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Compounds that are analog of macrolides that contain lactam rings in place of lactone rings; they are a class of antibiotics. Lactam rings are nitrogen analogs of lactone rings.
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Chemical. CAS 104987-12-4. Formula C43H69NO12. MW 792. Isolated from Streptomyces sp. Macrolide antibiotic. Ethyl analog of FK506. Strong immunosuppressant. Binds to the FK-506-binding protein FKBP12. This complex inhibits calcineurin protein phosphatase 2B PP2B. Suppresses the production of T helper type 1 Th1 interferon and IL-2 and Th2 IL-4 and IL-10 cytokines in T lymphocytes and preferentially inhibits the activation of mast cells. Anti-inflammatory. Used for topical treatment of inflammatory skin diseases. Potently inhibits anti-IgE-induced histamine and cytokine release and reduces IgE-dependent p38 MAPK activation in human basophils. Inhibits basophil degranulation at the initial phase of allergic skin reactions. Antifungal. Antimalaria compound. Anticonvulsant antiepileptic.
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Also available in 1 mg 10 mg 25 mg 50 mg 100 mg 500 mg and bulk. Please contact Fisher for quotes. FK-453 is a potent antagonist of non-xanthine adenosine A1 receptor with diuretic and renal vasodilatory activity. purity: 99%
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Tacrolimus monohydrate is a macrocyclic lactone immunosuppressant reagent that binds FK506 binding protein (FKBP) and inhibits calcineurin phosphatase, suppressing T-cell signaling and IL-2 transcription for in vitro immunology and biochemical studies.
High purity suitable for research applications.
Molecular formula C44H71NO13; molecular weight 822.03 g·mol⁻¹.
CAS number 109581-93-3 for unambiguous identification.
Store protected from light at 4°C; in solution store at -80°C for long-term stability.
Commonly used in assays targeting calcineurin and FKBP-mediated pathways.
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FK 453 is a potent, selective adenosine A1 receptor antagonist intended for research use. It inhibits human A1 receptor activity with an IC50 of 17.2 nM, appears as an off-white to light yellow solid, and also shows activity at adenosine A2B and in primary rat hepatocytes.
Tacrolimus monohydrate (Tacrolimus FK506) is a macrolide antibiotic that primarily acts as an inhibitor of calcineurin phosphatase by binding to FK506 binding protein (FKBP) This inhibition blocks calcium-dependent processes including interleukin-2 gene transcription nitric oxide synthase activation cell degranulation and apoptosis and also has immunosuppressive neuroregenerative and neuroprotective properties
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FK 866 hydrochloride (CAS 658084-64-1 free base) is a potent inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase) an enzyme essential for NAD biosynthesis exhibiting activity with IC50 values ranging from 0 09 nM to 27 2 nM By blocking NAD synthesis FK 866 disrupts ATP production induces mitochondria membrane depolarization and triggers autophagy independent of caspase activation It selectively targets hematologic cancer cells such as AML lines sparing normal hematopoietic progenitor cells FK 866 demonstrates antitumor efficacy in vivo significantly suppressing growth in AML-M4 and Namalwa xenograft models
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FK 453 is a non-xanthine adenosine A1 receptor antagonist (compound 1d) used in pharmacological research. It is reported as potent and selective, with an IC50 of 17.2 nM. The compound has chemical formula C23H25N3O2, molecular weight 375.46, and reported purity 99.20%.
Potent and selective A1 receptor antagonist (IC50 17.2 nM).
High reported purity suitable for research use (99.2%).
Chemical formula C23H25N3O2 and molecular weight 375.46.
Available in small research quantities, for example 50 mg.
Supplied with supporting analytical data such as COA, HPLC, and LCMS.
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Tacrolimus (FK506) analytical standard intended for research and analytical applications. Tacrolimus is a macrolide immunosuppressant that binds FK506 binding protein and inhibits calcineurin, affecting T-lymphocyte signal transduction. This reference material is supplied for assay calibration, method development, and quality control in analytical workflows.
High-purity reference material (99.6%).
Intended for analytical and research use, including assay calibration and method development.
Available in small mass quantities suitable for analytical workflows (e.g., 5 mg).
Provides a stable, characterized standard for quality control.
Supplied with documentation for purity and identity.
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