Tonlamarsen is a angiotensinogen synthesis reducer, with antihypertensive activity[1].
Triptophenolide is a colorless crystalline plate isolated from ethyl acetate extracts of Tripterygium wilfordii. IC50 value:Target:In vitro: Triptophenolide can remarkably inhibit the delayed type hypersensitivity (DTH) reaction induced by DNCB and BSA; and diminished the peripheral blood ANAE+lymphocytes in rats and micc. Moreover, triptophenolide can dramatically increase the amount of total serum complement and significautly decrcase the serum antibody products (1gG ) of rats and mice. The phagocytosis of perioneal exudate macrophages in mice present double effects in vitro [1].In vivo:
Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity. Protein kinase C (PKC) is involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins[1][2].
Piperilate (Pipethanate) is one of the mixtures of hetrazepine derivative PAF antagonists with anticholinergics, can be used for bronchial asthma research. Piperilate also causes hypotension and rescues mice poisoned by the organophosphates[1][2][3].
Iguratimod is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC50 of 20 μM (7.7 μg/mL), but shows no effect on COX-1. Iguratimod also inhibits macrophage migration inhibitory factor (MIF) with an IC50 of 6.81 μM.
Benzyl(2R)-3-N,N-dibenzylamino-2-fluoropropanoate-13C3 is a 13C-labeled and deuterium labeled Benzyl(2R)-3-N,N-dibenzylamino-2-fluoropropanoate[1].
Imiloxan hydrochloride is a potent and selective alpha 2B-adrenoceptor antagonist. Imiloxan hydrochloride has the potential for acute kidney injury research[1][2].
2-Nitrophenyl β-D-glucopyranoside is a substrate for β-glucosidase. 2-Nitrophenyl β-D-glucopyranoside can be used to test β-glucosidase activity[1][2].
AZD2858 is a potent, orally active GSK-3 inhibitor, with IC50s of 0.9 and 5 nM for GSK-3α and GSK-3β, respectively, used in the research of fracture healing.
HDAC-IN-44 is a HDAC inhibitor with the IC50 value of 61.2 nM. HDAC-IN-44 shows high anticancer activity towards multiple cancer cell lines[1].
Bisdemethoxycucurmin (p,p'-Dihydroxydicinnamoylmethane), a curcuminoid, has antioxidant and antiinflammatory activities[1][2].
WM382 is an orally active and potent dual plasmepsin IX/X (PMIX/X) inhibitor with IC50 values of 1.4 nM and 0.03 nM, respectively. WM382 has robust in vivo efficacy at multiple stages of the malaria parasite life cycle and an excellent resistance profile[1][2][3].
L-DOPA (Levodopa) sodium is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA sodium can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA sodium has anti-allodynic effects, and can be used for Parkinson's disease research[1][2][3].
Moexipril is an orally active and potent angiotensin-converting enzyme (ACE) inhibitor. Moexipril can readily penetrate lipid membranes and thus target plasma and tissue ACE. Moexipril may improve endothelial dysfunction and exert neuroprotective effects. Moexipril can used for cardiovascular disease research[1][2].
IDD388 is a potent aldose reductase (ALR2 or AKR1B1) inhibitor with IC50 of 0.4 uM, shows weak inhibition for AKR1B10 (IC50=4.4 uM).
9-β-D-Arabinofuranosylguanine is a Guanosine (HY-N0097) analog and shows high affinity for deoxyguanosine kinase (dGK) with a Km of 8.0 μM. 9-β-D-Arabinofuranosylguanine can be used for the research of T-cell lymphoblastic disease[1][2].
H-D-Phe(4-F)-OH.HCl is a phenylalanine derivative[1].
Pinatuzumab is a CD22 monoclonal antibody. Pinatuzumab targets the cell-surface antigen CD22. Pinatuzumab can be used for synthesis of antibody drug conjugates (ADCs) to research several diseases including non-Hodgkin lymphoma (NHL)[1][2].
eIF4A3-IN-18 (compound 74) is a silvestrol (HY-13251) analogue. eIF4A3-IN-18 interferes the assembling of eIF4F translation complex with EC50 values of 0.8, 35 and 2 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-18 also has cytotoxicity to RMPI-8226 cells with an LC50 of 0.06 nM. eIF4A3-IN-18 can be used for the research of human cancer pathogenesis[1].
Gadopentetic acid (Gd-DTPA) is an paramagnetic contrast agent commonly implemented by a bolus intravenous injection (i.v.) in Dynamic contrast-enhanced MRI (DCE-MRI) studies. The initial concentration of Gadopentetic acid (Gd-DTPA) in the plasma ([Gd-DTPA0]) is an important parameter for DCE-MRI. [Gd-DTPA0] is related to the administered bolus dose and varies with subjects. A bolus of 0.025 mmol/kg Gd-DTPA offers shorter acquisition time and less exposure of subjects, with a half-life of 37.3 mins, a mean residence time of 53.8 mins, and an AUC of 3.37 ± 0.47 mmol/min/L[1].
Sulamserod is a 5-HT4 receptor antagonist, with antiarrhythmic activities.
Emetine dihydrochloride hydrate is an anti-protozoal drug previously used for intestinal and tissue amoebiasis.
Favezelimab (MK-4280) is a humanized anti-LAG-3 monoclonal antibody that blocks the interaction between LAG-3 and its ligand MHC class II. Favezelimab has the potential for colorectal cancer (CRC) research combined with the PD-L1 inhibitor Pembrolizumab (HY-P9902)[1][2].
PF-04937319 is a glucokinase activator (GKA) with EC50 value of 154.4 μM, one of the most promising strategies for the treatment of type 2 diabetes mellitus[1].PF-04937319 is designed to maintain glucose-lowering efficacy while mitigating the risk of hypoglycaemia observed with many other GKAs[2].
Lucinactant is a novel synthetic peptide that functionally mimics surfactant protein B, a protein with anti-inflammatory properties. Lucinactant is a KL4-Surfactant, protects human airway epithelium from hyperoxia[1][2][3].
3-Pyridylacetic acid-d4 (hydrochloride) is the deuterium labeled 3-Pyridylacetic acid hydrochloride[1]. 3-Pyridineacetic acid hydrochloride is a higher homologue of nicotinic acid, a breakdown product of nicotine (and other tobacco alkaloids)[2][3].
Arecaidine hydrochloride, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrochloride is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake[1][2].
NBD-557 is a potentially HIV-1 inhibitor.IC50 Value: Target: HIVNBD-557, is small molecule organic compounds with drug-like properties. It showed potent cell fusion and virus-cell fusion inhibitory activity at low micromolar levels. A systematic study showed that NBD-557 target viral entry by inhibiting the binding of HIV-1 envelope glycoprotein gp120 to the cellular receptor CD4 but did not inhibit reverse transcriptase, integrase, or protease, indicating that they do not target the later stages of the HIV-1 life cycle to inhibit HIV-1 infection. NBD-557 potent inhibitors of both X4 and R5 viruses tested in CXCR4 and CCR5 expressing cell lines, respectively, indicating that its anti-HIV-1 activity is not dependent on the coreceptor tropism of the virus. A surface plasmon resonance study, which measures binding affinity, clearly demonstrated that NBD-557 bind to unliganded HIV-1 gp120 but not to the cellular receptor CD4. NBD-557 was active against HIV-1 laboratory-adapted strains including an AZT-resistant strain and HIV-1 primary isolates, indicating that NBD-557 can potentially be further modified to become potent HIV-1 entry inhibitors.
Promegestone (R-5020), a progestin, is a potent progesterone receptor (PR) agonist. Promegestone has the potential for endocrine regulation and cancer research[1].
D-Glucuronamide is the derivate of D-glucuronic acid[1].