Dimethyl Sulfoxide
Medchemexpress LLC Cimetidine sulfoxide | 54237-72-8 | 97.0% | 268.35 | 25 MG
Cimetidine sulfoxide is a sulfoxide metabolite of Cimetidine. Cimetidine acts as a histamine H2-receptor antagonist and has potential for treating peptic ulcer disease and upper gastrointestinal hemorrhage. Active transport of Cimetidine across the rat small intestine is observable at lower substrate concentrations. Cimetidine sulfoxide is detected after some incubations, and its enantiomeric composition has been determined in rat urine following Cimetidine administration.
- Histamine H2-receptor antagonist
- Potential for peptic ulcer disease treatment
- Potential for upper gastrointestinal hemorrhage treatment
- Sulfoxide metabolite
- Soluble in various solvents for in vitro and in vivo studies
- Store powder at -20°C for 3 years
- Store in solvent at -80°C for 6 months or -20°C for 1 month
Apexbio Technology LLC Purmorphamine 483367-10-8 10mM (in 1mL DMSO)
Purmorphamine (CAS 483367-10-8) is a synthetic small molecule agonist targeting the Smoothened (Smo) protein a critical component of the Hedgehog (Hh) signaling pathway By binding and activating Smo Purmorphamine induces downstream modulation of key pathway targets such as Gli1 and Patched In vitro studies demonstrated activation with an IC50 value of approximately 1 5 M during competitive assays with the antagonist cyclopamine and an EC50 of about 1 M for alkaline phosphatase (ALP) expression in C3H10T1/2 multipotent cells This agent has been applied in research contexts for inducing osteogenic differentiation with implications for studying bone regeneration and neural degeneration processes
Apexbio Technology LLC Fidaxomicin 873857-62-6 10mM (in 1mL DMSO)
Fidaxomicin is a macrocyclic antibiotic derived from Actinomycetes functioning through inhibition of bacterial RNA polymerase by targeting the -subunit thereby interfering with bacterial RNA synthesis It exhibits specific antibacterial effects against Clostridium difficile suppressing toxin production and reducing disease recurrence in Clostridium difficile infections (CDI) Fidaxomicin has entered phase III clinical investigation for treatment of CDI Experimental results indicate an intravenous LD50 of approximately 200 mg/kg in rats reported inhibitory concentrations (IC50) against C difficile RNA polymerase range in the nanomolar scale It is utilized in research for studying bacterial transcription mechanisms and evaluating treatment strategies aimed at CDI
Apexbio Technology LLC AZD7545 252017-04-2 10mM (in 1mL DMSO)
AZD7545 (CAS 252017-04-2) is a selective small molecule inhibitor targeting pyruvate dehydrogenase kinase 2 (PDHK2) PDHK2 negatively regulates the pyruvate dehydrogenase (PDH) enzyme complex which converts pyruvate to acetyl-CoA By inhibiting PDHK2 AZD7545 enhances PDH activity In biochemical assays AZD7545 shows potent inhibition of PDHK2 with an IC50 of 6 4 nM whereas it demonstrates somewhat lower potency against PDHK1 (IC50 36 8 nM) In vivo studies using Zucker (fa/fa) rats indicate that AZD7545 administration significantly elevates PDH activity in liver skeletal muscle and heart tissues Thus AZD7545 is proposed as a research tool or therapeutic candidate for metabolic disorders including type 2 diabetes
Apexbio Technology LLC Veliparib dihydrochloride 912445-05-7 10mM (in 1mL DMSO)
Veliparib dihydrochloride (CAS 912445-05-7) is a selective inhibitor of poly(ADP-ribose) polymerases PARP1 and PARP2 enzymes responsible for DNA repair processes frequently upregulated in various cancers Veliparib inhibits PARP1 and PARP2 with K(i) values of 5 2 and 2 9 nmol/L respectively In colon cancer cell lines (HCT-116 HT-29) veliparib enhances DNA damage and induces G2/M arrest when combined with SN38 or oxaliplatin In preclinical murine melanoma (B16F10) breast cancer (MX-1) and colon cancer (HCT-116) xenografts combination therapy with DNA-damaging agents shows improved antitumor effects
Apexbio Technology LLC Andarine 401900-40-1 10mM (in 1mL DMSO)
Andarine (S-4) is a selective androgen receptor (AR) antagonist with a Ki value of approximately 4 nM indicating strong receptor-binding affinity It functions by selectively targeting androgen receptors nuclear receptors involved in DNA-mediated transcription and gene expression regulation In vitro studies using AR-driven transcription assays illustrate Andarine s capacity to modulate AR activity at nanomolar concentrations Animal model studies in male Sprague-Dawley rats suggest Andarine administration induces a dose-dependent increase in tissues responsive to androgen activity including prostate gland seminal vesicles and levator ani muscle Due to its receptor specificity and manageable pharmacodynamics Andarine is widely investigated in biomedical research related to androgen receptor signaling pathways endocrine regulation and therapeutic responses involving AR-mediated mechanisms
Apexbio Technology LLC Anacetrapib (MK-0859) 875446-37-0 10mM (in 1mL DMSO)
Anacetrapib (MK-0859 CAS 875446-37-0) is a selective inhibitor of cholesteryl ester transfer protein (CETP) an enzyme involved in mediating the transfer of cholesteryl esters and triglycerides between lipoproteins In biochemical assays anacetrapib exhibits potent inhibition of CETP-driven lipid transfer with reported IC50 values of 16 nM for cholesteryl ester transfer and 29 nM for triglyceride transfer Metabolically it undergoes oxidation via CYP3A4 to form metabolites M1 M2 and M3 Due to its effect of significantly lowering LDL cholesterol and elevating HDL cholesterol anacetrapib is studied in research related to primary hypercholesterolemia and mixed dyslipidemia
Apexbio Technology LLC Dapagliflozin(Synonyms: Farxiga, Forxiga, BMS-512148, AZD-1656, Dapagliflozin propanediol, Dapagliflozin hydrate), 10mM (in 1mL DMSO), CAS: 461432-26-8.
Dapagliflozin (CAS 461432-26-8) is a selective inhibitor of sodium-glucose cotransporter 2 (SGLT2) an integral membrane protein primarily expressed in renal proximal tubules Acting via specific inhibition of SGLT2-mediated glucose reabsorption dapagliflozin facilitates urinary glucose excretion thereby regulating plasma glucose levels It exhibits a potent EC50 of approximately 1 1 nM for human SGLT2 and shows over 1 200-fold selectivity for hSGLT2 over hSGLT1 in vitro Preclinical studies demonstrate improved glucose tolerance enhanced urinary glucose excretion and reduction of hyperglycemia in diabetic animal models Thus dapagliflozin serves as an important investigational molecule for type 2 diabetes research
Apexbio Technology LLC Protionamide 14222-60-7 10mM (in 1mL DMSO)
Protionamide is a thiophene-derived antibacterial compound that inhibits the synthesis of mycolic acids a major component of the mycobacterial cell wall Through disruption of mycolic acid biosynthesis it interferes with cell wall integrity exhibiting antibacterial activity against pathogenic mycobacteria Protionamide is commonly employed in research involving Mycobacterium tuberculosis and Mycobacterium leprae primarily for investigating molecular mechanisms underlying drug resistance and cell wall biosynthesis pathways In laboratory experiments this compound is frequently utilized in vitro for cultivation assays antimicrobial screening and studies on synergistic effects when combined with other antimycobacterial agents It demonstrates reported IC50 values in the micromolar range dependent on experimental conditions and mycobacterial strains used
Apexbio Technology LLC Pralatrexate 146464-95-1 10mM (in 1mL DMSO)
Pralatrexate (CAS 146464-95-1) is a small molecule inhibitor targeting dihydrofolate reductase (DHFR) with a Ki value of 45 nM DHFR mediates the reduction of dihydrofolate to tetrahydrofolate a critical cofactor in purine thymidylate and amino acid biosynthesis Pralatrexate exhibits high affinity for folylpolyglutamate synthetase (FPGS) and reduced folate carrier-1 (RFC-1) facilitating intracellular accumulation It demonstrates notable antiproliferative activity against various human cancer cell lines in vitro and reduces tumor growth in NSCLC xenograft models indicating its suitability for oncology research
Apexbio Technology LLC DBeQ 177355-84-9 10mM (in 1mL DMSO)
DBeQ (CAS 177355-84-9) is a selective and reversible inhibitor of the ATPase p97 (also known as VCP or Cdc48 in yeast) exhibiting an IC50 value of approximately 1 5 M p97 is an essential abundantly expressed hexameric AAA ATPase implicated in multiple cellular processes including endoplasmic reticulum-associated degradation (ERAD) mitochondrial-associated degradation autophagy maturation and regulation of transcription factors DBeQ inhibits p97 by specifically targeting its D1 and D2 ATPase domains leading to blockage of ERAD and autophagosome maturation Research applications of DBeQ include investigating protein homeostasis cancer biology and apoptosis induction mediated through caspases-3 and -9 activation
Apexbio Technology LLC PD184352 (CI-1040) 212631-79-3 10mM (in 1mL DMSO)
PD184352 (CI-1040 CAS 212631-79-3) is a benzhydroxamate derivative that selectively inhibits the MEK1/2 kinases members of the MAP kinase kinase (MAPKK) family It interacts with a hydrophobic pocket adjacent to the Mg-ATP binding region of MEK1/2 triggering conformational shifts that favor the inactive non-phosphorylated state of these enzymes Acting via an ATP- and ERK1/2-independent inhibitory mechanism PD184352 robustly suppresses purified MEK1 enzyme activity (IC50 17 nM) Preclinical research demonstrates efficacy in reducing tumor growth notably in murine xenograft models of colon carcinoma underscoring its utility as a research tool in oncology
Apexbio Technology LLC CPI-169 1450655-76-1 10mM (in 1mL DMSO)
CPI-169 is a selective small-molecule inhibitor targeting enhancer of zeste homolog 2 (EZH2) a catalytic component of polycomb repressive complex 2 (PRC2) By inhibiting EZH2 enzymatic activity CPI-169 suppresses methylation at histone H3 lysine 27 (H3K27me3) thereby altering chromatin structure and gene expression profiles Pharmacological experiments demonstrate inhibition of EZH2 with subnanomolar IC50 values and cellular studies indicate reductions of H3K27 trimethylation at nanomolar concentrations CPI-169 has been utilized experimentally to investigate EZH2-dependent epigenetic processes cell proliferation apoptosis pathways and therapeutic potential particularly in lymphoma and cancer biology studies employing in vitro and in vivo models
Apexbio Technology LLC CP-673451 343787-29-1 10mM (in 1mL DMSO)
CP-673451 (CAS 343787-29-1) is an ATP-competitive inhibitor with specificity for platelet-derived growth factor receptors (PDGFR- / ) It exhibits inhibitory potency with IC50 values of 10 nM for PDGFR- and 1 nM for PDGFR- while demonstrating significantly less inhibition toward kinases such as VEGFR-1 VEGFR-2 Lck TIE-2 and EGFR In cellular assays CP-673451 effectively inhibits PDGFR- phosphorylation in PAE- cells (IC50 6 4 nM) and reduces c-kit activity in H526 cells at micromolar range Its anticancer efficacy has been established by suppressing tumor growth and vascularization in xenograft models indicating its potential utility in cancer research and angiogenesis studies