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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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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-3311 (COX-2 Inhibitor V) is a selective cell-permeable and orally available inhibitor of cyclooxygenase-2 (COX-2) with antiinflammatory FK-3311 has protective effects against hepatic warm ischemia-reperfusion injury by marked inhibition of TxA2
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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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FK 453 (compound 1d) is a potent and selective adenosine A1 receptor antagonist (IC50 17.2 nM) intended for research use. It is a non-xanthine small molecule used in pharmacological studies to probe A1 receptor function and ligand interactions.
Potent adenosine A1 antagonist (IC50 17.2 nM).
High purity 99.2%.
Molecular weight 375.46 g·mol⁻¹.
Chemical formula C23H25N3O2.
Supplied as 5 mg solid for laboratory research.
Suitable for in vitro pharmacology and receptor binding assays.
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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.
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(E/Z)-FK-506 26,28-allylic ester rearrangement impurity (FK506-A) is an impurity of tacrolimus used as a reference standard for analytical and stability studies. It is intended for research and analytical applications to identify, quantify, and qualify impurity profiles; consult the certificate of analysis for storage and handling details.
Reference impurity of tacrolimus for analytical method development.
Suitable for impurity identification, reporting, and qualification studies.
High-purity material for reliable chromatographic and mass spectrometric analysis (>90.0%).
Supplied as a solid for laboratory use; consult the certificate of analysis for storage instructions.
Molecular formula C44H69NO12 and molecular weight 804.02 for compound identification.
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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 that binds to FKBP to form a complex, inhibiting calcineurin phosphatase. This action suppresses T-lymphocyte signal transduction and IL-2 transcription, resulting in immunosuppressive properties. It is intended for research use only.
Inhibits T-lymphocyte signal transduction
Inhibits IL-2 transcription
Immunosuppressive properties
Potentiates glucocorticoid and progesterone actions
May enhance TGFβ-1 gene expression
Inhibits T cell proliferation
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This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.for further information and support please go to the website of the issuing Pharmacopoeia.
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