Metabolic Disease

Lysophosphatidylcholine 18:2 (1-Linoleoyl-2-Hydroxy-sn-glycero-3-PC), a lysophospholipid, is a potential biomarker identified from insulin resistance (IR) polycystic ovary syndrome (PCOS). Low plasma Lysophosphatidylcholine 18:2 also has been shown to predict impaired glucose tolerance, insulin resistance, type 2 diabetes, coronary artery disease, and memory impairment.

Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity. Miltefosine is an inhibitor of CTP-phosphocholine cytidyltransferase (CCT).

Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea.

SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC₅₀s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.

Erastin2, an Erastin (HY-15763) analog, is a ferroptosis inducer and a potent, selective inhibitor of the system xc(-) cystine/glutamate transporter

Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC₅₀ of 11 nM. Rosuvastatin potently blocks hERG current with an IC₅₀ of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.

CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP⁺-induced cytotoxicity through activation of the Keap1-Nrf2 cascade.

NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca²⁺ concentrations (IC₅₀=43 nM) elicited by activating the Ca²⁺ receptor in HEK 293 cells expressing the human Ca²⁺ receptor.

(-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a K_i of 0.73 nM.

Indole-3-carboxylic acid is an orally active urinary indolic tryptophan metabolite. Indole-3-carboxylic acid is a mediator of priming against Plectosphaerella cucumerina. Indole-3-carboxylic acid enhances the anti-colorectal cancer potency of Doxorubicin (HY-15142A) by inducing cell senescence. Indole-3-carboxylic acid can be used in liver disease research.

Homovanillic acid (Vanilacetic acid) is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency.

3-Indoleacrylic acid is a high-efficient antialgal agent. 3-Indoleacrylic acid increases reactive oxygen species (ROS) production, and inhibits the functions of all the nutrient assimilating genes, down-regulated ribulose-1,5-bisphosphate carboxylase/oxygenase II, and cytochrome f genes in P. donghaiense.

ATF3 inducer 1 is a potent ATF3 inducer. ATF3 inducer 1 increases the ATF3 protein and ATF3 mRNA expression. ATF3 inducer 1 shows anti-MetS activity in mouse.

Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC₅₀s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a K_d of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).

GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC₅₀s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (K_ATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.

2′-Deoxyadenosine is an adenine nucleoside that inhibits glucose-stimulated insulin release. 2′-Deoxyadenosine inhibits glucose-stimulated increases seen in islet cyclic AMP (cAMP) accumulation. 2'-Deoxyadenosine activates caspase-3 and promotes apoptosis. 2'-Deoxyadenosine inhibits the activity of S-adenosyl-L-homocysteine hydrolase (SAHH). 2'-Deoxyadenosine inhibits the growth of various cells. 2'-Deoxyadenosine has an anticancer effect on colon cancer.

BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with K_is of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.

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.

Vitexin is a c-glycosylated flavone, and is found in various medicinal plants species such as Trigonella foenum-graecum Linn. Vitexin has a wide range of pharmacological effects, including anti-oxidant, anti-cancer, anti-inflammatory, anti-hyperalgesic, and neuroprotective effects.

Pentadecylic acid is a saturated fatty acid with a 15-carbon backbone.