Etidronic acid (Etidronate) disodium is an orally and intravenously active bisphosphonate. Etidronic acid disodium inhibits resorption of bone, reduces arterial calcification and can be used for osteoporosis research. Etidronic acid disodium has anticancer activity. Etidronic acid disodium is a chelating agent and can be used to remove heavy metal in water[1][2][3][4].
γ-Glu-Gly-Gly is a tripeptide that can be used as a peptide substrate to generate Glu[1].
1-Azakenpaullone (1-Akp) is a highly selective and ATP-competitive inhibitor of glycogen synthase kinase-3 β (GSK-3β), with an IC50 value of 18 nM[1].
RBP4 ligand-1 is a non-retinoid ligands for (RBP4) retinol-binding protein 4. The hRBP4SPA IC50 and RBP4–TTR FRET IC50 values are 0.23±0.11 and 0.13±0.12 μM in the radioligand binding assay and FRET assay, respectively[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].
Orphan GPCR SP9155 agonist P550 (mouse, rat) (26RFa (mouse, rat)), a member of the RFamide peptide family with orexigenic effect, is the cognate ligand of the mouse orphan receptor GPR103, also designated SP9155 or AQ27[1][2].
PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.
β-Amyrin acetate is a triterpenoid with potent anti-inflammatory, antifungal, anti-diabetic, anti-hyperlipidemic activities. β-Amyrin acetate can inhibit HMG-CoA reductase activity by locating in the hydrophobic binding cleft of HMG CoA reductase[1][2][3][4].
Malvidin-3-O-arabinoside chloride ameliorates ethyl carbamate-induced oxidative damage by stimulating AMPK-mediated autophagy[1].
Pegylated synthetic human c-peptide retains bioactivity comparable to that of natural (i.e. non-polyethylene glycolated) C-peptides and has a prolonged circulating residence time in plasma for use in diabetic peripheral neuropathy studies[1].
all-trans-4-Oxoretinoic acid, an active metabolite of vitamin A, induces gene transcription via binding to nuclear retinoic acid receptors (RARs).
Haloxyfop is an aryloxyphenoxypropionic acid herbicide and is widely used in grass weeds in broad-leaf crops[2]. Haloxyfop inhibits the acetyl coenzyme A carboxylase (EC 6.4.1.2) from corn seedling chloroplasts with an IC50 of 0.5 μM, but has no effect on this enzyme in pea[2].
α-Amylase/α-Glucosidase-IN-1 (compound 33) is a potent α-amylase/α-glucosidase inhibitor with IC50s of 2.01, 2.09 µM for α-amylase and α-glucosidase, respectively. Kinetic studies predict that α-Amylase/α-Glucosidase-IN-1 has the potential of anti hyperglycemia[1].
SSAO inhibitor-2 (Compound 1) is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor with IC50s of <10 nM, and 10-100 μM for human SSAO and MAO-A, respectively. SSAO inhibitor-3 can be used for the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, multiple sclerosis, etc[1].
CB1 antagonist 1 is an antagonist of CB1 receptor, used in the research of metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, gastrointestinal disorders, and cardiovascular conditions.
Luspatercept (ACE-536) is a recombinant modified ActRIIB fusion protein that binds with transforming growth factor β superfamily ligands. Luspatercept increases the erythrocyte numbers and promotes maturation of erythroid precursors. Luspatercept binds with GDF11 and inhibits Smad2/3 signaling. Luspatercept can be used for the research of anemia[1].
A novel potent soluble guanylate cyclase (sGC) activator; reduces progression of renal damage in the ZSF1 rat, shows the potential as an effective therapy for diabetic nephropathy.
Glimepiride-d4-1 is deuterium labeled Glimepiride. Glimepiride (Glimperide) is a medium-to-long acting sulfonylurea anti-diabetic compound with an ED50 of 182 μg/kg.
4'-Deoxyphlorizin is an inhibitor of the glucose transport system. 4'-Deoxyphlorizi has good phlorizin hydrolase inhibitory activity with the Km value of 0.59 nM and the Ki value of 0.33 nM, respectively[1].
AZD8329 is a potent 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 9 nM for human 11β-HSD1, displays excellent selectivity versus 11β-HSD2, 17β-HSD1 and 17β-HSD3[1].
CYM-5520 is a selective and allosteric sphingosine 1-phosphate receptor 2 (S1PR2) agonist with an EC50 of 480 nM. CYM-5520 does not activate S1PR1, S1PR3, S1PR4 and S1PR5 receptors. CYM-5520 can co-bind in the S1PR2 receptor with S1P. CYM-5520 can be used for osteoporosis research[1][2].
SCH 39166 hydrobromide (SCH391660) is potent and selective antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. SCH 39166 hydrobromide shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). SCH 39166 hydrobromide can be used for the research of schizophrenia, cocaine addition, and obesity[1].
Ethyl tosylcarbamate is an intermediate in the synthesis of Gliclazide (G409877)[1][2]. Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM[3].
Lithocholic acid-d4 (3α-Hydroxy-5β-cholanic acid-d4) is the deuterium labeled Lithocholic acid, which is a toxic secondary bile acid[1].
Lapaquistat-d9 acetate (TAK-475-d9) is the deuterium labeled Lapaquistat acetate. Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor, blocking the conversion of farnesyl diphosphate (FPP) to squalene in the cholesterol biosynthesis pathway[1]. Lapaquistat acetate is effective at lowering low-density lipoprotein cholesterol, but it might cause liver damage. Lapaquistat acetate is used for hypercholesterolemia and mevalonate kinase deficiency (MKD) research[2].
GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9. GW1100 acts as a GPR40 inverse agonist.
Pomalidomid-C6-PEG3-butyl-N3 is a click chemistry reagent containing an azide group. Pomalidomid-C6-PEG3-butyl-N3 also is a crosslinker-E3 ligase ligand conjugate, which be used in click reactive protein degrader building block for PROTAC research.Pomalidomid-C6-PEG3-butyl-N3 also can be used in the template for synthesis of targeted protein degrader[1].
AP20187 is a cell-permeable ligand used to dimerize FK506-binding protein (FKBP) fusion proteins and initiate biological signaling cascades and gene expression or disrupt protein-protein interactions.
8-Dehydrocholesterol elevated concentration is one of the diagnostic biochemical hallmarks of classical Smith-Lemli-Opitz syndrome (SLOS).