2,2,2-Trichloroethanol, the active form of the sedative hypnotic drug chloral hydrate, is an agonist for the nonclassical K2P channels TREK-1 (KCNK2) and TRAAK (KCNK4)[1].
Ganoderic acid LM2 is a natural terpenoid isolated from the Fungus Ganoderma lucidum. Ganoderic acid LM2 possesses potential anti-tumor activity[1].
CP-775146 is a selective PPARα agonist that binds strongly to the PPARα ligand. CP-775146 efficiently alleviates obesity-induced liver damage, prevents lipid accumulation by activating the liver fatty acid β-oxidation pathway[1].
Naftifine Hydrochloride is a synthetic, broad spectrum, antifungal agent.Target: AntifungalNaftifine exhibits an interesting in vitro spectrum of activity against dermatophytes (38 strains; minimal inhibitory concentration (MIC) range 0.1 to 0.2 mg/mL), aspergilli (6 strains; MIC range, 0.8 to 12.5 mg/mL), Sporothrix schenckii (2 strains; MICs, 0.8 and 1.5 mg/mL), and yeasts of the genus Candida (77 strains; MIC range, 1.5 to greater than 100 mg/mL) [1]. The MIC of naftifine for C. albicans Δ63 is 100 mg/L in Sabouraud medium (initial pH 6.5). Naftifine (50 mg/L) gives greater than 99% inhibition of sterol biosynthesis both in whole cells and in cell extracts of C. albicans. The primary action of naftifine appears to be the blocking of fungal squalene epoxidation [2].Naftifine HCl 2% cream results in clinical cure rate and clinical success rate of 33% and 84% after treatment for 4 weeks, and week 2 efficacy response rates in Naftifine HCl 2% subjects are all lower than at week 4 but are significantly higher than week 2 vehicle-treated counterparts [3]. Naftifine causes interruption of fungal ergosterol synthesis and accumulation of squalene in fungal organisms. Naftifine also has demonstrated anti-inflammatory properties such as a reduction in superoxide production and a reduction in polymorphonuclear leukocyte chemotaxis/endothelial adhesion. Naftifine has shown good efficacy and safety for a variety of conditions and is a useful treatment that provides both antifungal action and relief of inflammatory signs and symptoms. Few adverse events have been noted with naftifine use, the most frequent being mild and transient burning, stinging, or itching in the application area [4].
Fmoc-Asp(OcHex)-OH is an aspartic acid derivative[1].
Sulbentine is an antifungal.
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].
5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a Ki of 0.18 nM for human κ-opioid receptor[1].
P2X7 receptor antagonist-3 is a potent P2X7 receptor antagonist with P2X7R IC50 values of 4.2 nM in humans and 6.8 nM in rats[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].
Granilin, a sesquiterpene lactone, can be found in the flower buds of Carpesium triste. Granilin can be used as the bactericide and fungicide[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].
N6-Bz-5’-O-DMTr-2’-O-hexadecanyl adenosine 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].
BCR-ABL-IN-5 (compound II) is a Bcr-Abl kinase (Breakpoint cluster region-Abelson) inhibitor. BCR-ABL-IN-5 inhibits Bcr-AblWT and Bcr-AblT3151 with the IC50 value of 0.014 μM and 0.45 μM, respectively. BCR-ABL-IN-5 has some anti-proliferative activity against leukemic cells[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].
5'-O-DMT-5-Ethynyl-2'-deoxyuridine 3'-CE phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
(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].
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.
Ro 363 hydrochloride, an effective inotropic stimulant, is a potent and highly selective β1-adrenoceptor agonist. Ro 363 hydrochloride is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility[1][2][3].
m-PEG6-(CH2)6-Phosphonic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
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].
Neticonazole is an imidazole derivative and a potent and long-acting antifungal agent. Neticonazole is also an orally active exosome biogenesis and secretion inhibitor. Neticonazole has anti-infection and anti-cancer effects[1][2][3].
N-Fmoc-4-(tert-butoxycarbonylmethoxy)-L-phenylalanine is a phenylalanine derivative[1].
CC-885-CH2-PEG1-NH-CH3 is a neoDegrader that can be used in the synthesis of Antibody neoDegrader Conjugate (AnDC)[1][2].
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).
Arecaidine, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake[1][2].