Placeholder

Sirolimus

  • # LGM Pharma is a Sirolimus CAS# 53123-88-9 API supplier distributor based in the USA. Inquire about DMF, cGMP, price, availability, samples, sourcing, purity and more.
  • # Questions? Call our customer API support number 1-(800)-881-8210.
  • # LGM Pharma offers this active ingredient but not the finished dosage forms.
  • Inquire about this product >>

Product Details:

  • Product Name: Sirolimus
  • CAS #: 53123-88-9
  • Mode of Action:

    Sirolimus inhibits T lymphocyte activation and proliferation that occurs in response to antigenic and cytokine (Interleukin IL-2, IL-4, and IL-15) stimulation by a mechanism that is distinct from that of other immunosuppressants. Sirolimus also inhibits antibody production. In cells, sirolimus binds to the immunophilin, FK Binding Protein-12 (FKBP-12), to generate an immunosuppressive complex. The sirolimus:FKBP-12 complex has no effect on calcineurin activity. This complex binds to and inhibits the activation of the mammalian Target Of Rapamycin (mTOR), a key regulatory kinase. This inhibition suppresses cytokine-driven T-cell proliferation, inhibiting the progression from the G1 to the S phase of the cell cycle.

  • Pharmacodynamics:

    Sirolimus, a macrocyclic lactone produced by Streptomyces hygroscopicus, is an immunosuppressive agent indicated for the prophylaxis of organ rejection in patients receiving renal transplants. It is recommended that sirolimus be used in a regimen with cyclosporine and corticosteroids.

  • ATC: L04AA10
  • PubChem: 5284616
  • DrugBank: DB00877 (APRD00178, DB02439)
  • Formula: C24H32O4S
  • Molecular Mass: 914.1719
  • Synonyms: (-)-Rapamycin Rapamycin
  • SMILES: [H][C@@]1(C[C@H](C)[C@]2([H])CC(=O)[C@H](C)C=C(C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)C=CC=CC=C(C)[C@H](C[C@]3([H])CC[C@@H](C)[C@@](O)(O3)C(=O)C(=O)N3CCCC[C@@]3([H])C(=O)O2)OC)CC[C@@H](O)[C@@H](C1)OC
  • AHFS Code: 32:00.0
  • InChl: QFJCIRLUMZQUOT-KLHQEZAJSA-N
  • General Reference:

    1. Pritchard DI: Sourcing a chemical succession for cyclosporin from parasites and human pathogens. Drug Discov Today. 2005 May 15;10(10):688-91. Pubmed
    2. Shuchman M: Trading restenosis for thrombosis? New questions about drug-eluting stents. N Engl J Med. 2006 Nov 9;355(19):1949-52. Pubmed
    3. Sun SY, Rosenberg LM, Wang X, Zhou Z, Yue P, Fu H, Khuri FR: Activation of Akt and eIF4E survival pathways by rapamycin-mediated mammalian target of rapamycin inhibition. Cancer Res. 2005 Aug 15;65(16):7052-8. Pubmed
    4. Chan S: Targeting the mammalian target of rapamycin (mTOR): a new approach to treating cancer. Br J Cancer. 2004 Oct 18;91(8):1420-4. Pubmed
    5. Graziani EI: Recent advances in the chemistry, biosynthesis and pharmacology of rapamycin analogs. Nat Prod Rep. 2009 May;26(5):602-9. Epub 2009 Mar 5. Pubmed

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

API’s From Quality Manufacturers:

  • Streamlined API supply towards initial research stages as well as larger quantities of cGMP material for clinical trials and product commercialization
  • Premium quality GMP certified and fully accredited API manufacturing plants

 

  • Technical packages as well as access to filed DMF,
    ASMF or CEP (subject to availability)
  • Regulatory and technical assistance towards any
    submission type based on specific customer requirements