3β-Acetoxyurs-12-en-11-one is a ursane triterpenoid with antimicrobial activity, can be isolated from the stem bark of Morus mesozygia and the leaves of Ficus hirta Vahl (Moraceae)[1][2].
7-Hydroxyflavanone is an aromatase (cytochrome P450 19; CYP19) inhibitor with an IC50 of 65 μM[1].
Rhodamine 6G is a rhodamine analog useful in Pgp efflux assays. It can be used in characterizing the kinetics of MRP1- mediated efflux, and as a laser dye and potential mitochondrial probe.
Benzyl-L-serine is a serine derivative[1].
Ditiocarb sodium (Sodium diethyldithiocarbamate) is an accelerator of the rate of copper cementation. Sodium diethyldithiocarbamate reduces the incidence of HIV infection.
Duloxetine hydrochloride is a serotonin-norepinephrine reuptake inhibitor (SNRI) with Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).Target: SNRIDuloxetine (sold under the brand names Cymbalta, Ariclaim, Xeristar, Yentreve, Duzela, Dulane) is a serotonin-norepinephrine reuptake inhibitor(SNRI) manufactured and marketed by Eli Lilly. It is prescribed for major depressive disorder and generalized anxiety disorder (GAD). Duloxetine also has approval for use in osteoarthiritis and musculoskeletal pain. Duloxetine failed the US approval for stress urinary incontinence amidst concerns over liver toxicity and suicidal events; however, it was approved for this indication in Europe, where it is recommended as an add-on medication in stress urinary incontinence instead of surgery. It can also relieve the symptoms of painful peripheral neuropathy, particularly diabetic neuropathy, and it is used to control the symptoms of fibromyalgia.The main uses of duloxetine are in major depressive disorder, general anxiety disorder, stress urinary incontinence, painful peripheral neuropathy,fibromyalgia, and chronic musculoskeletal pain associated with osteoarthritis and chronic lower back pain. It is being studied for various other indications.
Microstegiol is a diterpene that can be isolated from Salvia microstegia and the root of Zhumeria majdae[1].
Flurofamide is a potent bacterial urease inhibitor with potential clinical utility in the treatment of infection induced urinary stones[1].
Flucytosine (5-Fluorocytosine, 5-FC, Ancobon), a fluorinated pyrimidine analogue, is an antifungal drug.Target: antifungalFlucytosine, or 5-fluorocytosine, a fluorinated pyrimidine analogue, is a synthetic antimycotic drug. It is structurally related to the cytostatic fluorouracil and to floxuridine. It is available in oral and in some countries also in injectable form. A common brand name is Ancobon. Flucytosine was first synthesized in 1957 but its antifungal properties were discovered in 1964. The drug is dispensed in capsules of 250 mg and 500 mg strength. The injectable form is diluted in 250 mL saline solution to contain 2.5 g total (10 mg/mL). The solution is physically incompatible with other drugs including amphotericin B.Flucytosine is well absorbed (75 to 90%) from the gastrointestinal tract. Intake with meals slows the absorption, but does not decrease the amount absorbed. Following an oral dose of 2 grams peak serum levels are reached after approximately 6 hours. The time to peak level decreases with continued therapy. After 4 days peak levels are measured after 2 hours. The drug is eliminated renally. In normal patients flucytosine has reportedly a half-life of 2.5 to 6 hours. In patients with impaired renal function higher serum levels are seen and the drug tends to cumulate in these patients. The drug is mainly excreted unchanged in the urine (90% of an oral dose) and only traces are metabolized and excreted in the feces. Therapeutic serum levels range from 25 to 100 ?g/ml. Serum levels in excess of 100 ug are associated with a higher incidence of side effects. Periodic measurements of serum levels are recommended for all patients and are a must in patients with renal damage.
Boc-D-Phe(4-I)-OH is a phenylalanine derivative[1].
FM1-43, a styryl dye used to study endocytosis and exocytosis, behaves as a permeant blocker of the hair-cell mechanotransducer channel. FM1-43 also reduces the ototoxic effects of the aminoglycoside antibiotic neomycin sulfate[1].
Guanosine 5'-triphosphate (GTP), ammonium salt-d27 is the deuterium labeled Guanosine 5'-triphosphate (GTP), ammonium salt[1].
PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell.
ROCK1-IN-1 is a ROCK1 inhibitor with a Ki value of 540 nM. ROCK1-IN-1 can be used for the research of hypertension, glaucoma and erectile dysfunction[1].
Azide-PEG7-Tos is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
AMG 579 is a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A) with an IC50 of 0.1 nM.
Neuronostatin-13 human is a 13-amino acid peptide hormone encoded by the somatostatin gene and plays an important role in the regulation of hormonal and cardiac function.
5,6-trans-Travoprost is the inactive isomer of Travoprost (HY-B0584), and can be used as an experimental control. Travoprost (Fluprostenol isopropyl ester), an isopropyl ester proagent, is a high affinity, selective FP prostaglandin full receptor agonist. Travoprost has the ocular hypotensive efficacy and has the potential for glaucoma and ocular hypertension[1].
WAY-621089 is an active molecule for the study of amyloid diseases and synucleinopathies[1].
BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research[1][2][3][4].
Benzyl-PEG10-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Imiquimod hydrochloride is an immune response modifier that acts as a toll-like receptor 7agonist.
Sp-8-CPT-cAMPS, a cAMP analog, is a potent and selective activator of the cAMP-dependent protein kinas A (PKA I and PKA II). Sp-8-CPT-cAMPS selects site A of RI compares to site A of RII by 153-fold and site B of RII compares to site B of RI by 59-fold[1][2].
(+)-Mepivacaine is a racemic isomer of Mepivacaine (HY-B0517), which has analgesic and vasoconstrictive activity. Mepivacaine is an amide type agent that temporarily causes local loss of consciousness. Mepivacaine binds to specific voltage-gated sodium channels on neuronal cell membranes, inhibiting sodium influx and membrane depolarization[1].
Malvidin-3-galactoside chloride, an anthocyanin monomer, induces hepatocellular carcinoma (HCC) cells cycle arrest and apoptosis. Malvidin-3-galactoside chloride inhibits the production and accumulation of ROS. Malvidin-3-galactoside chloride has anti-tumor function[1].
L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92±0.03, 4.6±0.2, 3.9±0.2, 2.7±0.2, 4.0±0.2, and 3.94±0.08 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.
7-Xylosyl-10-Deacetyltaxol B (7-xylosyl-10-Deacetylpaclitaxel B) is a paclitaxel derivative derived from T. cuspidate. 7-Xylosyl-10-Deacetyltaxol B has anti-tumor activity and inhibits the growth of S180 sarcoma[1].
EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity[1].
3'-Methoxyflavonol is a selective agonist of neuromedin U 2 receptor (NMU2R).
Rescinnamine is a derivative of the indole alkaloid reserpine. Rescinnamine shows sedative effects. Rescinnamine can be used for hypertension research[1][2].