Magnesium sulphate is currently the anticonvulsant of choice for the prevention and control of eclamptic fits. Magnesium sulfate is also widely used as a tocolytic agent[1][2].
Senecionine acetate (O-Acetylsenecionine) is a pyrrolizidine alkaloid. Senecionine acetate inhibits the sequestration of Ca2+ in extramitochondrial and mitochondrial compartments possibly by inactivating free sulfhydryl groups[1].
Bis(6-methylheptyl) Phthalate-3,4,5,6-d4 is the deuterium labeled Bis(6-methylheptyl) phthalate[1].
Neobavaisoflavone, an isoflavone isolated from Psoralea corylifolia, has striking anti-inflammatory and anti-cancer effects. IC50 value: 42.93 μM (toward CCRF-CEM cells); 114.64 μM [against HCT116 (p53(+/+)) cells] [2]Target:In vitro: In the cancer cells, neobavaisoflavone sensitizes human U373MG glioma cells to TRAIL-mediated apoptosis; upregulated DR5 expression; induced TRAIL-mediated apoptosis in human glioma cells by suppressing migration and invasion, and by inhibiting anoikis resistance [1]. In caner cell lines, neobavaisoflavone is selectively active, and IC50 values below 115 μM were obtained on 6/9 cell lines, with values ranging from 42.93 μM (toward CCRF-CEM cells) to 114.64 μM [against HCT116 (p53(+/+)) cells] [2]. In vivo:
Ganoderic acid LM2 is a natural terpenoid isolated from the Fungus Ganoderma lucidum. Ganoderic acid LM2 possesses potential anti-tumor activity[1].
Fmoc-Asp(OcHex)-OH is an aspartic acid derivative[1].
AKR1C3-IN-6 (Compound 1) is a potent, selective AKR1C3 inhibitor with IC50 values of 0.31 μM and 73.23 μM against AKR1C3 and AKR1C2, respectively. AKR1C3-IN-6 shows antitumor activity[1].
Lacto-N-difucohexaose II (LNDFH II) is one of the oligosaccharides in human milk, it is important for infant health[1].
Dibenzyl aspartate 4-methylbenzenesulfonate is an aspartic acid derivative[1].
Ganoderenic acid A is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid A is a potent inhibitor of β-glucuronidase. Ganoderenic acid A has a potent hepatoprotective effect against CCl4-induced liver injury[1].
Selenocystine is a broad-spectrum anti-cancer agent. Selenocystine induces DNA damage in HepG2 cells, particularly in the form of DNA double strand breaks (DSBs). Selenocystine exhibits great promise as a therapeutic or adjuvant agent targeting DNA repair for cancer treatment[1].
Guattegaumerine is a bisbenzylisoquinoline alkaloid with antimitotic, cytotoxic and neuroprotective activities[1].
Lofepramine (Lopramine) is a potent tricyclic antidepressant and is extensively metabolised to Desipramine. The antidepressant activity of Lofepramine stems from the facilitation of noradrenergic neurotransmission by uptake inhibition. Lofepramine may also potentiate serotoninergic neurotransmission by inhibition of the neuronal uptake of serotonin and the enzyme tryptophan pyrrolase. Lofepramine has significant anxiolytic efficacy in addition to its antidepressant properties[1].
2-mercaptoethane sulfonate (Mesna), is a synthetic small molecule, widely used as a systemic protective agent against chemotherapy toxicity, but is primarily used to reduce hemorrhagic cystitis induced by cyclophosphamide.IC50 Value: 182 mM (decreased superoxide anion production stimulated with PMA (tetradecanoylphorbol acetate) in PMN in-vitro); 70mM (inhibited H2O2 production) [3]Target: in vitro: MESNA had no effect on the qualitative and quantitative characteristics of the indicated processes in both the types of the doxorubicin sensitive cells. The combined use of doxorubicin and phosphamide or cyclophosphane the use of MESNA for lowering the urotoxic action of oxazophosphorines had no effect on the biological efficacy of doxorubicin [4].in vivo: AMH-positive follicles were significantly decreased after cisplatin administration, which was significantly reversed when mesna was co-administered with cisplatin. The end product of lipid peroxidation, malondialdehyde (MDA), was significantly increased, but the anti-oxidative enzymatic activity of superoxide dismutase (SOD) and glutathione (GSH) were significantly decreased in cisplatin groups when compared with NS group. In contrast, after co-administration of cisplatin with mesna, MDA was significantly decreased whereas the activity of SOD and the concentration of GSH were increased. Moreover, mesna did not decrease the anti-tumor property of cisplatin in HePG2 cell lines [2]. After head trauma, tissue malondialdehyde levels increased; these levels were significantly decreased by MESNA administration. Caspase-3 levels were increased after trauma, but no effect of MESNA was determined in caspase-3 activity [1].Clinical trial: Effects of Mesna on Homocysteine in Kidney Failure . Phase2
Ezetimibe phenoxy glucuronide-D4 (Ezetimibe glucuronide-D4) is the deuterium labeled Ezetimibe phenoxy glucuronide. Ezetimibe phenoxy glucuronide is the active metabolite of Ezetimibe. Antihyperlipoproteinemic activity[1]. Ezetimibe is a potent cholesterol absorption inhibitor[2].
Fexofenadine Impurity F is the impurity of Fexofenadine. Fexofenadine, a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial[1].
Cystathionine-γ-lyase-IN-1 is a selective cystathionine γ-lyase (CSE) enzyme inhibitor with an IC50 of 6.3 μM[1].
(Z)-ONO 1301 is the inactive isomer of ONO 1301 (HY-106961), and can be used as an experimental control. ONO 1301 (ONO-AP 500-02), a prostaglandin (PG) I2 mimetic, is an orally active, long-acting prostacyclin agonist with thromboxane-synthase inhibitory activity. ONO 1301 promotes production of hepatocyte growth factor (HGF) from various cell types and ameliorates ischemia-induced left ventricle dysfunction in the mouse, rat and pig[1][2][3].
MB07803 is an orally available prodrug of a potent, noncompetitive inhibitor (MB07729) of fructose 1,6-bisphosphatase (FBPase), with EC50 of 140 nM and t1/2 of 7.6±2.9 h.
7'-Hydroxy ABA (7'-OH ABA) is a metabolite of Abscisic acid (Abscisic acid) through hydroxylation of the 7′-carbon atom of Abscisic acid. 7'-Hydroxy ABA exhibits significant hormonal activity[1].
Purpurin 18 methyl ester, a chlorophyll-a derivative, and is a photosensitizer that can be used in photodynamic therapy (PDT). Purpurin 18 methyl ester has photodynamic activity to induce cancer cell death[1].
Suomilide inhibits human trypsin-2 and -3, with IC50 values of 4.7 and 11.5 nM, respectively, while trypsin-1 is inhibited with an IC50 of 104 nM.
1-Heptadecanoyl-2-myristoleoyl-sn-glycero-3-phospho- L-serine-d5 (sodium) is deuterium labeled 1-Heptadecanoyl-2-myristoleoyl-sn-glycero-3-phospho- L-serine (sodium).
Ethyl acetoacetate (Ethyl acetylacetate) is an ester widely used as an intermediate in the synthesis of many varieties of compounds[1][2][3]. Ethyl acetoacetate is an inhibitor of bacterial biofilm[4].
N-Fmoc-4-(tert-butoxycarbonylmethoxy)-L-phenylalanine is a phenylalanine derivative[1].
6-Methylcoumarin is a synthetic fragrance widely used in cosmetics.
Calcitonin salmon, a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption. Sequence: Cys-Ser-Asn-Leu-Ser-Thr-Cys-Val-Leu-Gly-Lys-Leu-Ser-Gln-Glu-Leu-His-Lys-Leu-Gln-Thr-Tyr-Pro-Arg-Thr-Asn-Thr-Gly-Ser-Gly-Thr-Pro-NH2(Disulfide bridge: Cys1-Cys7).
Aspergillopepsin I (Aspergillus acid protease) is an aspartic endopeptidase that catalyses the hydrolysis of peptide bonds in proteins, with broad specificity[1].
Pronase E is a mixture of proteolytic enzymes that is obtained from Streptomyces griseus and could digest protein into individual amino acids.