Seladelpar is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist.
For explanation of superscript II in systematic name, see 2-carb.37. Reaction: UDP-α-D-galactose + β-D-galactosyl-(1→4)-β-D-glucosyl-(1↔1)-ceramide = UDP + α-D-galactosyl-(1→4)-β-D-galactosyl-(1→4)-β-D-glucosyl-(1↔1)-ceramide
KRP-297 is a PPARα and PPARγ agonist potentially for the treatment of type 2 diabetes and dyslipidemia. KRP-297 restores reduced lipid oxidation, and inhibits of enhanced lipogenesis and triglyceride accumulation in the liver.
LTβR-IN-1 is a potent, selective lymphotoxin β receptor (LTβR) inhibitor with an IC50 of 10 μM. LTβR-IN-1 is potent in TWEAK-stimulated p52 translocation assays with an IC50 of 10 μM and did not alter TNF-α–induced p65 nuclear translocation[1].
α-Melanocyte-Stimulating Hormone (MSH), amide TFA is an endogenous neuropeptide, with anti-inflammatory and antipyretic activities. α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC), acts as an endogenous melanocortin receptor 4 (MC4R) agonist[1][2].
1-Deoxynojirimycin (DNJ, Duvoglustat) is a potent α-glucosidase inhibitor, suppresses postprandial blood glucose, thereby possibly preventing diabetes mellitus. Target: α-glucosidase1-Deoxynojirimycin is an alpha-glucosidase inhibitor, most commonly found in mulberry leaves. Although it can be obtained in small quantities by brewing an herbal tea from mulberry leaves, interest in commercial production has led to research on developing mulberry tea higher in DNJ, and on alternate routes of production, such as via Bacillusspecies.
3-Methylbutanoic acid is a natural fatty acid and known to effect on neonatal death and possible Jamaican vomiting sickness in human.
L-Carnosine is a dipeptide of the amino acids beta-alanine and histidine and has the potential to suppress many of the biochemical changes that accompany aging.
Diaminopropionoyl tripeptide-33isa bioactive peptide with protects skin cells from UVA-induced DNA damages and has been reported used as a cosmetic ingredient[1].
Bupleuroside XIII is a natural hepatoprotective saponin[1].
(3S,5S)-Atorvastatin is a inactive enantiomer of Atorvastatin. (3S,5S)-Atorvastatin can activate pregnane X receptor (PXR). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids[1][2].
CP-346086 is a potent and orally active microsomal triglyceride transfer protein (MTP) inhibitor, with an IC50 of 2.0 nM for human and rodent MTP. CP-346086 can lower plasma cholesterol and triglycerides in vivo[1].
M77976 is a specific ATP-competitive inhibitor of PDK4 (pyruvate dehydrogenase kinase isoforms 4), with an IC50 of 648 μM. M77976 is potential for the research of obesity and diabetes[1].
Hispidin, a PKC inhibitor and a phenolic compound from Phellinus linteus, has been shown to possess strong anti-oxidant, anti-cancer, anti-diabetic, and anti-dementia properties[1].
AZP-531 is an analogue of unacylated ghrelin designed to improve glycaemic control and reduce weight.
Osteostatin (human), a fragment of parathyroid hormone-related protein (PTHrP) 107-139, promotes bone repair in animal models of bone defects and prevents bone erosion in inflammatory arthritis[1].
PKD-IN-1 (compound 32), an aminoethylamino-aryl (AEAA) compound, acts as PKD-1 inhibitor. PKD-IN-1 can be used for protein kinase D (PKD)-mediated diseases research[1].
AP5 sodium is a potent, orall active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 sodium demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 sodium has the potential for type II diabetes research[1].
Urocortin II, mouse is a potent and selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor with Ki values of 0.66 nM and ﹥100 nM for CRFR2 and CRFR1, respectively. Urocortin II, mouse activates CRF2 receptors in a cAMP/PKA- and Ca2+/CaMKII-dependent manner.Urocortin II, mouse is expressed in discrete areas of the central nervous system, and activates central neurons involved in the processing of visceral sensory information, and in modulating autonomic outflow[1][2][3].
SQDG is a glycolipid that possesses sugar moieties in their head groups. SQDG is a membrane lipid that can be used to investigate the effects of structural lipid in LNP formulations[1].
Lixisenatide acetate is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes mellitus (T2DM).
Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research[1].
(R)-2-Hydroxybutanoic acid is the inactive isomer of 2-Hydroxybutyric acid (HY-113381), and can be used as an experimental control. 2-Hydroxybutyric acid (α-Hydroxybutyric acid ) is converted from 2-Aminobutyric acid, with 2-oxobutyric acid as an intermediate metabolite[1].
The acceptor is Galβ1,3GalNAc-R, where R is H, a threonine or serine residue in a glycoprotein, or a glycolipid. Lactose can also act as acceptor. May be identical with EC 2.4.99.2 monosialoganglioside sialyltransferase. Reaction: CMP-N-acetylneuraminate + β-D-galactosyl-(1→3)-N-acetyl-α-D-galactosaminyl-R = CMP + α-N-acetylneuraminyl-(2→3)-β-D-galactosyl-(1→3)-N-acetyl-α-D-galactosaminyl-R
hiCE inhibitor-1, a sulfonamide derivative, is a selective human intestinal enzyme (hiCE) inhibitor with a Ki value of 53.3 nM. hiCE inhibitor-1 can be used to improve Irinotecan (HY-16562)-induced diarrhoea[1].
Ampkinone is an indirect AMP-activated protein kinase (AMPK) activator.
Cyclohexaneacetic acid is an endogenous metabolite.
Glucarpidase is an enzyme that inactivates methotrexate. Glucarpidase can be used for renal dysfunction diseases research[1].
L-Alanine-1-13C,15N (L-2-Aminopropionic acid-1-13C,15N) is the 13C- and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Epoetin beta (rhEPO) is a recombinant form of erythropoietin. Epoetin beta is responsible for the maintenance of erythropoiesis and can be used for anaemia research[1].