Metabolism

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  1. IMPDH inhibitor

    Mycophenolate mofetil is a reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH) in purine biosynthesis (specifically guanine synthesis) which is necessary for the growth of T cells and B cells.
  2. Cyclosporin A (Cyclosporine A) is an immunosuppressant agent widely used in post-allogeneic organ transplant to reduce the activity of the immune system.
  3. Deflazacort is a glucocorticoid used as an anti-inflammatory and immunosuppressant.
  4. glucocorticoid receptor agonist

    Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs. It acts as an anti-inflammatory and immunosuppressant. Its potency is about 20-30 times that of the naturally occurring hormone hydrocortisone and 4-5 times of prednisone.
  5. mTOR inhibitor

    FK-506 is an immunosuppressive drug that is mainly used after allogeneic organ transplant to reduce the activity of the patient's immune system and so lower the risk of organ rejection. It reduces interleukin-2 (IL-2) production by T-cells.
  6. S1P Receptor antagonist

    FTY720 is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine.
  7. Hydrocortisone is a steroid hormone or glucocorticoid produced by the adrenal gland.
  8. Mizoribine is an imidazole nucleoside immunosuppressant agent that was first isolated from the mold Eupenicillium brefeldimium with antibiotic and cytotoxic effects.
  9. Mycophenolic Acid is an immunosuppressant small molecule isolated as a fermentation product from several Penicillium species.
  10. mTOR Inhibitors

    Rapamycin (Sirolimus) prevents activation of T cells and B-cells by inhibiting their response to interleukin-2 (IL-2).
  11. 6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) is an anti-leukemia and immunosuppressant agent,
  12. Triptolide is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii.
  13. mTOR inhibitor

    Zotarolimus is an immunosuppressant. It is a semi-synthetic derivative of rapamycin. It was designed for use in stents with phosphorylcholine as a carrier.
  14. Immunomodulators

    Cyclosporin B is an immunosuppressant that has revolutionized organ transplantation through its use in the prevention of graft rejection.
  15. Calcineurin inhibitor

    Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation.
  16. Calcineurin/PP2B inhibitor

    Ascomycin is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties. It has been researched for the treatment of autoimmune diseases and skin diseases, and to prevent rejection after an organ transplant.
  17. Hydrocortisone Acetate is the synthetic acetate salt form of hydrocortisone, a corticosteroid with anti-inflammatory and immunosuppressive properties
  18. S1P antagonist

    Fingolimod is a sphingosine 1-phosphate (S1P) antagonist with IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant.
  19. antifolate agent

    Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).
  20. Hydrocortisone buteprate (Hydrocortisone probutate) is a medium potent, non-halogenated double-ester of hydrocortisone with a favorable benefit/risk ratio for the treatment of inflammatory skin disorders.
  21. immunosuppressant

    Tacrolimus monohydrate (FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate) is a macrocyclic lactone with potent immunosuppressive properties, an immunosuppressant.
  22. Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases T cell and B cell proliferation.
  23. Anti-inflammatory

    Hydrocortisone butyrate is a topical corticosteroid use to treat a variety of dermatological conditions. It acts as an antiinflammatory, antiproliferative and immunosuppresive agent.
  24. S1PR1 agonist

    FTY720 (S)-Phosphate is an agonist of S1P receptor 1 (S1PR1), used in the research of acute inflammatory diseases such as acute lung injury.
  25. Gusperimus trihydrochloride (Spanidin) is a derivative of the antitumor antibiotic spergualin with immunosuppressant activity.
  26. JAK3/STAT5 inhibitor

    BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.

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