DHPG ((RS)-3,5-DHPG) is an amino acid, which acts as a selective and potent agonist of group I mGluR (mGluR 1 and mGluR 5), shows no effect on Group II or Group III mGluRs[1]. DHPG ((RS)-3,5-DHPG) is also an effective antagonist of mGluRs linked to phospholipase D[2].
Linderaspirone A is a natural compound that can be isolated from the roots of Lindera aggregate. Linderaspirone A shows significant inhibitory effects on the production of prostaglandin E2 (PGE2),TNF-α, and IL-6 [1][2].
4-Hydroperoxy Cyclophosphamide-d4 is the deuterium labeled 4-Hydroperoxy cyclophosphamide. 4-Hydroperoxy cyclophosphamide is the active metabolite form of the prodrug Cyclophosphamide. 4-Hydroperoxy cyclophosphamide crosslinks DNA and induces T cell apoptosis independent of death receptor activation, but activates mitochondrial death pathways through production of reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide has the potential for lymphomas and autoimmune disorders[1][2].
Dimethyl malonate is a competitive inhibitor of succinate dehydrogenase (SDH). Dimethyl malonate is able to cross the blood-brain barrier and hydrolyse to malonate. Dimethyl malonate reduces neuronal apoptosis[1].
Byakangelicol, isolated from Angelica dahurica, inhibits interleukin-1beta (IL-1beta) -induced prostaglandin E2 (PGE2) release in A549 cells mediated by suppression of cyclooxygenase-2 (COX-2) expression and the activity of COX-2 enzyme. Byakangelicol has therapeutic potential as an anti-inflammatory drug on airway inflammation[1].
IMP2-IN-2 (compound 6) is a potent and selective IMP2 inhibitor, with IC50s of 120.9 μM and 236.7 μM for IMP2 interaction with RNA_A and RNA_B, respectively. IMP2-IN-2 can be used for the research of cancer[1].
Allopurinol (Zyloprim) is a xanthine oxidase inhibitor with an IC50 of 7.82±0.12 μM.Target: XAOAllopurinol (Zyloprim, and generics) is a drug used primarily to treat hyperuricemia (excess uric acid in blood plasma) and its complications, including chronic gout. It is a xanthine oxidase inhibitor which is administered orally. A common misconception is that allopurinol is metabolized by its target, xanthine oxidase, but this action is principally carried out by Aldehyde oxidase. The active metabolite of allopurinol is oxypurinol, which is also an inhibitor of xanthine oxidase. Allopurinol is almost completely metabolized to oxypurinol within two hours of oral administration, whereas oxypurinol is slowly excreted by the kidneys over 18–30 hours. For this reason, oxypurinol is believed responsible for the majority of allopurinol's effect.Allopurinol is a purine analog; it is a structural isomer of hypoxanthine (a naturally occurring purine in the body) and is an inhibitor of the enzyme xanthine oxidase. In addition to blocking uric acid production, inhibition of xanthine oxidase causes an increase in hypoxanthine and xanthine. While xanthine cannot be converted to purine ribotides, hypoxanthine can be salvaged to the purine ribotides adenosine and guanosine monophosphates. Increased levels of these ribotides may cause feedback inhibition of amidophosphoribosyl transferase, the first and rate-limiting enzyme of purine biosynthesis. Allopurinol, therefore, decreases uric acid formation and may also inhibit purine synthesis.
Aflatoxin M1 is a major metabolite of Aflatoxin B1. Aflatoxin M1 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2[1].
Glutaric anhydride-d6 is the deuterium labeled Glutaric anhydride[1].
Mapenterol hydrochloride is a type of β2-adrenoceptor agonist[1].
Sodium Picosulfate inhibits absorption of water and electrolytes, and increases their secretion.Target: OthersSodium Picosulfate displays cytotoxic effects on cultured liver cells. 800 and 1600 mg/mL induces dose-dependently vacuolic and fatty change as well as necrosis combined with a lowered mitotic activity and a slight increase in LDH values of the rapidly growing cultured liver cells of rabbit. Comparable but less severe effects are observed in 4-day old liver cell cultures of rat, while liver cells cultured for 6 to 11 days tolerate 1600 mg/mL Sodium Picosulfate. In human liver cultures the number of cells is slightly lowered at 800 and 1600 mg/mL and the number of nuclei in division is decreased dependent on dose [1]. Sodium Picosulphate has no major influence on ileal and colonic epithelial cell proliferation. In a 12 weeks study, 10 mg/kg Sodium Picosulphate continuously treatment does not influence the labeling index of Brdu (LI) in the ileum and induces no statistically significant increase of the LI when the treated groups are compared with the control group. The proliferative pattern along the crypts remains unchanged with sodium picosulphate treatment throughout the study [2]. Sodium Picosulphate does not induce chronic changes in colonic motility in rats under long-term treatment. 10mg/kg/day Sodium Picosulphate pretreated for 23 weeks does not induce any significant change in the duration of long spike bursts (LSB) which are associated with phasic contractions, or in LSB frequency in the fasted state or after a 3-gram meal [3].
BPN14770 is a selective phosphodiesterase 4D (PDE4D) allosteric inhibitor with IC50s of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3 (two different dimeric forms of PDE4D), respectively[1].
Clenbuterol hydrochloride (NAB-365 hydrochloride) is a β2 adrenergic receptor agonist. It is a powerful bronchodilator withfat burning properties.
PSMA-11 is a positron emission tomography (PET) tracer. PSMA-11 detects prostate cancer relapses and metastases by binding to the extracellular domain of prostate-specific membrane antigen (PSMA)[1].
Padmatin is a dihydroflavonol isolated from the heartwood of Prunus puddum[1].
6a,12a-Dehydro-α-toxicarol is a natural product that can be isolated from Amorpha fruticosa[1].
Opioid receptor modulator 1 is a opioid receptor modulator extracted from patent WO2014072809A2, Compound RA11 in EXAMPLE 7.
Fluoroclebopride binds reversibly to dopamine receptors. 18F labeled fluoroclebopride has been used as a probe for studying D2/D3 receptor availability via PET in various monkey models[1][2].
Epmedin C, a natural product, has estrogen-like effects for ovariectomized mice.IC50 value:Target:In vitro:In vivo: Anesthetized with 0.4%pentobarbital sodium, mice of the ovariectomized group were conducted with Bilateral oophorectomy, while fat beside ovaries were removed on mice of the sham-operation group. Compared with the sham-operation group, body weight of mice of model group were significantly increased, uterus weight and uterine factor and estradiol levels were significantly reduced, which suggested a significant difference. In comparison of the ovariectomized group, body weight of mice were relieved significantly and uterus weight and uterine factor and estradiol levels were increased significantly in all Epmedin C groups [1].
Ursonic acid methyl ester is an esterified derivative of Ursolic acid (HY-N0140). Ursonic acid methyl ester shows growth inhibitory activity against four tumor cell lines, HL-60, BGC, Bel-7402 and Hela with ED50 values of >100 µg/ml[1].
8-Hydroxypinoresinol is a tetrahydrofurofuran lignan that has cytoprotective effects against peroxynitrite-induced LLC-PK1 cell damage[1].
Fenoterol-d6 hydrobromide (Th-1165a-d6) is the deuterium labeled Fenoterol hydrobromide. Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research[1][2].
Seneciphylline is a toxic pyrrolizidine alkaloid in Senecio plants[1]. Seneciphylline significantly increases the activities of epoxide hydrase and glutathione-S-transferase but causes reduction of cytochrome P-450 and related monooxygenase activities[2].
Bryodulcosigenin is an extract of the roots of Bryoniadioica with anti-inflammatory effect[1].
CPI-1328 is an EZH2 inhibitor with a Ki value of 63 fM.
Nosantine racemate is the racemate of Nosantine. Nosantine is an inducer of IL-2 or enhancer of IL-2 induction by phytohemagglutinin (PHA).
Clarithromycin is a macrolide antibiotic and a CYP3A4 inhibitor.Target: Antibacterial; CYP3A4Clarithromycin is a macrolide antibiotic used to treat pharyngitis, tonsillitis, acute maxillary sinusitis, acute bacterial exacerbation of chronic bronchitis, pneumonia (especially atypical pneumonias associated with Chlamydophila pneumoniae), skin and skin structure infections. Clarithromycin prevents bacteria from growing by interfering with their protein synthesis. It binds to the subunit 50S of the bacterial ribosome and thus inhibits the translation of peptides. Clarithromycin has similar antimicrobial spectrum as erythromycin, but is more effective against certain Gram-negative bacteria, particularly Legionella pneumophila. Besides this bacteriostatic effect, clarithromycin also has bactericidal effect on certain strains, such as Haemophilus influenzae, Streptococcus pneumoniae and Neisseria gonorrhoeae. Clarithromycin is a CYP3A4 inhibitor. Even low doses of the cytochrome P4503A4 (CYP3A4) inhibitor clarithromycin increase the plasma concentrations and effects of repaglinide. Concomitant use of clarithromycin or other potent inhibitors of CYP3A4 with repaglinide may enhance its blood glucose-lowering effect and increase the risk of hypoglycemia [1, 2].
Flutropium bromide (Ba 598Br) is a organic bromide salt of flutropium. Flutropium bromide shows an anticholinergic effect. Flutropium bromide effectively suppresses spasms and it can be used for the research of asthma and chronic obstructive pulmonary disease[1][2][3].
KY-1044 (Alomfilimab; SAR 445256) is a fully human IgG1 antibody targeting inducible costimulatory receptor (ICOS). KY-1044 depletes ICOShigh cells via antibody-dependent cellular cytotoxicity (ADCC) through the engagement of FcgRIIIa. KY-1044 act as a costimulatory molecule on cells expressing lower ICOS levels, such as CD8+ TEff cells (through FcgR-dependent clustering). KY-1044 exploit the differential expression of ICOS on T-cell subtypes to improve the intratumoral immune contexture and restore an antitumor immune response[1].
Medicarpin is a flavonoid isolated from Medicago sativa. Medicarpin induces apoptosis and overcome multidrug resistance in leukemia P388 cells by modulating P-gp-mediated efflux of drugs[1].