Metabolic Disease

Arimoclomol maleate (BRX-220) is an orally active co-inducer of heat shock proteins (HSP). Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system.Arimoclomol maleate can be used for the study of Niemann–Pick disease type C.

Tryptamine is a selective, blood-brain-penetrating 5-HT4 receptor agonist (EC50=1-3 mM) and an endogenous ligand of the aryl hydrocarbon receptor (AHR) (Kd=10-50 nM). Tryptamine promotes intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs) and accelerates gastrointestinal motility. Tryptamine regulates Th17/Treg balance to inhibit neuroinflammation, competitively binds to 5-HT receptors to regulate central nervous system activity, and participates in temperature regulation and spinal reflex regulation as a neuromodulator. Tryptamine can be used to study intestinal motility disorders such as functional constipation, and has shown significant efficacy in multiple sclerosis models.

α-Glucosidase, Yeast (α-D-Glucosidase, Yeast), a carbohydrate hydrolyzing enzyme, catalyzes the liberation of α-glucose from the non-reducing end of the substrate. α-Glucosidase can facilitate the absorption of glucose by the small intestine. Inhibition of α-Glucosidase is an effective management of non-insulin-dependent diabetes mellitus (NIDDM).

Tambiciclib (GFH009, JSH-009) is an orally active, highly potent and selective CDK9 inhibitor (IC₅₀ = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib can be used for AML research.

PF-04620110 is a potent, selective and orally bioavailable diglyceride acyltransferase-1 (DGAT-1) inhibitor with an IC₅₀ of 19 nM.

Givosiran (ALN-AS1) sodium is a small interfering RNA that targets hepatic aminolevulinate synthase 1 (ALAS1) messenger RNA. Givosiran sodium downregulates ALAS1 mRNA and prevents accumulation of neurotoxic δ-aminolevulinic acid (ALA) and porphobilinogen (PBG) levels. Givosiran sodium demonstrates potent inhibitory activity against ALAS1 in mouse, rat, and cynomolgus monkey models. Givosiran sodium can be used for the research of acute hepatic porphyria (AHP).

SKF-34288 (3-Mercaptopicolinic acid) hydrochloride is an orally active phosphoenolpyruvate carboxykinase (PEPCK) inhibitor (K_i: 2-9 μM). SKF-34288 hydrochloride is a potent hypoglycemic agent by inhibiting glucose synthesis. SKF-34288 hydrochloride also inhibits Asn metabolism and increases amino acids and amides.

D-Erythrose 4-phosphate sodium is a phosphate sodium of the simple sugar Erythrose. Erythritol is actually converted into D-Erythrose 4-phosphate that involves three isomerases.

Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule in the de novo pyrimidine biosynthetic pathway in T. gondii.

Stevioside is an orally active sweetener that can be isolated from Stevia rebaudiana, with antihypertensive, antihyperglycemic, antioxidant, anti-inflammatory and anti-tumor activities.

Seladelpar (MBX-8025) is an orally active, potent and specific PPARδ agonist with an EC₅₀ of 2 nM. Seladelpar shows more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively. Seladelpar can be used for the study of primary biliary cholangitis.

BODIPY 581/591 C11 (solution) is a BODIPY borofluoroprene derivative with good light stability and low fluorescence artifacts. BODIPY 581/591 C11 can be used for study lipid peroxidation and antioxidant properties in living cells, or detect ferroptosis by reaction with hydroxyl radicals. BODIPY 581/591 C11 is emitted at 591 nm (reduced prototype) , or redshifted to 510 nm (oxidized type). The excitation wavelengths were 581 nm (reduced prototype) and 500 nm (oxidized type) .
Solvent and concentration: DMSO: 2 mM

PFK-015, a derivative of 3PO, is a specific PFKFB3 inhibitor. PFK-015 inhibits recombinant PFKFB3 with an IC₅₀ value of 110 nM and inhibits PFKFB3 activity in cancer cells with an IC₅₀ value of 20 nM. PFK-015 can be used for the research of multiple cancers such as lung cancer, stomach cancer, colon cancer and esophageal squamous cell carcinoma (ESCC).

Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning.

Adenosine 5′-diphosphoribose (ADP ribose) is a nicotinamide adenine nucleotide (NAD⁺) metabolite. Adenosine 5′-diphosphoribose is the most potent and primary intracellular Ca²⁺-permeable cation TRPM2 channel activator. Adenosine 5′-diphosphoribose also can enhance autophagy.

AMP-PNP (Adenylyl-imidodiphosphate) tetralithium is a non-hydrolyzable ATP analog. AMP-PNP tetralithium binds to ATP binding sites competely but is not hydrolyzed by enzymes, providing stable experimental conditions for studying ATP-dependent processes. AMP-PNP tetralithium can also be used to study enzyme activity, kinase regulation, DNA/RNA metabolism, ion channel function, and protein complex assembly.

Chicoric acid (Cichoric acid), an orally active dicaffeyltartaric acid, induces reactive oxygen species (ROS) generation. Chicoric acid inhibits cell viability and induces mitochondria-dependent apoptosis in 3T3-L1 preadipocytes through ROS-mediated PI3K/Akt and MAPK signaling pathways. Chicoric acid increases glucose uptake, improves insulin resistance, and attenuates glucosamine-induced inflammation. Chicoric acid has antidiabetic properties and antioxidant, anti-inflammatory effects.

MZ-101 (GYS1-IN-2) is an orally active, potent and selective small-molecule glycogen synthase 1 (GYS1) inhibitor with with an IC₅₀ value of 0.041 µM. MZ-101 reduces glycogen concentrations in cells and in mice. MZ-101 can used to study GYS1 -mediated Pompe disease and other glycogen storage diseases.

Alagebrium chloride (ALT711) is an advanced glycation end product (AGE) inhibitor.

Gly-Phe-β-naphthylamide is a substrate of Cathepsin C (HY-P2922) and belongs to the lysosomal agonist. Gly-Phe-β-naphthylamide can freely pass through the cell membrane and organelle membrane. Gly-Phe-β-naphthylamide will be specifically hydrolyzed by Cathepsin C, ultimately leading to a permeability lysis when it enters the acidic compartment. Gly-Phe-β-naphthylamide can be used to study lysosomal hydrolysis, lysosomal membrane permeability, and the function of cathepsin C.