9-[2'-O-Acetyl-3'-azido-3'-deoxy-5'-O-toluoyl-b-L-ribofuranosyl)-6-chloropurine 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].
N-5984 (KRP-204) is a potent and selective agonist of β3-adrenergic receptor. N-5984 has the potential for developing as one of the clinically effective drugs for obesity and diabetes mellitus[1].
Raltegravir is a potent integrase (IN) inhibitor, used to treat HIV infection.
AMG-1694 is a potent glucokinase–glucokinase regulatory protein (GK-GKRP) disruptors and promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, indirectly increasing GK enzymatic activity. AMG-1694 potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation. AMG-1694 normalizes blood glucose levels in several rodent models of diabetes and lowes blood glucose restricted to diabetic and not normoglycaemic animals[1].
Autophinib is a potent autophagy inhibitor, which can inhibit autophagy induced by starvation or rapamycin by targeting the lipid kinase VPS34 with IC50s of 90, 40 and 19 nM, respectively.
Ethyl chrysanthemate is an allelochemical compound used as an attractant[1].
Stem bromelain (EC 3.4.22.32) is a cysteine proteinase, isolated from pineapple (Ananas comosus) stem. Stem bromelain is a major bromelain, which exhibits various fibrinolytic, antiedematous, antithrombotic, and anti-inflammatory activities. Stem bromelain has in vivo antitumoral and antileukemic activity, as well as antimetastatic action[1][2].
Yohimbine hydrochloride is an alpha 2-adrenoreceptor antagonist, blocking the pre- and postsynaptic alpha-2 adrenoreceptors and causing an increased release of noradrenaline and dopamine.IC50 value:Target:In vitro:In vivo: Yohimbine hydrochloride (0.2 mg/kg, i.p.) was administered to rats 1h before the stress session daily for 14 consecutive days and its effect was assessed. Results of this section revealed that, immersion of rats in cold water significantly decreased sexual arousal and motivation as indicated by increased latencies and intervals. Decreased copulatory activity was confirmed by decreased testosterone, luteinizing hormone (LH) and follicle-stimulating-hormone (FSH) levels as well as decreased cholesterol content in rat testes. Treatment with yohimbine significantly increased the sexual arousal and potency and corrected the effects induced by stress on the mating behavior of male rats [1].
Lenvervimab (GC1102) is a IgG1-type recombinant human hepatitis B Immunoglobulin. Lenvervimab can be used for research of hepatitis B virus infection[1][2].
1,5-Anhydrosorbitol-13C is the 13C labeled 1,5-Anhydrosorbitol. 1,5-Anhydrosorbitol is a short-term marker for glycemic cont[1][2].
NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a Gsα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs[1][2].
Lapachol is a naphthoquinone that was first isolated from Tabebuia avellanedae (Bignoniaceae). Lapachol shows anti-infection and antitumor activity[1]
Vortioxetine is a inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
19-methyleicosanoic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Luliconazole(NND 502) is an azole antifungal indicated for the topical treatment of interdigital tinea pedis.IC50 Value: Target: AntifungalLuliconazole is an antifungal that belongs to the azole class. Although the exact mechanism of action against dermatophytes is unknown, luliconazole appears to inhibit ergosterol synthesis by inhibiting the enzyme lanosterol demethylase. Inhibition of this enzyme’s activity by azoles results in decreased amounts of ergosterol, a constituent of fungal cell membranes, and a corresponding accumulation of lanosterol. In a fertility study in rats, subcutaneous doses of 1, 5 and 25 mg/kg/day luliconazole were administered prior to and during mating and through early pregnancy. Treatment related effects on reproductive function were noted in females (decreased live embryos and decreased corpus luteum) at 5 and 25 mg/kg/day and males (decreased sperm counts) at 25 mg/kg/day. No treatment related effects on fertility or reproductive function were noted at 1 mg/kg/day (0.1X MRHD based on BSA comparisons).
Vatiquinone is a potent cellular oxidative stress protectant, which could be used to treat mitochondrial diseases.
Rentiapril racemate is the racemate of Rentiapril. Rentiapril is an angiotensin converting enzyme (ACE) inhibitor.
Digoxigenin bisdigitoxoside is an anticancer drug. Digoxigenin bisdigitoxoside is cytotoxic[1].
2'-OMe-Ac-C Phosphoramidite is a modified phosphoramidite and can be used for the oligonucleotide synthesis.
Tetra-n-propyl-ammonium-d28 (bromide) is the deuterium labeled Tetra-n-propyl-ammonium bromide[1].
Protosappanin B is a phenolic compound extracted from Lignum Sappan. Anti-cancer activity[1]. Protosappanin B induces apoptosis and causes G1 cell cycle arrest in human bladder cancer cells[2].
TC-S 7005 is a Polo-like kinases (Plks) inhibitor with IC50s of 4 nM, 24 nM and 214 nM for Plk2, Plk3, and Plk1, respectively[1].
CXCR4 antagonist 6 (compound 46) is a potent CXCR4 antagonist with an IC50 value of 79 nM. CXCR4 antagonist 6 inhibits CXCL12 induced cytosolic calcium flux (IC50 = 0.25 nM). CXCR4 antagonist 6 significantly mitigates CXCL12/CXCR4 mediated cell migration. CXCR4 antagonist 6 exhibits marked efficacy in a cancer metastasis model in mice[1].
INCB 3284 is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 can be used in the research of acute liver failure.
Lipoxamycin hemisulfate is an antifungal antibiotic and a potent serine palmitoyltransferase inhibitor with an IC50 of 21 nM[1][2].
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].
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].
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].
Pyridoxine-d5 (Pyridoxol-d5) is a deuterium labeled Pyridoxine (HY-B1328). Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.