Lobeglitazone is a new type of thiazolidinedione. Lobeglitazone can be used to prevent type 2 diabetes mellitus (T2DM)[1].
UPF-648 is a potent kynurenine 3-monooxygenase (KMO) inhibitor; exhibits highly active at 1 uM (81 ± 10% KMO inhibition); ineffective at blocking KAT activity.IC50 value: 1 uM(81 ± 10 % inhibition) [1]Target: KMO inhibitorin vitro: BFF 122 inhibited KAT activity almost completely at both 1 and 0.1 mM. The effect was still remarkable at 0.01 mM (70 ± 1 % inhibition). At the same three concentrations, BFF 122 did not affect KMO activity significantly. In contrast, UPF 648 totally blocked KMO at 0.1 and 0.01 mM and was still highly active at 0.001 mM (81 ± 10 % inhibition), but the compound was essentially ineffective at blocking KAT activity [1]. UPF 648 binds close to the FAD cofactor and perturbs the local active-site structure, preventing productive binding of the substrate l-kynurenine. Functional assays and targeted mutagenesis reveal that the active-site architecture and UPF 648 binding are essentially identical in human KMO, validating the yeast KMO-UPF 648 structure as a template for structure-based drug design [3].in vivo: Applying an identical experimental design, separate rats were used to study the effect of KMO inhibition on the de novo synthesis of KP metabolites in the lesioned striatum. These animals were bilaterally injected with 0.1 mM UPF 648 and 3H-kynurenine in PBS. 0.1 mM UPF 648 significantly reduced the neosynthesis of 3-HK and QUIN in the lesioned striatum (by 77 % and 66%, respectively) and moderately (27%) but significantly increased the de novo formation of KYNA [1]. Administered to pregnant rats or mice on the last day of gestation, UPF 648 (50 mg/kg, i.p.) produced qualitatively similar changes (i.e., large increases in kynurenine and KYNA and reductions in 3-HK and QUIN) in the brain and liver of the offspring. Rat pups delivered by UPF 648-treated mothers and immediately exposed to neonatal asphyxia showed further enhanced brain KYNA levels [2]. UPF 648, has an IC50 of 20 nM and provides protection against intrastriatal QUIN injections in kynurenine aminotransferase (KAT II) deficient mice. UPF 648 treatment also shifts KP metabolism towards enhanced neuroprotective KYNA formation [3].
Anivamersen sodium is an RNA aptamer to reverse the anticoagulant effect of the parenteral factor IXa inhibitor pegnivacogin. REG1 is a novel anticoagulation system consisting of pegnivacogin, an RNA aptamer inhibitor of coagulation factor IXa, and anivamersen, a complementary sequence reversal oligonucleotide.
Scholaricine (compound 13 ) is an alkaloid isolated from the leaf and stem-bark extracts of Alstonia spatulata. Scholaricine reverse multidrug resistance in vincristine-resistant KB cells with an IC50 value of 13.35 μM[1].
MrgprX2 antagonist-3 is an MrgprX2 antagonist extracted from patent WO2021092240A1, example E117. MrgprX2 antagonist-3 can be used for the research of inflammatory disorders of the skin[1].
5-FAM-Amylin (human) is a biologically active peptide.
Dihydrojasmonic acid is a plant growth regulator[1].
Phosphoenolpyruvate carboxylase (PEPC) is a carbon dioxide fixing enzyme that in an irreversible manner and in the presence of Mg2+, converts phosphoenolpyruvate and bicarbonate into oxaloacetate and inorganic phosphorus. Phosphoenolpyruvate carboxylase catalyses the primary assimilation of CO(2) in Crassulacean acid metabolism plants. Phosphoenolpyruvate carboxylase plays a major role in setting the day-night pattern of metabolism in plants[1][2].
14-Benzoylneoline is found in Aconitum subcuneatum[1].
Tinospinoside C is a bioactive?clerodane diterpene glycoside compound. Tinospinoside C shows inhibitory activities of NO production with an IC50 value of 218 μM[1].
ERα antagonist 1 (Compound 19d) is a potent, selective, covalent estrogen receptor α (ERα) antagonist. ERα antagonist 1 induces apoptosis and cell cycle G0/G1 phase arrest in MCF-7 cells[1].
Orsellinic acid is a compound produced by Lecanoric acid treated with alcohols. Lecanoric acid is a lichen depside isolated from a Parmotrema tinctorum specimen[1].
Ipfencarbazone is a substance being developed for the control of weeds such as watergrass in rice; herbicide agent.
Phthalic acid bis(3,7-dimethyloctyl) ester-d4 is the deuterium labeled Phthalic acid bis(3,7-dimethyloctyl) ester[1].
Polyoxypropylene stearyl ether can be used as an excipient, such as surfactant, softener, lubricating, wetting, plasticizing, solubilizing and dispersing properties. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs[1].
JHU395 is an orally-bioavailable and a plasma stable lipophilic glutamine antagonists (GA) prodrug. JHU395 delivers 6-diazo-5-oxo-L-norleucine (DON) to malignant peripheral nerve sheath tumor (MPNST) in vitro and in vivo, and has antitumor activity in MPNST[1].
5,7-Dimethoxy-2,2-dimethylchromene is a synthetic precocenoid, has potential insect control function. 5,7-Dimethoxy-2,2-dimethylchromene induces loss of pigmentation in hatching larvae of shield bug (Eurgaster integriceps)[1][2].
Fargesin is a bioactive neolignan isolated from magnolia plants，with antihypertensive and anti-inflammatory effects[1][2][3].
P-BP-SFAC is a fluorescence molecule. P-BP-SFAC exhibits an apparent absorption band with a peak at about 377 nm, indicative of a stronger ICT effect[1].
Butibufen is a non-steroidal compound. Butibufen shows analgesic and antipyretic properties. Butibufen can be used for the research of inflammation[1][2].
H-Ser-Gln-OH is a biologically active peptide.
Brevianamide F , also known as cyclo-(L-Trp-L-Pro), belongs to a class of naturally occurring 2,5-diketopiperazines.Brevianamide F possess interesting breast cancer resistance protein inhibitory activity.[1] brevianamide F once used as aromatic substrate. [2]
Milpocitide is a low-density lipoprotein receptor (human LDL receptor, LDLR), (293-333)-peptide fragment (EGF-like domain 1)[1].
3-Keto petromyzonol, a main component of Sea lamprey male sex pheromones, modulates both synthesis and release of gonadotropin releasing hormone (GnRH), and subsequently, hypothalamic-pituitary-gonadal (HPG) output in immature sea lamprey[1].
Dimethyl pimelate-d4 is the deuterium labeled Dimethyl pimelate[1].
α-Lactose (α-D-Lactose) is the major sugar present in milk. Lactose exists in the form of two anomers, α and β. The α form normally crystallizes as a monohydrate[1][2].
Terbutryn-d5 is the deuterium labeled Terbutryn[1].
Uridylate kinase is a member of the nucleoside mono-phosphate (NMP) kinase family and catalyzes the reaction ATP+NMP?ADP+NDP with moderate specificity for UMP[1].
Antioxidant agent-4 (Compound 2) is an effective antioxidant molecule with antilipid peroxidative activity[1].
Polzastobart (JTX-8064) is a humanized IgG4 monoclonal antagonist antibody that selectively binds LILRB2 and prevents it from binding its ligands, classical and non-classical MHC I molecules. Polzastobart enhances pro-inflammatory cytokine production in macrophages by blocking the ability of LILRB2 to bind HLA-A/B and/or HLA-G, a marker of immunotolerance on cancer cells. Polzastobart is a macrophage immune checkpoint inhibitor[1].