Rifamycin sodium (Rifamycin SV monosodium) belongs to the family of ansamycin antibiotics and has been isolated from the fermentation of A. mediterranei or its mutants. Rifamycin sodium displays a broad spectrum of antibiotic activity against Gram-positive and, to a lesser extent, Gram-negative bacteria[1].
Boc-Pen(Mob)-OH is a phenylalanine derivative[1].
Zinc phthalocyanine is commonly applied in industry (catalysts, photoconductors) and biomedical (photodynamic therapy, PDT)[1]. Zinc phthalocyanine can be used to photooxidise cyclohexane[2].
N-Methylformamide-d4 is the deuterium labeled N-Methylformamide[1].
Antibacterial agent 45, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Altertoxin I (Dihydroalterperylenol) is a quinone-type mycotoxin produced by Alternaria alternata fungi, which is mutagenic and cytotoxic, and can weakly disrupts metabolic communication[1].
Loganetin is a non-toxic natural product that may be applied in the antibacterial drug development for treating multidrug-resistant Gram negative infections.
DL-Tyrosine is an aromatic nonessential amino acid synthesized from the essential amino acid phenylalanine. DL-Tyrosine is a precursor for several important neurotransmitters (epinephrine, norepinephrine, dopamine)[1].
NF-κB-IN-7 (compound 1B) is a potent NF-κB inhibitor. NF-κB-IN-7 can be used for the research of cancer, inflammation, autoimmune diseases, diabetes and diabetes complications, infections, cardiovascular disease and defective reperfusion injury[1].
Metyrapone is an inhibitor of cytochrome P450-mediated ω/ω-1 hydroxylase activity and CYP11B1.Target: CYP11B1Metyrapone is a drug used in the diagnosis of adrenal insufficiency and occasionally in the treatment of Cushing's syndrome (hypercortisolism). Metyrapone blocks cortisol synthesis by reversibly inhibiting steroid 11β-hydroxylase. This stimulates ACTH secretion, which in turn increases plasma 11-Deoxycortisol levels.
Telomerase-IN-2 is a telomerase inhibitor, and inhibits telomerase activity by decreasing expression of dyskerin, with an IC50 of 0.89 µM. Anti-cancer activity[1].
trans-trans-Muconic acid-d4-1 is a deuterium labeled trans-trans-Muconic acid (HY-113247). trans-trans-Muconic acid is a urinary metabolite of benzene and has been used as a biomarker of exposure to benzene in human.
(R)-Lercanidipine hydrochloride is the R-enantiomer of Lercanidipine. (R)-lercanidipine hydrochloride is a calcium channel blocker[1].
Hypaconitine, an active and highly toxic constituent derived from Aconitum species, is widely used to treat rheumatism. IC50 value:Target:In vitro: The present study investigated the metabolism of hypaconitine in vitro using male human liver microsomes. The primary contributors toward HA metabolism were CYP3A4 and 3A5, with secondary contributions by CYP2C19, 2D6 and CYP2E1 [1].In vivo:
Echimidine ((+)-Echimidine) is the major alkaloid detected in the honey used to produce the mead[1].
2-Amino-4-(ethylthio)butanoic acid is a Methionine (HY-13694) derivative[1].
Fmoc-(FmocHmb)Lys(Boc)-OH is a lysine derivative[1].
Hydroxyprogesterone caproate is a synthetic, steroidal progestin; an ester derivative of 17α-hydroxyprogesterone formed from caproic acid.
(3S,5S)-Pitavastatin (hemicacium) is the enantiomer of Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor[1].
Olprinone(Loprinone) is a selective phosphodiesterase 3 (PDE3) inhibitor. IC50 value:Target: PDE3Olprinone is used as cardiotonic agent with positive inotropic and vasodilating effects. Olprinone has been reported to improve microcirculation and attenuate inflammation. Olprinone is often used to increase cardiac output after cardiopulmonary bypass (CPB). Olprinone was infused at a rate of 0.2 μg/kg/min when weaning from CPB was started. Olprinone has also shown potent antioxidative and anti-inflammatory effects in the meconium-induced oxidative lung injury.
GPR3 agonist-2(compound 32) is a potent full agonist of G protein-coupled receptor 3, with the IC50of 260 nM[1].
(+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1, with an IC50 of 10.4 nM.
20:0-20:1-20:0 TG-d5 is deuterium labeled 20:0-20:1-20:0 TG.
Pyrazoloadenine is a potent RET (REarranged during Transfection) lung cancer oncoprotein inhibitor. Pyrazoloadenine shows anticancer activity[1][2].
MSDC 0160 act as an insulin sensitizer and a modulator of mitochondrial pyruvate carrier (MPC), a key controller of cellular metabolism that influences mTOR (mammalian target of rapamycin) activation. In Vitro: MSDC-0160 acts as insulin sensitizers without activating PPARγ. MSDC-0160 (10 μM) pretreatment (1 hour) prevents the MPP+ (10 μM)-induced loss of both tyrosine hydroxylase (TH)-immunoreactive differentiated Lund human mesencephalic (LUHMES) cells. MSDC-0160 protects only TH-immunoreactive neurons, which is consistent with the selected concentration of MPP+ primarily being toxic to dopamine neurons. In addition, MSDC-0160 counteracts both MPP+-induced shortening of neurite length and reduces branching in both LUHMES cells. MSDC-0160 (10 or 100 μM) prevents the loss of GFP-fluorescent dopaminergic neurons induced by MPP+ (0.75 mM) in nematodes (P =0.0001), whereas 1 μM MSDC-0160 does not. MSDC-0160 (10 μM) blocks LPS-induced increases in iNOS expression in BV2 cell lysates. MSDC-0160 is mainly to prevent the activation of mTOR produced by the metabolic changes rather than to directly inhibit mTOR kinase activity[1]. PPARγ sparing TZD, MSDC-0160, reduces resistance in the insulin/IGF-1 signaling pathway and restores IGF-1-induced akt phosphorylation. MSDC-0160 (10-20 μM) in conbination with IGF-1 prevents the loss of insulin content and maintains insulin secretion. Treatment of human islets with MSDC-0160 (1-50 μM) activates AMPK and downregulates mTOR. MSDC-0160 (1-50 μM) treatment maintains human β-cell phenotype[2]. The combined treatment with PPARγ ligands (MSDC 0160) and γ-radiation synergistically induces caspase-dependent apoptotic cell death, and PPARγ ligands significantly enhance the γ-radiation-induced DNA damage response in a PPARγ-independent manner[3].In Vivo: MSDC-0160 (30 mg/kg per day, p.o.) can be observed in plasma and brain tissue of the mice, proving MSDC-0160 can effectively enter the brain. MSDC-0160 (30 mg/kg per day, p.o.) treatment 3 days after MPTP injection, improves motor behavior, protects nigrostriatal neurons, and suppresses disease progression in the MPTP mouse model of Parkinson’s disease (PD), improves motor behavior in the open-field and rotarod tests in the En1+/- genetic mouse model of PD, and prevents dopaminergic neurodegeneration in the En1+/- genetic mouse model of PD. MSDC-0160 (30 mg/kg, p.o.) modulates mTOR signaling in C. elegans and the MPTP mouse model of PD. MSDC-0160 down-regulates mTOR signaling and restores autophagy in the En1+/- genetic mouse model of PD[1].
OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study[1].
Cy3B NHS ester is a fluorescent dye compound that is commonly used in biomarking and fluorescent labeling experiments, especially for labeling biomolecules containing amino functional groups (amine groups), such as proteins, antibodies or peptides.
Momelotinib-3,3,5,5-d6 (CYT387-3,3,5,5-d6) is the deuterium labeled Momelotinib (HY-10961). Momelotinib has inhibitory activity for JAK1/JAK2[1][2].
Brombuterol hydrochloride (Bromobuterol hydrochloride) is a β-adrenergic receptor agonist[1].
(2E,9Z)-Octadeca-2,9-dienoic acid, a polyunsaturated fatty acid, can be used for the research of lipoxygenase-dependent metabolism[1].