SIB-1553A hydrochloride is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A hydrochloride is also a selective neuronal nAChR ligand. SIB-1553A hydrochloride is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders[1][2].
Cromakalim is a potassium channel opener. Cromakalim can be used as a bronchodilator in asthma. Cromakalim inhibits the spontaneous tone of human isolated bronchi in a concentration-related manner being nearly as effective as isoprenaline or theophylline[1].
Balipodect (TAK-063) is a highly potent, selective and orally active PDE10A inhibitor with IC50 of 0.30 nM; >15000-fold selectivity over other PDEs.
Pomalidomide-7-NH2 is the Pomalidomide-based cereblon ligand used in the recruitment of CRBN protein. Pomalidomide-7-NH2 can be connected to the ligand for protein by a linker to form PROTACs[1].
Azido-PEG8-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
HAPSBC is an S-benzyl iron chelator that mobilizes intracellular 59Fe distribution[1].
3-epi-Maslinic acid is an acidic pentacyclic triterpene isolated from Hexane and dichloromethane extracts of Platostoma africanum P. Beauv[1].
Barusiban (FE-200440) is an oxytocin receptor (OT-R) antagonist (Ki=0.8 nM), inhibits OT-induced contraction. Barusiban can be used in preterm labor (PTL), in vitro fertilisation (IVF) and infertility research[1][2][3].
5,7,3',4'-Tetrahydroxy-3-methoxy-8-geranylflavone is a prenylflavone with anti-proliferation effect on breast cancer cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8-geranylflavone can be isolated from an ethyl acetate-soluble extract of the barks of Broussonetia papyrifera[1].
GSK-LSD1 Dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.
Fosfluconazole is a prodrug of Fluconazole that is widely used as an antifungal agent.
Neohesperidin dihydrochalcone is a synthetic glycoside chalcone, is added to various foods and beverages as a low caloric artificial sweetener.
Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
GGACK (H-Glu-Gly-Arg-CMK) is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor[1].
Petrolatum (white) is an ointment vehicle for many drugs, due to its low skin irritation. Petrolatum (white) can be used as an excipient, such as ointment base, lubricant, adhesive, viscous agent, excipient. 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][2].
pBD-1 is an endogenous and constitutively expressed antimicrobial peptide (AMP) from porcine tissues, particularly expresses in pig mucosal epithelial sites. pBD-1 has antimicrobial activities and contributes to mucosal and systemic host defenses in pigs[1].
Tafamidis(Fx1006A) is a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascade.Target: OthersTafamidis is a drug for the amelioration of transthyretin-related hereditary amyloidosis.Tafamidis functions by kinetic stabilization of the correctly folded tetrameric form of the transthyretin (TTR) protein. Tafamidis binds selectively and with negative cooperativity (K(d)s ~2 nM and ~200 nM) to the two normally unoccupied thyroxine-binding sites of the tetramer, and kinetically stabilizes TTR. Patient-derived amyloidogenic variants of TTR, including kinetically and thermodynamically less stable mutants, are also stabilized by tafamidis binding. The crystal structure of tafamidis-bound TTR suggests that binding stabilizes the weaker dimer-dimer interface against dissociation, the rate-limiting step of amyloidogenesis [1].
NG-012, potentiator of nerve growth factor (NGF), were isolated from the culture broth of Penicillium verruculosum F-4542. NG-012 potentiates the neurite outgrowth induced by NGF in rat pheochromocytoma cell line (PC12)[1].
2',4'-Dihydroxy-7-methoxy-8-prenylflavan (compound 6) is a compound isolated from a chloroform-soluble extract of dried Morus alba fruits[1].
Toddaculin is a natural coumarin that can induce differentiation and apoptosis in leukemic cells. Toddaculin suppresses excess osteoclast activity and enhances osteoblast differentiation and mineralization. Toddaculin also exhibits anti-inflammatory activity[1][2][3].
Nanrilkefusp alfa (SO-C101; SOT101) is fusion protein, is a selective and potent agonist fusion protein of IL-15 and IL-15Rα sushi+ domain. Nanrilkefusp alfa inhibits tumor by inducing proliferation and activation of memory CD8+ T cells, natural killer (NK) cells, γ/δ T cells and NKT cells. Nanrilkefusp alfa exhibits excellent anti-metastatic activity against melanoma and suppresses tumor growth in various mouse tumor models[1][2].
Evocarpine, a quinolone alkaloid that could be isolated from Evodiae fructus, inhibitss Ca2+ influx through voltage-dependent calcium channels. Antimycobacterial activity[1][2].
JW67 inhibits the canonical Wnt signaling with an IC50 of 1.17μM[1]. JW67 affects the multiprotein complex consisting of β-catenin/GSK-3β/AXIN/APC/CK1 that rapidly reduces active β-catenin with a subsequent downregulation of Wnt target genes. JW67 also inhibits colorectal cancer cell growth[1].
D,L-Buthionine-(S,R)-sulfoximine is a potent inhibitor of glutamylcysteine synthetase biosynthesis.
Liquiritin apioside, a main flavonoid component of licorice, possesses antitussive effects[1].
Pivalylbenzhydrazine (Pivhydrazine) is a potent monoamine oxidase (MAO) inhibitor. Pivalylbenzhydrazine decreases cartilage growth in normal rats. Pivalylbenzhydrazine can be used in research of depression[1].
Cinnamyl acetate has a wide application in the flavor and fragrance industry[1]. Cinnamyl acetate is a new broad spectrum antibacterial agent[2].
Teplizumab (MGA-031) is a Fc receptor non-binding anti-human CD3 monoclonal antibody. Teplizumab reduces the loss of beta-cell function. Teplizumab can be used in the research of type 1 diabetes[1][2].
S6 peptide is a potentially important lamin kinase. S6 peptide is involved in the process of cardiac hypertrophy induced by mechanical loading. S6 peptide can be activated by many kinds of growth factors[1].
Endokinin D is a human tachykinin and consist of 14 amino acid residues[1].