Tebufenozide-d9 is the deuterium labeled Tebufenozide[1]. Tebufenozide is a nonsteroidal ecdysone agonist used to control pest. Tebufenozide has cytotoxic and induces apoptosis in HeLa and insect Tn5B1-4 cells[2][3].
3,5,7,8,3′,4′-Hexamethoxyflavone is a flavonoid. 3,5,7,8,3′,4′-Hexamethoxyflavone can be isolated from the leaves of Melicope triphylla MERR[1].
LSKL, Inhibitor of Thrombospondin (TSP-1) is a peptide derived from the latency-associated peptide, inhibits thrombospondin (TSP-1) activation of TGF-β and prevents the progression of hepatic damage and fibrosis.
Sipoglitazar is an orally active agonist of PPAR. Sipoglitazar can be used to study diabetes[1].
Anthragallol-2-methyl ether (compound 4) can be isolated from the fruits of Morinda citrifolia[1].
Loracarbef-d5 is the deuterium labeled Loracarbef. Loracarbef, a cephalosporin antibiotic, is an orally active second-generation synthetic beta-lactam antibiotic of the carbacephem class[1][2].
2-Isopropyl-3-methoxypyrazine-d3 is the deuterium labeled 2-Isopropyl-3-methoxypyrazine[1].
Tetramethylrhodamine (TMR, TRITC) has been a widely used fluorophore for preparing bioconjugates, especially fluorescent antibody and avidin derivatives used in immunochemistry. Under the name TAMRA, the carboxylic acid of 6-TAMRA has also achieved prominence as a dye for oligonucleotide labeling and automated DNA sequencing applications.
OS-3-106 is a potent, BBB-penetrated and selective dopamine D3 receptor (D3R) agonist. OS-3-106 binds with high affinity (Ki = 0.2 nM) at the D3R. OS-3-106 reduces cocaine self-administration and sucrose reinforcement rates. OS-3-106 can be used for psychostimulant addiction research[1].
Boc-Ethylmercapto-L-cysteine (dicyclohexylammonium) salt is a cysteine derivative[1].
Hexahydrohippuric acid is a metabolite of Shikimate acid in both liver and kidney, under microbial metabolism effect. Hexahydrohippuric acid is made of cyclohexane carboxylic acid and glycinamide, and shows antibacterial activity[1][2].
Syzalterin is an inhibitor of NO production with an IC50 of 1.87 μg/mL.
PF-06260933 is a highly selective small-molecule inhibitor of MAP4K4 with IC50s of 3.7 and 160 nM for kinase and cell, respectively.
NVP-231 is a potent, specific, and reversible CerK inhibitor(IC50=12±2 nM) that competitively inhibits binding of ceramide to CerK.IC50 Value: 12±2 nM [1]Target: CERKin vitro: NVP-231 showed an IC50 value of 12 ± 2 nM and 90% inhibition at 100 nM in the radioassay. NVP-231 did not compete with ATP but rather with ceramide, displaying an inhibition constant (Ki) of 7.4 nM. Furthermore, inhibition by NVP-231 was instantaneous and fully reversible, implying that this compound does not covalently modify CerK. At 10 nM, NVP-231 inhibited C1P formation by >50%; at 100 nM, NVP-231 achieved complete inhibition. Thus the potency and efficacy of NVP-231 observed in cell culture are consistent with those found in vitro. It is noteworthy that, NVP-231 did not inhibit GlcCer and SM formation; rather, it increased these metabolites in correlation with compound concentration, demonstrating that NVP-231 does not act as a general inhibitor of ceramide metabolism [1]. The EC(50) of NVP-231 in this assay is in the low nanomolar range, consistent with the IC(50) determined in activity assays in vitro using purified CerK [2].
Sodium stearyl fumarate can be used as an excipient. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs[1].
Transtorine is a quinoline alkaloid, found from Ephedra transitoria, with antibacterial activity[1].
Allicin (diallyl thiosulfinate), a highly potent natural antimicrobial activity substance, inhibits growth of a variety of microorganisms, among them antibiotic-resistant strains[1].
Thalidomide-O-C8-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
Fluorescein Di-β-D-Glucopyranoside is a specific β-glucocerebrosidase substrate that can be used for the intralysosomal β-galactosidase[1].
Desfluoro-ezetimibe is a desfluoro impurity of Ezetimibe. Ezetimibe is a potent, metabolically stable cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator[1][2].
D77 is anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells).IC50 value: 23.8 μg/ml (EC50, in MT-4 cell ), 5.03 μg/ml (EC50, in C8166 cell)Target: HIV-1in vitro: D77 exhibits a highly specific binding affinity to HIV-1 integrase catalytic core domain.D77 induces a dramatic concentration-dependent decrease of α-galactosidase activity compared to the D77-untreated cells. D77 reveals a significant inhibition activity against the interaction of IN with IBD.
3,4,6-trichlorocatechol (TCC) is the metabolite produced by industrial pollutant through post-mitochondrial liver fraction from Aroclor-1254 induced rats[1].
(-)-11,12-Methylenedioxykopsinaline (Compound 4) is the single terpenoids indole alkaloids which is isolated from Kopsia officinalis[1].
Gibberellin A1-d2 is the deuterium labeled Gibberellin A1 (HY-N7443). Gibberellin A1 is a kind of plant hormones[1].
Mavoglurant is a structurally novel, non-competitive mGlu5 receptor antagonist, has an IC50 of 30 nM in a functional assay with human mGluR5.IC50 value: 30 nMTarget: mGluR5in vitro: Mavoglurant is a selective non-competitive antagonist which showed efficacy in the treatment of L-dopa induced dyskinesias in Parkinson's disease and Fragile X mental retardation in proof of principle studies. Mavoglurant is selective over the other mGluR subtypes, iGluRs and a panel of 238 CNS relevant receptors, transporter or enzymes. [1]In vivo: Mavoglurant shows an improved pharmacokinetic profile in rat and efficacy in the stress-induced hyperthermia test in mice as compared to the prototypic mGluR5 antagonist MPEP.[1]
NIR dye-1 (Compound 1h) is a near-infrared (NIR) fluorescent dye. NIR dye-1 has absorption and emission in the NIR region, while retaining an optically tunable hydroxyl group[1].
Ozagrel(OKY-046) sodium salt is an antiplatelet agent working as a thromboxane A2 synthesis inhibitor.Target: Thromboxane A2 SynthaseOzagrel was selected as the best compound of highly selective inhibitors of TXA2 synthase. The inhibition of TXA2 synthase by ozagrel was more effective on human and rabbit enzymes than those of other species. Ozagrel increased 6-keto-PGF1 alpha, one of stable metabolites of PGI2, in various isolated cells and tissues perhaps via accumulated PG endoperoxides resulted by the inhibition of TXA2 synthase [1]. Ozagrel was estimated to be a reversible mixed-type inhibitor of diphenolase activity with the constants (K (S1), K (S2), K (i1), and K (i2)) determined to be 2.21, 3.89, 0.454, and 0.799 mM, repectively [2]. Infusion of OKY-046 significantly inhibited pulmonary thromboxane B2 delivery, attenuated the early increase in pulmonary vascular resistance, and blocked the increase in systemic vascular resistance. In addition, OKY-046 blunted and delayed the decrease in cardiac output and maintained end-systolic pressure-diameter relation, +dp/dt, and lung lymph flow at baseline values [3].
28-Deoxonimbolide is a nimbin (HY-N3187) type limonoid, that can be isolated from Azadirachta indica seed extracts. 28-Deoxonimbolide shows anticancer activity. 28-Deoxonimbolide induces apoptotic cell death in HL60 cells via both the mitochondrial- and the death receptor-mediated pathways[1].
Direct Black 38 is an azo dye. Direct Black 38 induces unscheduled DNA synthesis in liver and micronucleus in bone marrow of rats in vivo[1].
3-Bromopyruvic acid is a hexokinase II inhibitor, is an effective antitumor agent on the hepatoma cells.Target: hexokinase II in vitro: 3-BrPA dissociates HK II from this complex, causing cell death, and thus, having an anti-tumor effect. In vitro treatment of cells with 3-BrPA significantly inhibited their growth, as evaluated by MTT assay and adenosine triphosphate-tumor chemosensitivity assay (ATP-TCA). [1] 3-Bromopyruvic acid (3-BP) is a glycolytic inhibitor and a promising anticancer compound, induces oxidative stress and depletes cells of glutathione (GSH). [2]in vivo: 3-BrPA treatment (50 mg/kg ip. daily, 6 days/week for three weeks) is effective in the animal model by attenuating tumor growth and causing tumor necrosis. Toxic signs were not observed. The acute toxicity study provided an LD50 of 191.7 mg/kg for 3-BrPA. [1]