Macitentan is an orally active, non-peptide endothelin receptor antagonist for the treatment of idiopathic pulmonary fibrosis and pulmonary arterial hypertension.
2,3-Dimethoxybenzaldehyde (o-Veratraldehyde) is a benzaldehyde analog, with high antifungal activity (MIC=2.5 mM) 2,3-Dimethoxybenzaldehyde (o-Veratraldehyde) could be used for the synthesis of berberine[1].
Vanillylmandelic acid is the endproduct of epinephrine and norepinephrine metabolism. Vanillylmandelic acid can be used as an indication of the disorder in neurotransmitter metabolism as well. Vanillylmandelic acid has antioxidant activity towards DPPH radical with an IC50 value of 33 μM[1].
2-PAT, an analogue of Rasagiline and Selegiline, a reversible MAO-A inhibitor with an IC50 of 0.721 µM. 2-PAT is an inactivator of MAO-B with an IC50 of 14.6 µM. 2-PAT has the potential for Parkinson’s disease and depression research[1].
Glucocorticoid receptor-IN-2 (Compound WX019) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-2 exhibits very good transcriptional repressive activity with an IC50 of 0.171 nM against hMMP1, and comparable transcriptional activation activity with an EC50 of 0.94 nM against MMTV[1].
1-Bromoheptane-d3 is the deuterium labeled 1-Bromoheptane[1].
(S)-2-(tert-butoxycarbonylamino)-3-(4-carbamoyl-2,6-dimethylphenyl)propanoic acid is a phenylalanine derivative[1].
N-Feruloyloctopamine, isolated from Garlic skin, is an antioxidant constituent. N-Feruloyloctopamine significantly decreases the phosphorylation levels of Akt and p38 MAPK[1].
Omeprazole sulfone is a metabolite of Omeprazole, which is a proton pump inhibitor.
A12B4C3 is a potent human polynucleotide kinase/phosphatase (hPNKP) inhibitor with an IC50 value of 0.06 μM. A12B4C3 has antiproliferative activity against cancer cells. A12B4C3 can also enhance the radiosensitivity of certain cancer cells[1].
Domvanalimab (AB154) is an anti-TIGIT humanized monoclonal antibody. Domvanalimab binds human TIGIT9 and blocks the TIGIT-CD155 interaction. Domvanalimab can be used in research of cancer[1].
?PKC(85–92),Myristoylated is a cell permeable myristic acid conjugated PKC? peptide activator that enhances NO release in cultured human umbilical vein endothelial cells (HUVECs)[1].
UPF-648 sodium salt 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].
H-Gly-Leu-Phe-OH (GLF), an immunostimulatory tripeptide derived from α-lactalbumin, inhibits anticancer agent Etoposide-induced alopecia, epidermal thickening, and thinning of the adipocyte layer[1].
Cimetropium Bromide is a mAChR antagonist for long-term treatment of irritable bowel syndrome.
(2S)-5-Methoxyflavan-7-ol (compound 2) is a nature product that could be isolated form Dragon's blood resin[1].
Cyclohexanoyl coenzyme A is the active form of cyclohexane carboxylic acid (CHC) from anaerobic degradation in Rhodopseudomonas palustris[1].
Trilepisflavan is a flavan, which can be isolated from Trilepisium madagascariense. Trilepisflavan derivates serval analogues with anti-cancer activity against human cancer cells[1][2].
Oxethazaine-d6 (Oxetacaine-d6) is the deuterium labeled Oxethazaine. Oxethazaine (Oxetacaine), a precursor of phentermine acidic, is an acid-resistent and orally active analgesic agent. Oxethazaine (Oxetacaine) has the potential for the relief of pain associated with peptic ulcer disease or esophagitis[1][2].
MMP-9/MMP-13 Inhibitor I is a potent MMP-9 and MMP-13 inhibitor with IC50s of both 0.9 nM. MMP-9/MMP-13 Inhibitor I shows >20-folds selectivity for MMP-9/MMP-13 over other MMPs[1].
EC330 is a leukemia inhibitory factor (LIF) inhibitor.
Asthma relating compound 1 is an anti-asthmatic agent candidate extracted from patent EP0295656A1.
Dirucotide (MBP8298) is a synthetic peptide that consists of 17 amino acids linked in a sequence identical to that of a portion of human myelin basic protein. Dirucotide can be used for the research in autoimmune disorder of the central nervous system, such as Multiple sclerosis (MS)[1].
Sograzepide (Netazepide;YF476) is a gastrin/cholecystokinin 2 receptor (CCK2) antagonist.
Apigenin-4'-α-L-rhamnoside is a potent inhibitor of HBV. Apigenin-4'-α-L-rhamnoside inhibits the secretory level of HBV surface antigen (HBsAg) in HepG2.2.15 cells[1].
360A iodide is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.
Captopril disulfide is a metabolite of Captopril with antihypertensive activity[1].
FPH1(BRD-6125) increases the number and activity of primary human hepatocytes in vitro and promotes the differentiation of iPS cells towards a hepatic lineage[1].
Astressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B antagonizes CRF2-mediated inhibition of gastric emptying[1][2][3].
TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death[1].