Amphotericin A is a potent antifungal antibiotic[1].
(αR)-α-[[(1,1-Dimethylethoxy)carbonyl]amino]benzeneacetic acid is a Glycine (HY-Y0966) derivative[1].
Olanexidine is an antibacterial agent. Olanexidine is active against a wide range of bacteria, imcluding both Gram-positive and Gram-negative bacteria Olanexidine is also an antiseptic. Olanexidine can be used in the research of infection and inflammation[1][2][3].
TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists[1].
Hypocretin (70-98), human is a polypeptide that is capable of binding to an orexin receptor OX1R and promotes Apoptosis[1].
Trimetrexate (CI-898) isethionate is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate isethionate can also inhibit the growth of various cancer cells. Trimetrexate isethionate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer[1][2][3][4][5].
Diphenylterazine is a bioluminescence agent.
HPB (HDAC6 inhibitor HPB) is a selective HDAC6 inhibitor with an IC50 of 31 nM. HPB exhibits >30-flod selectivity for HDAC6 over HDAC1[1].
Indecainide hydrochloride is a potent and orally active class I local anesthetic antiarrhythmic agent[1].
Propionylglycine is a peptide[1].
MDM2-p53-IN-16 is a MDM2-p53 complex inhibitor with an IC50 value of 4.3 nM to dissociate human p53/MDM2 complex. MDM2-p53-IN-16 reactivates p53, and induces Glioblastoma Multiforme (GBM) cell apoptosis and cell-cycle arrest. MDM2-p53-IN-16 can be used for the cancer research[1].
Yubeinine is an alkaloid, isolated from the bulbs of Fritillaria yuminensis[1].
Rivanicline (RJR-2403) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM).IC50 value: 26 nM [1]Target: α4β2 nAChRin vitro: At concentrations up to 1 mM, Rivanicline does not significantly activate nAChRs in PC12 cells, muscle type nAChRs or muscarinic receptors. Dose-response curves for agonist-induced ileum contraction indicate that Rivanicline is less than one-tenth as potent as nicotine with greatly reduced efficacy. Rivanicline does not antagonize nicotine-stimulated muscle or ganglionic nAChR function (IC50 > 1 mM). Chronic exposure of M10 cells to Rivanicline (10 microM) results in an up-regulation of high-affinity nAChRs phenomenologically similar to that seen with nicotine [1].in vivo: Rivanicline significantly improved passive avoidance retention after scopolamine-induced amnesia and enhanced both working and reference memory in rats with ibotenic acid lesions of the forebrain cholinergic projection system in an 8-arm radial maze paradigm. By comparison, Rivanicline was 15 to 30-fold less potent than nicotine in decreasing body temperature, respiration, Y-maze rears and crosses and acoustic startle response [2]. Metanicotine was about 5-fold less potent than nicotine in the tail-flick test after s.c administration, but slightly more potent after central administration [3].
Trigonelline chloride, an alkaloid with potential antidiabetic activity, is present in considerable amounts in coffee.
Fluindione is a inhibitor of 5-lipoxygenase with the IC50 of 15 μM. Fluindione has antiinflammatory activity[1].
(2S,3S)-2-Acetamido-3-methylpentanoic acid is an isoleucine derivative[1].
Antifungal agent 2 is a broad-spectrum fungal inhibitor which inhibits growth of pertinent species of Candida, Cryptococcus, and Aspergillus at a concentration as low as 0.5 μg/mL.
Deoxynivalenol, a mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors[1].
Tamsulosin is a selective α1 receptor antagonist.Target: α1 receptorTamsulosin is a selective α1 receptor antagonist that has preferential selectivity for the α1A receptor in the prostate versus the α1B receptor in the blood vessels. Tamsulosin-treated patients had a 0.30-fold lower risk of developing acute urinary retention compared with control patients. None of the International Continence Society male questionnaire domain scores showed significant changes between the groups [1]. tamsulosin can be recommended for treating men after catheterization for AUR, and can reduce the likelihood of the need for re-catheterization [2].
ERK5-IN-6 (compound 5J) is an ERK5 kinase inhibitor with anticancer activity. ERK5-IN-6 exhibits good anti-proliferative activity with the IC50 value of 4.56 µg/mL for A549 cells[1].
Benzthiazide is a long-acting diuretic[1] and a hypertension agent. Benzthiazide is an inhibitor of carbonic anhydrase 9 (CA9), with Kis of 8.0, 8.8 and 10 nM for CA9, CA2 and CA1, respectively. Benzthiazide also suppresses proliferation of cancer cells[2].
Tumulosic acid, a triterpenoid, inhibits KLK5 protease activity (IC50= 14.84 μM). Tumulosic acid suppresses the proteolytic processing of LL-37 in keratinocytes at ≤10 μM[1].
β-Damascone is an aroma active rice volatile and is widely used in perfume compositions. β-Damascone has also received certain attention as a potential cancer chemopreventive and a mosquito and muscoid insecticide[1][2].
3-O-Feruloyl-6′-O-(4-O-β-D-glucopyranosylferuloyl)sucrose is a natural compound that can be isolated from Lilium henryi Baker [1].
Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[1][2][3].
GK56 is a carboxyl nicotine hapten, which contains a linker attached to the 6-position of nicotine. GK56 conjugates to KLH via carbodiimide-mediated reactions[1].
Ibuprofen ((±)-Ibuprofen) sodium is an orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen sodium inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen sodium is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen sodium can be used in the research of pain, swelling, inflammation, infection, immunology, cancers[1][2][5][8].
Methenamine hippurate (Hexamine hippurate) is an orally active urinary antiseptic agent with a wide antibacterial spectrum. Methenamine hippurate is effective against most common urinary tract pathogens[1][2].