research[1].
TUG-891 is a potent and selective agonist of the long chain free fatty acid (LCFA) receptor 4.
CD3254 a potent and selective retinoid-X-receptor (RXR) agonist[1].
BPH-652 is a S. aureus dehydrosqualene synthase (CrtM) inhibitor, with a Ki of 1.5 nM and an IC50 of 100-300 nM (S. aureus pigment formation)[1].
Lacto-N-neodifucohexaose II (Compd 9) is a derivative of key human milk tetrasaccharide[1].
Amylin (1-37) (human) (hIAPP (1-37)) is a peptide hormone, present in pancreatic betacell secretory granules. The C-terminus of Amylin (1-37) (human) is amidated and there is a disulfide bond between cysteine residues 2 and 7[1].
T-863(DGAT-1 inhibitor) is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells.IC50 value:Target: DGAT1T863 causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.
S-(5'-Adenosyl)-L-methionine iodide (S-Adenosyl-L-methionine iodide) is an important methyl donor that is found in all living organisms[1].
Xanthine oxidoreductase-IN-2 (Compound IVa) is a xanthine oxidoreductase (XOR) inhibitor with the IC50 of 7.2 nM. Xanthine oxidoreductase-IN-2 shows hypouricemic effects in mice[1].
Adenosylcobalamin (Coenzyme B12;Cobamamide;AdoCbl) is an active form of Vitamin B12 which is a cofactor for methylmalonyl CoA mutase[1]
Masoprocol (meso-Nordihydroguaiaretic acid) is a potent and orally active lipoxygenase inhibitor. Masoprocol shows antihyperglycemic activity. Masoprocol decreases the glucose concentration and hepatic triglyceride in vivo. Masoprocol has the potential for the research of type II diabetes[1][2][3].
EP3 antagonist 4 (Compound 28) is an EP3 antagonist, with a Ki value of 2 nM for hEP. EP3 antagonist 4 shows low in vivo clearance, high oral AUC, and good bioavailability in the rat full PK studies. EP3 antagonist 4 can be used for research of beta cell dysfunction in diabetes[1].
2'-NH2-ATP (2'-Amino-2'-deoxyadenosine-5'-triphosphate), an adenosine derivative, is a weak competitive inhibitor of ATP, with a Ki of 2.3 mM. 2'-NH2-ATP can be used in nucleic acid labeling[1][2][3].
BMS-604992 (EX-1314) is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 demonstrates high-affinity binding (Ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 can stimulate food intake in rodents[1].
SB756050 is a selective TGR5 agonist currently in phase 1clinical trials for the treatment of type 2 diabetes.
TC AQP1 1 (m-Phenylenediacrylic acid) is a potent AQP1 inhibitor. TC AQP1 1 inhibits AQP1-mediated water flux in oocytes, with an IC50 of 8 μM[1].