ASP7657 (ASP-7657) is a potent, selective, orally active prostaglandin EP4 receptor antagonist with Ki values of 6.02 nM and 2.21 nM for rat and human EP4 receptors, resepctively; potently inhibits the PGE2-induced cAMP increase in CHO cells expressing rat EP4 receptors and human lymphoblastoid T (Jurkat) cells, with IC50 values of 0.86 nM and 0.29 nM, respectively; does not inhibit the PGE2-induced intracellular calcium increase in HEK293 cells expressing rat EP1 and EP3 receptors, or cAMP increase in CHO cells expressing rat EP2 receptors; dose-dependently inhibits the PGE2-mediated inhibition of LPS-induced TNF-α release from rat whole blood culture, attenuates albuminuria in type 2 diabetic mice at dose of 0.1 mg/kg. Diabetes Phase 1 Discontinued
BCPA is a Pin1 regulator without cytotoxicity. BCPA attenuates the reduction of Pin1 protein to inhibit receptor activator of RANKL-induced osteoclastogenesis. BCPA regulates osteoclast activation, used to osteoporosis research[1].
24, 25-Dihydroxy VD3 is a compound which is closely related to 1,25-dihydroxyvitamin D3, the active form of vitamin D3, but like vitamin D3 itself and 25-hydroxyvitamin D3 is inactive as a hormone both in vitro and in vivo.
AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM.
SCH-900271 is an orally active, potent nicotinic acid receptor (NAR) agonist with an EC50 of 2 nM in the hu-GPR109a assay. SCH-900271 exhibits dose-dependent inhibition of plasma free fatty acid (FFA). SCH-900271 has an improved therapeutic window to flushing[1].
Tegaserod is a serotonin receptor 4 agonist (HTR4) used in the treatment of irritable bowel syndrome (IBS). Anti-tumor activity[1].
MGAT2-IN-2 is a potent and selective acyl CoA:monoacylglycerol acyltransferase 2 (MGAT2) inhibitor with an IC50 of 3.4 nM.
OSBPL7-IN-1 is an orally active oxysterol binding protein like 7 (OSBPL7) inhibitor. OSBPL7-IN-1 promotes an increase of ABCA1 at the plasma membrane without affecting mRNA expression[1].
RO5166017 is an orally active and species-crosses TAAR1 agonist, with Ki values of 1.9 nM, 2.7 nM, 31 nM and 24 nM for mouse, rat, human and cynomolgus monkey, respectively[1].
Imirestat (AL 1576) is an aldose reductase inhibitor, used for the treatment of diabetes.
GDP-L-fucose is a nucleotide sugar that is a key substrate for the biosynthesis of fucose oligosaccharides, providing the fucose moiety for the oligosaccharides.The formation of GDP-L-fucose occurs through two pathways, the major ab initio metabolic pathway and the minor remedial metabolic pathway[1].
Tripeptide-41(CG-Lipoxyn)isa bioactive peptide withreduce fat accumulationeffect and has been reported used as a cosmetic ingredient[1].
KGA-2727 is a potent, selective SGLT1 inhibitor with Ki of 97.4 nM, >100-fold selectivity over SGLT2; attenuates the elevation of plasma glucose after glucose loading in streptozotocin-induced diabetic rats, preserves glucose-stimulated insulin secretion and reduces urinary glucose excretion with improved morphological changes of pancreatic islets and renal distal tubules in ZDF rats.
Glicoricone, a phenolic compound, is isolated from a species of licorice. Glicoricone is an inhibitor of monoamine oxidase (MAO), with an IC50 of 140 μM. Glicoricone binds to estrogen receptor (ER) and shows estrogen antagonist activity[1][2].
Tenapanor (AZD1722) hydrochloride is a potent and orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor hydrochloride reduces intestinal phosphate absorption predominantly through reduction of passive paracellular phosphate flux. Tenapanor hydrochloride has the potential for the research of hyperphosphatemia[1][2].
Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
FF-MAS is a potent meiotic maturation agonist. FF-MAS promotes meiotic maturation and preimplantation development of mouse oocytes maturing in vitro. FF-MAS promotes the completion of meiotic maturation to metaphase II (MII) and improves competence to complete the 2-cell stage to blastocyst transition[1][2].
AU-224 is a benzamide derivative used as a promising gastrointestinal prokinetic agent without significant side effects.
GDP-L-fucose disodium is a nucleotide sugar that is a key substrate for the biosynthesis of fucose oligosaccharides. GDP-L-fucose disodium provides the fucose moiety for the oligosaccharides. The formation of GDP-L-fucose disodium occurs through two pathways, the major de novo metabolic pathway and the minor remedial metabolic pathway[1].
Oct-1-en-3-ol, a fatty acid fragrant, is a self-stimulating oxylipin messenger. Oct-1-en-3-ol serves as a signaling molecule in plant cellular responses, plant-herbivore interactions, and plant-plant interactions. Oct-1-en-3-ol causes dopamine neuron degeneration through disruption of dopamine handling[1][2].
WS-12 is an agonist of TRPM8 with an EC50 of 39 nM.
BYK 191023 is a highly selective inducible nitric-oxide synthase (iNOS) inhibitor. BYK 191023 interacts with the catalytic center of the enzyme. BYK 191023 can be used to study the in vivo and in vitro effects mediated by iNOS [1].
(R)-Pantetheine is the biosynthetic precursor to CoA.(R)-Pantetheine and its corresponding disulfide pantethine, play a key role in metabolism as a building block of coenzyme A (CoA)[1].
5-Methyltetrahydrofolic acid is a biologically active form of folic acid. 5-Methyltetrahydrofolic acid is a methylated derivate of tetrahydrofolate. 5-Methyltetrahydrofolic acid is the predominant natural dietary folate and the principal form of folate in plasma and cerebrospinal fluid[1].
Mildronate dihydrate (Meldonium dihydrate) functions as a cardioprotective drug by cpmpetetively inhibiting BBOX1 and OCTN2. Mildronate (Meldonium) exhibits IC50 values of 34-62 μM for human recombinant BBOX and an EC50 of 21 μM for human OCTN2. Mildronate (Meldonium) treatment-induced redirection of long-chain FA metabolism from mitochondria to peroxisomes[1].
L17E, an endosomolytic peptide, is a cationic amphiphilic peptide with specific membrane lytic activity for late endosomes (LEs). L17E diminishes the TS5-p45 induced apoptosis in a dose-dependent manner. L17E is endocytosed into cells and trafficked to LEs. Within the acidic environment of LEs, L17E perturbs and lyses the LE membrane, leading to disruption of LE membrane and release of LE content to the cytosol. L17E is used to investigate the role of the endosomal protein trafficking pathway[1].
Arteanoflavone, a natural compound that can be isolated from A. iwayomogi, possess inhibitory activities on AGEs formation[1].
Adomeglivant is a potent and selective glucagon receptor antagonist that is used in clinical trial for type 2 diabetes mellitus.
γ-Glu-Gly-Gly is a tripeptide that can be used as a peptide substrate to generate Glu[1].
Levoglucosan-13C6 is the 13C labeled Levoglucosan[1]. Levoglucosan (1,6-Anhydro-β-D-glucopyranose) is an anhydrosugar produced through glucan pyrolysis and is widely found in nature[2].