EXP3179 is an important intermediate aldehyde metabolite of Losartan. EXP3179 has no AT1-R–blocking activity, but potently inhibits the expression of endothelial cyclooxygenase (COX)-2. EXP3179 exerts potent anti-inflammatory actions[1].
NF864, a suramin analog, is a P2X1 receptor inhibitor.
Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10 μM[1][2].
N-Nitrosodibutylamine (N-Nitroso-di-n-butylamine) is a nitrosamine enriched in the drinking water[1].
Desmedipham is a selective systemic phenyl-carbamate herbicide. Desmedipham acts by disrupting CO2 fixation and the production of intermediary energy components-ATP and NADPH2 and inhibition of Hill reaction[1].
Tetrapeptide-21 is a bioactive peptide with anti-wrinkle and and reducing skin hyperpigmentation effect, and has been reported used as a cosmetic ingredient[1].
GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease[1].
MC-Val-Cit-PAB-rifabutin has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Val-Cit-PAB-rifabutin is used for the antibody-drug conjugates (ADC) that are effective and stable in vitro and in vivo to treat various diseases or disorders[1].
Telomestatin is a very potent telomerase inhibitor and can be isolated from Streptomyces anulatus 3533-SV4. Telomestatin selectively facilitates the formation of intramolecular G-quadruplexes, in particular, that produced from the human telomeric sequence d[T2AG3]4. Telomestatin is an ADC cytotoxin and can be used for cancer research[1].
Fexinidazole is a 5-nitroimidazole drug currently in clinical development for the treatment of human sleeping sickness (human African trypanosomiasis [HAT]), caused by infection with species of the protozoan parasite Trypanosoma brucei. Target: Antiparasiticin vivo: Fexinidazole shows dose-related efficacy in the T. b. rhodesiense (STIB900) acute mouse model at intraperitoneal (i.p.) doses of 20 to 50 mg/kg/day and oral (per os [p.o.]) doses of 25 to 100 mg/kg/day given on four consecutive days, with 100 mg/kg/day p.o. being 100% curative. Fexinidazole is shown to be effective in the GVR35 mouse model, which mimics the advanced and fatal stage of the disease, when parasites have disseminated into the brain. [1]
MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.
DMTr-dH2U-amidite is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
KRAS G12C inhibitor 34 is a KRAS G12C inhibitor extracted from patent WO2021239058A1, compound Z1. KRAS G12C inhibitor 34 can be used for the research of cancer[1].
Allocholic acid is a typically fetal bile acid found in vertebrates and reappears during liver regeneration and carcinogenesis. Allocholic acid is also a potent and specific stimulant of the adult olfactory system[1][2][3].
Glucagon hydrochloride (Porcine glucagon hydrochloride) is a peptide hormone, produced by pancreatic α-cells. Glucagon hydrochloride stimulates gluconeogenesis[1]. Glucagon hydrochloride decreases the activity of HNF-4[2]. Glucagon hydrochloride increases HNF4α phosphorylation[3].
Dynole 34-2 is a dynamin GTPase inhibitor (IC50s=6.9 and 14.2 µM for dynamin1 and dynamin2 GTPase activity, respectively) with antimitotic effect. Dynole 34-2 induces apoptosis, as revealed by cell blebbing, DNA fragmentation, and PARP cleavage[1]. Dynole 34-2 also potently inhibits receptor mediated endocytosis (RME)[2].
Z-D-His-OH is a histidine derivative[1].
Raloxifene Bismethyl Ether is a metabolite of Raloxifene and an estrogen receptor inactive compound on which both hydroxyl groups are absent[1].
H-4-Pal-OH is an alanine derivative[1].
Foretinib is a multi-target tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.
1,4-Dicaffeoylquinic acid (1,4-DCQA) is a phenylpropanoid from Xanthii fructus, inhibits LPS-stimulated TNF-α production[1].
Penta-alanine (Penta-L-alanine) is a petide. Penta-alanine can be used for neurological disease research[1][2].
BMS-986224 is a potent, selective and orally bioavailable APJ receptor agonist (Kd = 0.3 nM). BMS-986224 exhibits similar receptor binding and signaling profile to (Pyr1) apelin-13. BMS-986224 has the potential for the research of heart failure[1].
ACTH (2-24) (human, bovine, rat) is a peptide analogue of ACTH.
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer[1].
Coralyne chloride is a protoberberine alkaloid with potent anti-cancer activities. Coralyne chloride acts as a potent topoisomerase I poison and induces Top I mediated DNA cleavage[2]. Coralyne chloride can be used for preparing coralyne derivatives as DNA binding fluorescent probes[3].
MK-886 (L 663536) sodium salt is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 sodium salt is also a non-competitive PPARα antagonist and can induce apoptosis[1][2][3].
PMX 205 is a potent complement C5a receptor (C5aR; CD88) antagonist.
SPHINX is a selective SRPK1 inhibitor with an IC50 value of 0.58 μM. SPHINX effectively reduces Choroidal Neovascularization (CNV) in vivo. SPHINX can be used for the research of (age-related macular degenaration) AMD[1].
Guanylin (mouse, rat), a petide, is composed of 15 amino acids. Guanylin (mouse, rat) is an activator of intestinal guanylate cyclase. Guanylin (mouse, rat) can be used for the research of diarrhea[1].